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WO2024094329A1 - Blister-packaged capsule preparation containing isavuconazonium sulfate - Google Patents

Blister-packaged capsule preparation containing isavuconazonium sulfate Download PDF

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Publication number
WO2024094329A1
WO2024094329A1 PCT/EP2023/063704 EP2023063704W WO2024094329A1 WO 2024094329 A1 WO2024094329 A1 WO 2024094329A1 EP 2023063704 W EP2023063704 W EP 2023063704W WO 2024094329 A1 WO2024094329 A1 WO 2024094329A1
Authority
WO
WIPO (PCT)
Prior art keywords
capsule
capsule preparation
preparation
blister
packaged
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/EP2023/063704
Other languages
French (fr)
Inventor
Steffen HÖFT
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Basilea Pharmaceutica International Ag Allschwil
Original Assignee
Basilea Pharmaceutica International Ag Allschwil
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from JP2022175640A external-priority patent/JP7527333B2/en
Application filed by Basilea Pharmaceutica International Ag Allschwil filed Critical Basilea Pharmaceutica International Ag Allschwil
Publication of WO2024094329A1 publication Critical patent/WO2024094329A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B65—CONVEYING; PACKING; STORING; HANDLING THIN OR FILAMENTARY MATERIAL
    • B65D—CONTAINERS FOR STORAGE OR TRANSPORT OF ARTICLES OR MATERIALS, e.g. BAGS, BARRELS, BOTTLES, BOXES, CANS, CARTONS, CRATES, DRUMS, JARS, TANKS, HOPPERS, FORWARDING CONTAINERS; ACCESSORIES, CLOSURES, OR FITTINGS THEREFOR; PACKAGING ELEMENTS; PACKAGES
    • B65D75/00—Packages comprising articles or materials partially or wholly enclosed in strips, sheets, blanks, tubes or webs of flexible sheet material, e.g. in folded wrappers
    • B65D75/28—Articles or materials wholly enclosed in composite wrappers, i.e. wrappers formed by associating or interconnecting two or more sheets or blanks
    • B65D75/30—Articles or materials enclosed between two opposed sheets or blanks having their margins united, e.g. by pressure-sensitive adhesive, crimping, heat-sealing, or welding
    • B65D75/32—Articles or materials enclosed between two opposed sheets or blanks having their margins united, e.g. by pressure-sensitive adhesive, crimping, heat-sealing, or welding one or both sheets or blanks being recessed to accommodate contents
    • B65D75/325—Articles or materials enclosed between two opposed sheets or blanks having their margins united, e.g. by pressure-sensitive adhesive, crimping, heat-sealing, or welding one or both sheets or blanks being recessed to accommodate contents one sheet being recessed, and the other being a flat not- rigid sheet, e.g. puncturable or peelable foil
    • B65D75/327—Articles or materials enclosed between two opposed sheets or blanks having their margins united, e.g. by pressure-sensitive adhesive, crimping, heat-sealing, or welding one or both sheets or blanks being recessed to accommodate contents one sheet being recessed, and the other being a flat not- rigid sheet, e.g. puncturable or peelable foil and forming several compartments
    • B65D75/328—Articles or materials enclosed between two opposed sheets or blanks having their margins united, e.g. by pressure-sensitive adhesive, crimping, heat-sealing, or welding one or both sheets or blanks being recessed to accommodate contents one sheet being recessed, and the other being a flat not- rigid sheet, e.g. puncturable or peelable foil and forming several compartments the compartments being interconnected, e.g. by small channels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61J—CONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J1/00—Containers specially adapted for medical or pharmaceutical purposes
    • A61J1/03—Containers specially adapted for medical or pharmaceutical purposes for pills or tablets
    • A61J1/035—Blister-type containers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4808—Preparations in capsules, e.g. of gelatin, of chocolate characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B65—CONVEYING; PACKING; STORING; HANDLING THIN OR FILAMENTARY MATERIAL
    • B65D—CONTAINERS FOR STORAGE OR TRANSPORT OF ARTICLES OR MATERIALS, e.g. BAGS, BARRELS, BOTTLES, BOXES, CANS, CARTONS, CRATES, DRUMS, JARS, TANKS, HOPPERS, FORWARDING CONTAINERS; ACCESSORIES, CLOSURES, OR FITTINGS THEREFOR; PACKAGING ELEMENTS; PACKAGES
    • B65D81/00—Containers, packaging elements, or packages, for contents presenting particular transport or storage problems, or adapted to be used for non-packaging purposes after removal of contents
    • B65D81/24—Adaptations for preventing deterioration or decay of contents; Applications to the container or packaging material of food preservatives, fungicides, pesticides or animal repellants
    • B65D81/26—Adaptations for preventing deterioration or decay of contents; Applications to the container or packaging material of food preservatives, fungicides, pesticides or animal repellants with provision for draining away, or absorbing, or removing by ventilation, fluids, e.g. exuded by contents; Applications of corrosion inhibitors or desiccators
    • B65D81/266—Adaptations for preventing deterioration or decay of contents; Applications to the container or packaging material of food preservatives, fungicides, pesticides or animal repellants with provision for draining away, or absorbing, or removing by ventilation, fluids, e.g. exuded by contents; Applications of corrosion inhibitors or desiccators for absorbing gases, e.g. oxygen absorbers or desiccants
    • B65D81/268—Adaptations for preventing deterioration or decay of contents; Applications to the container or packaging material of food preservatives, fungicides, pesticides or animal repellants with provision for draining away, or absorbing, or removing by ventilation, fluids, e.g. exuded by contents; Applications of corrosion inhibitors or desiccators for absorbing gases, e.g. oxygen absorbers or desiccants the absorber being enclosed in a small pack, e.g. bag, included in the package
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds

Definitions

  • the present invention relates to a blister-packaged capsule preparation containing isavuconazonium sulfate.
  • Blister packaging is understood to be packaging resulting from molding a sheet of plastic or aluminum foil so as to make one or more depressions (sometimes referred to as pockets), placing a preparation therein, covering the openings with a plastic film or sheet, aluminum foil, or the like, and adhering or fixing the peripheral portions thereof. When the blister-packaged preparation is to be taken out, the film or foil is peeled off. Blister packaging is used for packaging capsules, tablets, and the like.
  • a press through pack (PTP) is known as one form of blister packaging that is commonly used in the field of medications.
  • a PTP comprises a container material in which pockets to be filled with contents such as tablets or capsules are formed, and a cover material (sometimes referred to as a lidding material), which is attached to the container material so as to seal the side thereof on which the pockets open.
  • a PTP by pressing a pocket portion so as to break through the cover material, with the contents that are accommodated therein, said contents can be taken out (Patent Document 2).
  • a blister pack provided with aluminum foil for both the container material and the lidding material is sometimes referred to as an aluminum blister pack.
  • aluminum blister packs have high barrier functions for the contents.
  • Aluminum blister packs are said to present the problem of a higher risk of dose loss/pill dropping than transparent PTPs, because the preparations, such as tablets and capsules cannot be seen in advance when these are opened (Non-Patent Document 2).
  • Peel-type blister packaging is sometimes adopted for low-hardness preparations that cannot withstand loads when being pushed out, but if this is used with aluminum blister packs, the dose may fly out when the aluminum foil is peeled off (Non-Patent Document 2).
  • packaging has also been developed in which the peel-type aluminum blister packaging is configured so that, after the aluminum foil serving as the lidding material is peeled off, a transparent film remains, and the contents can be taken out by pushing out with the contents in view (Non-Patent Document 2).
  • Non-Patent Documents 3 and 4 capsule preparations containing isavuconazonium sulfate have been used in clinical practice.
  • the preparations are packaged in aluminum blister packs, with seven doses of the capsule preparation packaged in one sheet (Non-Patent Documents 3 and 4).
  • the blister packaging for these preparations comprises two pockets for one capsule preparation, one pocket containing a desiccant and the other pocket containing the capsule preparation (Non-Patent Document 3).
  • Tear lines are provided in the cover material, corresponding to the two pockets, and by severing along a tear line, a blister pack containing one capsule preparation and one desiccant can be obtained (Non-Patent Document 3).
  • the cover material has a laminated structure, and the instructions indicate that, when the sheet at the cover material surface is peeled off (peeled away), the aluminum sheet is exposed, allowing the capsule preparation to be taken out (Non-Patent Document 3).
  • Capsules generally used for capsule preparations are classified into hard capsules and soft capsules. Hard capsules are generally further classified according to their size into 8 categories from large to small (No. 000, No. 00, No. 0, No. 1, No. 2, No. 3, No. 4, No. 5) (Non-Patent Document 1).
  • the size of the No. 3 capsule is listed as 5.8 mm (outer diameter) x 15.9 mm (total length after filling, i.e. overall closed length) (Non-Patent Document 7). Including the tolerances, the No. 3 capsule is listed as having a size of 5.83 ⁇ 0.06 mm (outer diameter) x 15.9 ⁇ 0.30 mm (total length after filling) (Non-Patent Document 7).
  • the aforementioned capsule preparation containing 186.3 mg of isavuconazonium sulfate (100 mg in terms of isavuconazole) has a length of 24.2 mm, which corresponds to a length between those of capsules No. 0 and No. 00, and thus differs from the No. 3 capsule, which has a total length of 15.9 mm.
  • the present invention provides a blister-packaged No. 3 capsule preparation containing isavuconazonium sulfate, which has excellent physical properties.
  • One aspect of the present invention is a blister-packaged capsule preparation containing isavuconazonium sulfate, which satisfies the following conditions (1) to (4):
  • the capsule used in the capsule preparation is Capsule Standard No. 3;
  • the major axis of a pocket containing the capsule preparation is 150 to 200% of the total length of 15.9 mm;
  • the minor axis of the pocket containing the capsule preparation is 295 to 345% of the outer diameter of 5.8 mm;
  • the height of the pocket containing the capsule preparation is 100 to 150% of the outer diameter of 5.8 mm.
  • One aspect of the present invention is a method for preventing decomposition of isavuconazonium sulfate during storage of a blister-packaged capsule preparation containing said isavuconazonium sulfate, characterized in that the capsule preparation is a capsule preparation that satisfies the aforementioned conditions (1) to (4).
  • One aspect of the present invention is a method for preventing an increase in water content in a blister-packaged capsule preparation containing isavuconazonium sulfate during storage of said preparation, characterized in that the capsule preparation is a capsule preparation that satisfies the aforementioned conditions (1) to (4).
  • One aspect of the present invention is a method for storing a blister-packaged capsule preparation containing isavuconazonium sulfate, characterized in that the capsule preparation satisfies the aforementioned conditions (1) to (4).
  • the present invention relates to the following aspects and embodiments and the like.
  • the capsule used in the capsule preparation is Capsule Standard No. 3;
  • the major axis of a pocket containing the capsule preparation is 170 to 180% of the total length of 15.9 mm;
  • the minor axis of the pocket containing the capsule preparation is 315 to 325% of the outer diameter of 5.8 mm;
  • the height of the pocket containing the capsule preparation is 105 to 115% of the outer diameter of 5.8 mm.
  • the capsule used in the capsule preparation is Capsule Standard No. 3;
  • the major axis of a pocket containing the capsule preparation is 165 to 185% of the total length of 15.9 mm;
  • the minor axis of the pocket containing the capsule preparation is 310 to 330% of the outer diameter of 5.8 mm;
  • the height of the pocket containing the capsule preparation is 100 to 120% of the outer diameter of 5.8 mm.
  • the capsule used in the capsule preparation is Capsule Standard No. 3;
  • the major axis of a pocket containing the capsule preparation is 165 to 185% of the total length of 15.9 mm;
  • the minor axis of the pocket containing the capsule preparation is 310 to 330% of the outer diameter of 5.8 mm;
  • the height of the pocket containing the capsule preparation is 100 to 120% of the outer diameter of 5.8 mm.
  • the capsule used in the capsule preparation is Capsule Standard No. 3;
  • the major axis of a pocket containing the capsule preparation is 165 to 185% of the total length of 15.9 mm;
  • the minor axis of the pocket containing the capsule preparation is 310 to 330% of the outer diameter of 5.8 mm;
  • the height of the pocket containing the capsule preparation is 100 to 120% of the outer diameter of 5.8 mm.
  • the capsule used in the capsule preparation is Capsule Standard No. 3;
  • the major axis of a pocket containing the capsule preparation is 165 to 185% of the total length of 15.9 mm;
  • the minor axis of the pocket containing the capsule preparation is 310 to 330% of the outer diameter of 5.8 mm;
  • the height of the pocket containing the capsule preparation is 100 to 120% of the outer diameter of 5.8 mm.
  • Figure 1 is a view showing one example of a capsule preparation of the present invention.
  • (1) indicates a blister pack
  • (2) indicates a pocket containing a capsule preparation
  • (3) indicates a pocket for storing a desiccant described hereafter
  • (4) indicates a capsule preparation
  • (5) indicates a desiccant for purposes of preventing degradation of the capsule preparation due to moisture, which is packaged together therewith
  • (a) indicates the minor axis
  • (b) indicates the major axis
  • c) indicates the height.
  • (2) and (3) are spatially connected.
  • isavuconazole means a compound represented by the following formula (I).
  • Isavuconazonium sulfate is a compound represented by the following formula (II). Isavuconazonium sulfate can be hydrolyzed in vivo to isavuconazole.
  • Isavuconazole or the prodrug thereof, isavuconazonium sulfate can be produced or prepared by methods that are known per se (Patent Document 1, Non-Patent Documents 3 and 4, and the like).
  • blister packaging is understood to be packaging resulting from molding a sheet of plastic or aluminum foil so as to make one or more depressions (sometimes referred to as pockets), placing a preparation therein, covering the openings with a plastic film or sheet, aluminum foil, or the like, and adhering or fixing the peripheral portions thereof.
  • Blister packaging is used for capsules, tablets, and the like.
  • the method for producing the blister pack is not particularly limited, and can be a conventional method (Non-Patent Document 6, etc.).
  • a PTP pack (PTP sheet) can be produced by using a PTP packaging machine (blister packaging machine) to continuously form a thermoplastic resin film into a predetermined shape, placing a solid preparation such as a capsule therein, and welding with a composite film, such as one including aluminum foil.
  • Materials used for the container material and the lidding material of the blister packaging are not particularly limited. Examples include polyvinyl chloride (PVC), polychlorotrifluoroethylene (PCTFE), non-oriented polypropylene (CPP), and polyethylene terephthalate (A-PET). Alternatively, this may be a laminate produced by laminating with aluminum foil or the like (Patent Document 3) and, for example, various films including a barrier layer (such as a barrier packaging material including an oxygen absorbing barrier layer between polypropylene resins) or an aluminum laminate film (sometimes referred to as an aluminum blister foil) can be used for the container material and the lidding material.
  • a barrier layer such as a barrier packaging material including an oxygen absorbing barrier layer between polypropylene resins
  • an aluminum laminate film sometimes referred to as an aluminum blister foil
  • packaging with an aluminum blister foil is preferred.
  • One feature of the present invention is the size of the pocket in the blister packaging.
  • the pocket provides space that can accommodate a No. 3 capsule (e.g. a Japanese Pharmacopoeia Capsule Standard No. 3 capsule preparation as defined in paragraph [0046]).
  • hard capsules are generally further classified according to their size into 8 categories from large to small (No. 000, No. 00, No. 0, No. 1, No. 2, No. 3, No. 4, No. 5) (Non-Patent
  • Non-Patent Document 7 The size of the No. 3 capsule is listed as 5.8 mm (outer diameter) x total length after filling (15.9 mm) (Non-Patent Document 7). Including the tolerances, the No. 3 capsule is listed as having a size of 5.83 ⁇ 0.06 mm (outer diameter) x 15.9 ⁇ 0.30 mm (total length after filling) (Non-Patent Document 7). Therefore, the pocket in the blister packaging of the present invention is of a size that can accommodate a hard capsule preparation (which is to say, a Japanese Pharmacopoeia Capsule Standard No. 3 capsule preparation) having a size of 5.8 mm (outer diameter) x total length after filling (15.9 mm).
  • a hard capsule preparation which is to say, a Japanese Pharmacopoeia Capsule Standard No. 3 capsule preparation
  • No. 3 capsule No. 3 capsule size
  • capsule size No. 3 no. 3
  • Capsule Standard No. 3 are synonymous with each other and refer to a hard capsule having the above-mentioned dimensions, i.e. 5.8 mm (outer diameter) x 15.9 mm (total length after filling), which preferably includes the above-mentioned tolerances. In terms of tolerances this means that the “No. 3 capsule”, “No. 3 capsule size”, “capsule size No. 3”, “No. 3” or “Capsule Standard No.
  • the capsule preparation is in conformity with hard capsule preparations as described in the Japanese Pharmacopeia, in particular the 18 th Edition dated 7 June 2021, i.e. it is not excluded by the description of capsule preparations in the Japanese Pharmacopeia, in particular the 18 th Edition dated 7 June 2021.
  • the terms “Japanese Pharmacopeia Capsule Standard No. 3” and “specified by Japanese Pharmacopeia Capsule Standard No. 3” refer to a hard capsule preparation of capsule size No.
  • the size of the pocket in the blister packaging of the present invention can be exemplified as follows.
  • the major axis of the pocket containing the capsule preparation is 150 to 200% of the total length of 15.9 mm (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3).
  • the minor axis of the pocket containing the capsule preparation is 295 to 345% of the outer diameter of 5.8 mm (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3).
  • the height of the pocket containing the capsule preparation is 100 to 150% of the outer diameter of 5.8 mm (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3).
  • the major axis of the pocket For example, 150 to 200% of the total capsule length of 15.9 mm, 160 to 190% of the total capsule length of 15.9 mm, 165 to 185% of the total capsule length of 15.9 mm, or 170 to 180% of the total capsule length of 15.9 mm can be mentioned as preferred for the major axis of the pocket.
  • the shape of that portion of the lidding material corresponding to the pocket accommodating one capsule preparation unit is generally rectangular or elliptical
  • the major axis of the pocket corresponds to the major axis of that rectangle or ellipse ( Figure 1). (“Total capsule length” is the total capsule length after filling.)
  • the minor axis of the pocket For example, 295 to 345% of the outer capsule diameter of 5.8 mm, 305 to 335% of the outer capsule diameter of 5.8 mm, 310 to 330% of the outer capsule diameter of 5.8 mm, or 315 to 325% of the outer capsule diameter of 5.8 mm can be mentioned as preferred for the minor axis of the pocket.
  • the shape of the portion of the lidding material corresponding to the pocket accommodating one capsule preparation unit is generally rectangular or elliptical
  • the minor axis of the pocket corresponds to the minor axis of that rectangle or ellipse ( Figure 1).
  • the height of the pocket for example, 100 to 150% of the outer capsule diameter of 5.8 mm, 100 to 130% of the outer capsule diameter of 5.8 mm, 100 to 120% of the outer capsule diameter of 5.8 mm, or 105 to 115% of the outer capsule diameter of 5.8 mm can be mentioned as preferred.
  • the height of the pocket means the distance from the lidding material corresponding to a pocket accommodating one unit of capsule preparation to the top of the pocket (see Figure 1).
  • the major axis of the pocket containing the capsule preparation is 170 to 180% of the total length of 15.9 mm (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3).
  • the minor axis of the pocket containing the capsule preparation is 315 to 325% of the outer diameter of 5.8 mm (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3).
  • the height of the pocket containing the capsule preparation is 105 to 115% of the outer diameter of 5.8 mm (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3).
  • Using the sizes described above as the size for the pocket in the blister pack can prevent an increase in water content in the capsule preparation accommodated therein during storage of said preparation.
  • using the sizes described above for the size of the pocket in the blister pack can prevent decomposition of the isavuconazonium sulfate in the capsule preparation accommodated therein during storage of said preparation.
  • the blister pack may have a further pocket containing a desiccant.
  • the pocket containing the capsule preparation and the pocket containing the desiccant are spatially connected.
  • the blister-packaged capsule preparation is a hard capsule (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3 (see paragraph [0046])).
  • the Japanese Pharmacopoeia which is sometimes also referred to as the Pharmacopoeia Law, is a nationally stipulated document published by the Ministry of Health, Labor and Welfare, which stipulates standards for the quality, purity, and strength of medications, and also lists methods for testing and determination of the efficacy of medications. Medications that meet said standards are sometimes referred to as "pharmaceutical products", and a list of these medications is also given in the Japanese Pharmacopoeia.
  • a capsule preparation is a preparation resulting from filling a capsule with a powdered or liquid medication or the like, or from encapsulating the same with a capsule membrane.
  • the former is sometimes referred to as a hard capsule, and the latter is sometimes referred to as a soft capsule.
  • capsules are preparations enclosed in capsules or wrapped with capsule bases, intended for oral administration. Capsules are classified into hard capsules and soft capsules. Capsules are usually prepared by the following methods. Coloring agents, preservatives, etc. may be added to the capsule bases.
  • Hard capsules A homogeneous mixture of active substance(s) with diluents and other suitable excipients, or granules or formed masses prepared by a suitable method, are fdled into capsule shells as they are or after slight compression.
  • Soft capsules Active substance(s) and suitable excipients (including solvents) are mixed, enclosed by a suitable capsule base such as gelatin plasticized by addition of glycerin, D-sorbitol, etc. and molded in a suitable shape and size.
  • a suitable capsule base such as gelatin plasticized by addition of glycerin, D-sorbitol, etc. and molded in a suitable shape and size.
  • capsules meet the requirements of Uniformity of Dosage Units as described at paragraph 6.02 and meet the requirements of Dissolution Test or Disintegration Test as described at paragraphs 6.10 and 6.09 respectively of the Japanese Pharmacopoeia 18 th Edition dated 7 June 2021.
  • Hard capsules are generally further classified according to their size into 8 categories from large to small (No. 000, No. 00, No. 0, No. 1, No. 2, No. 3, No. 4, No. 5) (Non-Patent Document 1).
  • the size of the No. 3 capsule is listed as 5.8 mm (outer diameter) x total length after filling (15.9 mm) (Non-Patent Document 7).
  • the No. 3 capsule is listed as having a size of 5.83 ⁇ 0.06 mm (outer diameter) x 15.9 ⁇ 0.30 mm (total length after filling) (Non-Patent Document 7).
  • the method for producing the capsule preparation is not particularly limited, and may be a conventional method.
  • capsule preparations can, for example, be produced by sieving various components such as active components, excipients, and disintegrants, then mixing, filling the mixture into capsules, and performing primary packaging such as blister packaging.
  • a blister-packaged preparation (sometimes simply referred to as a blister sheet) can also be subjected to secondary packaging in which this is packaged in an individual box and sealed.
  • the capsules can likewise be produced by production techniques that are known per se.
  • capsules can be produced by way of dissolving capsule starting materials (for example, gelatine, hypromellose, titanium oxide) and the like in purified water or the like and stirring to make a uniform jelly, uniformly depositing the jelly on mold pins, drying the jelly on the mold pins, cutting, and temporary joining.
  • Hard capsules may be made for example from hard gelatin or hydroxypropyl methylcellulose (HPMC). Both hard capsules and soft capsules are well known to the person skilled in the art and commercially available, such as the CapsugelTM range of capsules from Lonza, such as the VcapsTM and VcapsTM plus capsules.
  • the content of isavuconazonium sulfate contained in the hard capsule preparation is not particularly limited, but is exemplified by 10 to 200 mg, 30 to 150 mg, 50 to 100 mg, or 70 to 80 mg, and is preferably exemplified by 74.5 mg (40 mg in terms of isavuconazole).
  • preventing decomposition means preventing decreases in the content of isavuconazonium sulfate contained in the preparation in the course of storing the blister-packaged capsule preparation containing isavuconazonium sulfate according to the present invention, as compared to the content of isavuconazonium sulfate at the start of storage.
  • the content of isavuconazonium sulfate contained in the preparation can be measured by a method such as LC/MS/MS.
  • the storage conditions are not particularly limited, and refrigerated storage or room temperature storage may be used, and dark storage may also be used. Furthermore, in order to more clearly confirm changes over time in the content of isavuconazonium sulfate connected with undergoing storage, preparations can be stored under conditions adopted for long-term storage tests, accelerated tests, and severe tests, and changes in the preparations over time can be observed. These can, for example, be exemplified by storage conditions such as 25°C/60% relative humidity (RH) and 40°C/75% RH.
  • RH relative humidity
  • the period for which the preparation is stored is preferably 1 month or more, and 2 months or more, 3 months or more, or 6 months or more is preferred.
  • preventing an increase in water content means preventing an increase in water content contained in the filling composition of the preparation, the capsule, and/or the overall preparation, after the start of storage, in the course of storing the blister-packaged capsule preparation containing isavuconazonium sulfate according to the present invention, as compared to the water content contained in the filling composition of the preparation, the capsule, and/or the overall preparation at the start of storage.
  • a person skilled in the art can easily measure the water content of the filling composition of the preparation, capsule, or the overall preparation.
  • the measurement method is not particularly limited, this can, for example, be exemplified by the loss-on-drying test method and Karl Fischer method.
  • the storage conditions are not particularly limited, and refrigerated storage or room temperature storage may be used, and dark storage may also be used. Furthermore, in order to more clearly confirm changes in the water content, preparations can be stored under conditions generally adopted for long-term storage tests, accelerated tests, and severe tests, and changes in the preparations over time can be observed. These can, for example, be exemplified by storage conditions such as 25°C/60% RH and 40°C/75% RH.
  • the period for which the preparation is stored is preferably 1 month or more, and 2 months or more, 3 months or more, or 6 months or more is preferred. Furthermore, sometimes other modes for the period for which the preparation is stored may preferably be exemplified by 9 months or more, 12 months or more, 18 months or more, 24 months or more, or 30 months or more.
  • the capsule preparation of the present invention is preferably stored in the state resulting from primary packaging in an aluminum blister pack.
  • a desiccant together therewith for the purpose of reducing the effects of moisture in the air on the preparation.
  • the type of desiccants is not particularly limited, this can, for example, be exemplified by silica gel, calcium oxide (quicklime), and silica-alumina gel-based compounds (montmorillonite, and the like).
  • the amount of desiccant may be 10% or more, preferably 20% or more, 30% or more, or 50% or more of the content of isavuconazonium sulfate in the preparation.
  • the capsule preparation of the present invention can be secondarily packaged in an individual box, polyethylene bag, or the like, and it is preferable to enclose a desiccant in the secondary packaging as well.
  • the capsule preparation of the present invention may be stored at room temperature but is preferably stored refrigerated.
  • the capsule preparation of the present invention is preferably stored in an environment with low air humidity and in a dark room.
  • the period for which the preparation is stored is not particularly limited, this is preferably 1 month or more, and 2 months or more, 3 months or more, or 6 months or more is preferred. Furthermore, sometimes other modes for the period for which the preparation is stored may preferably be exemplified by 9 months or more, 12 months or more, 18 months or more, 24 months or more, or 30 months or more.
  • the capsule preparation of the present invention can be used, for example, as a pharmaceutical preparation for treating fungal infections. That is to say, among other uses, by administering the preparation of the present invention to patients with fungal infections, it is possible to treat fungal infections.
  • the administrative route, frequency of administration, the dose, and the subject of administration can be determined by a physician or the like.
  • the blister-packaged capsule preparation containing isavuconazonium sulfate, of the invention satisfies the following conditions (1) to (4):
  • the capsule used in the capsule preparation is Japanese Pharmacopoeia Capsule Standard No. 3;
  • the major axis of a pocket containing the capsule preparation is 150 to 200% of the total length of 15.9 mm specified by Japanese Pharmacopoeia Capsule Standard No. 3;
  • the minor axis of the pocket containing the capsule preparation is 295 to 345% of the outer diameter of 5.8 mm specified by Japanese Pharmacopoeia Capsule Standard No. 3;
  • the height of the pocket containing the capsule preparation is 100 to 150% of the outer diameter of 5.8 mm specified by Japanese Pharmacopoeia Capsule Standard No. 3; wherein preferred dimensions of the pocket containing the capsule preparation are as described in paragraphs [0049], [0050] and [0051],
  • the blister-packaged capsule preparation containing isavuconazonium sulfate of the invention satisfies the following conditions (1) to (4):
  • the capsule used in the capsule preparation is of Japanese Pharmacopoeia Capsule Standard No. 3;
  • the major axis of a pocket containing the capsule preparation is 170 to 180% of the total length of 15.9 mm specified by Japanese Pharmacopoeia Capsule Standard No. 3;
  • the minor axis of the pocket containing the capsule preparation is 315 to 325% of the outer diameter of 5.8 mm specified by Japanese Pharmacopoeia Capsule Standard No. 3;
  • the height of the pocket containing the capsule preparation is 105 to 115% of the outer diameter of 5.8 mm specified by Japanese Pharmacopoeia Capsule Standard No. 3.
  • Capsule Preparation 1 containing isavuconazonium sulfate was produced by a method known per se.
  • the various components filled into the No. 3 capsules were as shown in Table 1 above, and the No. 3 capsule itself was produced using the components shown in Table 2, by way of a conventional method.
  • Aluminum blister packaging was performed in a mode in which seven doses of the same preparation were packaged in one sheet. As shown in Figure 1, this pack was structured such that one dose of desiccant (25 mg) was packaged together with one dose of this preparation. That is to say, the structure was such that a pocket (recess) containing one dose of this preparation and a pocket (recess) containing one dose of the desiccant are spatially connected.
  • the aluminum blister pack was produced by a conventional method.
  • the major axis of the pocket containing this preparation was 177% of the total length of 15.9 mm .
  • the minor axis of this pocket was 319% of the outer diameter of 5.8 mm .
  • the height of this pocket was 108% of the outer diameter of 5.8 mm specified by No. 3.
  • the Capsule Preparation 1 produced in Example 1 was stored under conditions of 25°C/60% RH for 6 months.
  • the content of isavuconazonium sulfate contained in the preparation was measured at the start of storage and 6 months after the start of storage.
  • a relative value (%) with respect to the theoretical isavuconazonium sulfate content of 74.5 mg was used for the content.
  • Measurement of isavuconazonium sulfate content was carried out using a validated high-performance liquid chromatography (HPLC) method.
  • the decomposition rate is defined as the value (%) obtained by subtracting the isavuconazonium sulfate content after 6 months of storage from the isavuconazonium sulfate content at the start of storage, dividing the result by the isavuconazonium sulfate content at the start of storage, and multiplying by 100.
  • the Capsule Preparation 1 Surprisingly, with the Capsule Preparation 1, it was found that decomposition of isavuconazonium sulfate during storage was found to be lower as compared with Capsule Preparation 2.
  • Capsule Preparation 2 A capsule preparation containing isavuconazonium sulfate (Capsule Preparation 2) was produced by a method known per se. Here, the various components filled into the No. 3 capsules were as shown in Table 1 above, and the capsule itself was produced using the components shown in Table 2, by way of a conventional method. Capsule Preparation 2 was identical to Capsule Preparation 1.
  • Aluminum blister packaging was performed in a mode in which seven doses of the same preparation were packaged in one sheet. As shown in Figure 1, this pack was structured such that one dose of desiccant (25 mg) was packaged together with one dose of this preparation. That is to say, the structure was such that a pocket (recess) containing one dose of this preparation and a pocket (recess) containing one dose of the desiccant were spatially connected.
  • the aluminum blister pack was produced by a conventional method.
  • the capsule preparation of the present invention exhibits excellent physical properties.
  • the present invention is extremely useful in the pharmaceutical industry.
  • Patent Document 1 JP 3787307 B
  • Patent Document 2 JP 5727972 B
  • Patent Document 3 JP 2019-135090 A
  • Non-Patent Document 1 Matsuyoshi & Co., Ltd.; online; retrieved December 9, 2021; internet ⁇ URL: https://www.matsuyoshi.co.jp/catalog-pdf/19/19-7805-00.pdf>
  • Non-Patent Document 2 Shionogi & Co., Ltd.; online; retrieved December 9, 2021; internet ⁇ URL: https://www.shionogi-ph.co.jp/news/2020/ll/1109.html>
  • Non-Patent Document 3 CRESEMBA® (isavuconazonium sulfate) 186 mg capsules PATIENT
  • Non-Patent Document 4 CRESEMBA® pack insert (2015)
  • Non-Patent Document 5 PRODUCT MONOGRAPH INCLUDING PATIENT MEDICATION INFORMATION ' 'CRESEMBATM. AVIR Pharma Inc. (2018)
  • Non-Patent Document 6 CKD Technical Journal (2017) Vol. 3, pp. 2 to 7
  • Non-Patent Document 7 Technical Reference File VcapsTM Capsules

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Abstract

The present invention provides a blister-packaged No. 3 capsule preparation containing isavuconazonium sulfate, which has excellent physical properties. The preparation satisfies the following conditions (1) to (4): (1) the capsule used in the capsule preparation is Capsule Standard No. 3; (2) the major axis of a pocket containing the capsule preparation is 150 to 200% of the total length of 15.9 mm; (3) the minor axis of the pocket containing the capsule preparation is 295 to 345% of the outer diameter of 5.8 mm; and (4) the height of the pocket containing the capsule preparation is 100 to 150% of the outer diameter of 5.8 mm.

Description

BLISTER-PACKAGED CAPSULE PREPARATION CONTAINING
ISAVUCONAZONIUM SULFATE
Technical Field
[0001] The present invention relates to a blister-packaged capsule preparation containing isavuconazonium sulfate.
Background Technology
[0002] Some medications are affected by moisture, light, and the like, and thus medications are often packaged in an inner bag. Blister packaging is commonly used as the inner bag. Inner bags that are in direct contact with the medication are sometimes referred to as primary packaging.
[0003] Blister packaging is understood to be packaging resulting from molding a sheet of plastic or aluminum foil so as to make one or more depressions (sometimes referred to as pockets), placing a preparation therein, covering the openings with a plastic film or sheet, aluminum foil, or the like, and adhering or fixing the peripheral portions thereof. When the blister-packaged preparation is to be taken out, the film or foil is peeled off. Blister packaging is used for packaging capsules, tablets, and the like. [0004] A press through pack (PTP) is known as one form of blister packaging that is commonly used in the field of medications. A PTP comprises a container material in which pockets to be filled with contents such as tablets or capsules are formed, and a cover material (sometimes referred to as a lidding material), which is attached to the container material so as to seal the side thereof on which the pockets open. With a PTP, by pressing a pocket portion so as to break through the cover material, with the contents that are accommodated therein, said contents can be taken out (Patent Document 2).
[0005] A blister pack provided with aluminum foil for both the container material and the lidding material is sometimes referred to as an aluminum blister pack. In general, aluminum blister packs have high barrier functions for the contents.
[0006] Aluminum blister packs are said to present the problem of a higher risk of dose loss/pill dropping than transparent PTPs, because the preparations, such as tablets and capsules cannot be seen in advance when these are opened (Non-Patent Document 2). Peel-type blister packaging is sometimes adopted for low-hardness preparations that cannot withstand loads when being pushed out, but if this is used with aluminum blister packs, the dose may fly out when the aluminum foil is peeled off (Non-Patent Document 2). Thus, packaging has also been developed in which the peel-type aluminum blister packaging is configured so that, after the aluminum foil serving as the lidding material is peeled off, a transparent film remains, and the contents can be taken out by pushing out with the contents in view (Non-Patent Document 2).
[0007] Meanwhile, capsule preparations containing isavuconazonium sulfate have been used in clinical practice (Non-Patent Documents 3 and 4). The preparations are packaged in aluminum blister packs, with seven doses of the capsule preparation packaged in one sheet (Non-Patent Documents 3 and 4).
[0008] The blister packaging for these preparations comprises two pockets for one capsule preparation, one pocket containing a desiccant and the other pocket containing the capsule preparation (Non-Patent Document 3). Tear lines are provided in the cover material, corresponding to the two pockets, and by severing along a tear line, a blister pack containing one capsule preparation and one desiccant can be obtained (Non-Patent Document 3). The cover material has a laminated structure, and the instructions indicate that, when the sheet at the cover material surface is peeled off (peeled away), the aluminum sheet is exposed, allowing the capsule preparation to be taken out (Non-Patent Document 3).
[0009] It has been reported that a capsule preparation containing 186.3 mg of isavuconazonium sulfate (100 mg in terms of isavuconazole) has a length of 24.2 mm (Non-Patent Document 5).
[0010] Capsules generally used for capsule preparations are classified into hard capsules and soft capsules. Hard capsules are generally further classified according to their size into 8 categories from large to small (No. 000, No. 00, No. 0, No. 1, No. 2, No. 3, No. 4, No. 5) (Non-Patent Document 1).
[0011] The size of the No. 3 capsule is listed as 5.8 mm (outer diameter) x 15.9 mm (total length after filling, i.e. overall closed length) (Non-Patent Document 7). Including the tolerances, the No. 3 capsule is listed as having a size of 5.83 ± 0.06 mm (outer diameter) x 15.9 ± 0.30 mm (total length after filling) (Non-Patent Document 7).
[0012] The aforementioned capsule preparation containing 186.3 mg of isavuconazonium sulfate (100 mg in terms of isavuconazole) has a length of 24.2 mm, which corresponds to a length between those of capsules No. 0 and No. 00, and thus differs from the No. 3 capsule, which has a total length of 15.9 mm.
[0013] The manner in which capsule preparations containing isavuconazonium sulfate filled into No. 3 capsules is affected by the specifications for blister packaging and the like is completely unknown.
[0014] The present invention provides a blister-packaged No. 3 capsule preparation containing isavuconazonium sulfate, which has excellent physical properties.
Summary of the Invention
[0015] One aspect of the present invention is a blister-packaged capsule preparation containing isavuconazonium sulfate, which satisfies the following conditions (1) to (4):
(1) the capsule used in the capsule preparation is Capsule Standard No. 3;
(2) the major axis of a pocket containing the capsule preparation is 150 to 200% of the total length of 15.9 mm;
(3) the minor axis of the pocket containing the capsule preparation is 295 to 345% of the outer diameter of 5.8 mm; and
(4) the height of the pocket containing the capsule preparation is 100 to 150% of the outer diameter of 5.8 mm.
[0016] One aspect of the present invention is a method for preventing decomposition of isavuconazonium sulfate during storage of a blister-packaged capsule preparation containing said isavuconazonium sulfate, characterized in that the capsule preparation is a capsule preparation that satisfies the aforementioned conditions (1) to (4).
[0017] One aspect of the present invention is a method for preventing an increase in water content in a blister-packaged capsule preparation containing isavuconazonium sulfate during storage of said preparation, characterized in that the capsule preparation is a capsule preparation that satisfies the aforementioned conditions (1) to (4).
[0018] One aspect of the present invention is a method for storing a blister-packaged capsule preparation containing isavuconazonium sulfate, characterized in that the capsule preparation satisfies the aforementioned conditions (1) to (4).
[0019] Furthermore, the present invention relates to the following aspects and embodiments and the like.
[0020] Capsule preparation according to paragraph [0015], wherein the blister pack is an aluminum blister pack.
[0021] Methods according to any of paragraphs [0016], [0017] and [0018], wherein the blister pack is an aluminum blister pack.
[0022] Blister-packaged capsule preparation containing isavuconazonium sulfate, which satisfies the following conditions (1) to (4):
(1) the capsule used in the capsule preparation is Capsule Standard No. 3;
(2) the major axis of a pocket containing the capsule preparation is 170 to 180% of the total length of 15.9 mm;
(3) the minor axis of the pocket containing the capsule preparation is 315 to 325% of the outer diameter of 5.8 mm; and
(4) the height of the pocket containing the capsule preparation is 105 to 115% of the outer diameter of 5.8 mm.
[0023] Capsule preparation according to paragraph [0022], wherein the blister pack is an aluminum blister pack.
[0024] Method for preventing decomposition of isavuconazonium sulfate during storage of a blister- packaged capsule preparation containing said isavuconazonium sulfate, characterized in that the capsule preparation is a capsule preparation that satisfies the aforementioned conditions (1) to (4) in paragraph [0022],
[0025] Method for preventing an increase in water content in a blister-packaged capsule preparation containing isavuconazonium sulfate during storage of said preparation, characterized in that the capsule preparation is a capsule preparation that satisfies the aforementioned conditions (1) to (4) in paragraph [0022],
[0026] Method for storing a blister-packaged capsule preparation containing isavuconazonium sulfate, characterized in that the capsule preparation satisfies the aforementioned conditions (1) to (4) in paragraph [0022],
[0027] Methods according to any of paragraphs [0024], [0025] and [0026], wherein the blister pack is an aluminum blister pack.
[0028] [1] Blister-packaged capsule preparation containing isavuconazonium sulfate, which satisfies the following conditions (1) to (4):
(1) the capsule used in the capsule preparation is Capsule Standard No. 3;
(2) the major axis of a pocket containing the capsule preparation is 165 to 185% of the total length of 15.9 mm;
(3) the minor axis of the pocket containing the capsule preparation is 310 to 330% of the outer diameter of 5.8 mm; and
(4) the height of the pocket containing the capsule preparation is 100 to 120% of the outer diameter of 5.8 mm.
[0029] [2] Capsule preparation according to the aforementioned [1], wherein the blister pack is an aluminum blister pack.
[0030] [3] Method for preventing decomposition of isavuconazonium sulfate during storage of a blisterpackaged capsule preparation containing said isavuconazonium sulfate, characterized in that the capsule preparation is a capsule preparation that satisfies the following conditions (1) to (4):
(1) the capsule used in the capsule preparation is Capsule Standard No. 3;
(2) the major axis of a pocket containing the capsule preparation is 165 to 185% of the total length of 15.9 mm;
(3) the minor axis of the pocket containing the capsule preparation is 310 to 330% of the outer diameter of 5.8 mm; and
(4) the height of the pocket containing the capsule preparation is 100 to 120% of the outer diameter of 5.8 mm.
[0031] [4] Method for preventing an increase in water content in a blister-packaged capsule preparation containing isavuconazonium sulfate during storage of said preparation, characterized in that the capsule preparation is a capsule preparation that satisfies the following conditions (1) to (4):
(1) the capsule used in the capsule preparation is Capsule Standard No. 3;
(2) the major axis of a pocket containing the capsule preparation is 165 to 185% of the total length of 15.9 mm;
(3) the minor axis of the pocket containing the capsule preparation is 310 to 330% of the outer diameter of 5.8 mm; and
(4) the height of the pocket containing the capsule preparation is 100 to 120% of the outer diameter of 5.8 mm.
[0032] [5] Method for storing a blister-packaged capsule preparation containing isavuconazonium sulfate, characterized in that the capsule preparation satisfies the following conditions (1) to (4):
(1) the capsule used in the capsule preparation is Capsule Standard No. 3;
(2) the major axis of a pocket containing the capsule preparation is 165 to 185% of the total length of 15.9 mm;
(3) the minor axis of the pocket containing the capsule preparation is 310 to 330% of the outer diameter of 5.8 mm; and
(4) the height of the pocket containing the capsule preparation is 100 to 120% of the outer diameter of 5.8 mm.
[0033] [6] Methods according to any of the aforementioned [3] to [5], wherein the blister pack is an aluminum blister pack.
Effects of the Invention
[0034] With the present invention it is possible to provide a blister-packaged No. 3 capsule preparation containing isavuconazonium sulfate, which has excellent physical properties.
Brief Description of the Drawings
[0035] Figure 1 is a view showing one example of a capsule preparation of the present invention. (1) indicates a blister pack, (2) indicates a pocket containing a capsule preparation, (3) indicates a pocket for storing a desiccant described hereafter, (4) indicates a capsule preparation, and (5) indicates a desiccant for purposes of preventing degradation of the capsule preparation due to moisture, which is packaged together therewith, (a) indicates the minor axis, (b) indicates the major axis (c) indicates the height. (2) and (3) are spatially connected. Detailed Description of the Invention
[0036] Hereinafter, the present invention will be described in detail based on specific modes of embodiment. However, the present invention is not restricted to the following modes of embodiment, and can be embodied in any mode within a scope that does not depart from the gist of the present invention.
[0037] 1, Active Component In the present invention, isavuconazole means a compound represented by the following formula (I).
[0038]
Figure imgf000009_0001
[0039] The CAS number for isavuconazole is 241479-67-4. In the United States, preparations containing isavuconazonium sulfate, a prodrug of isavuconazole, are in clinical use (Non-Patent Documents 3 and 4). Isavuconazonium sulfate is a compound represented by the following formula (II). Isavuconazonium sulfate can be hydrolyzed in vivo to isavuconazole.
[0040]
Figure imgf000009_0002
( II ) [0041] Isavuconazole or the prodrug thereof, isavuconazonium sulfate, can be produced or prepared by methods that are known per se (Patent Document 1, Non-Patent Documents 3 and 4, and the like).
[0042] 2, Blister Packaging
In the present invention, blister packaging is understood to be packaging resulting from molding a sheet of plastic or aluminum foil so as to make one or more depressions (sometimes referred to as pockets), placing a preparation therein, covering the openings with a plastic film or sheet, aluminum foil, or the like, and adhering or fixing the peripheral portions thereof. When the blister-packaged preparation is to be taken out, the film or foil is peeled off. Blister packaging is used for capsules, tablets, and the like.
[0043] The method for producing the blister pack is not particularly limited, and can be a conventional method (Non-Patent Document 6, etc.). Here, taking PTP packaging as an example of a case in which a thermoplastic resin is used for the container material, a PTP pack (PTP sheet) can be produced by using a PTP packaging machine (blister packaging machine) to continuously form a thermoplastic resin film into a predetermined shape, placing a solid preparation such as a capsule therein, and welding with a composite film, such as one including aluminum foil.
[0044] Materials used for the container material and the lidding material of the blister packaging are not particularly limited. Examples include polyvinyl chloride (PVC), polychlorotrifluoroethylene (PCTFE), non-oriented polypropylene (CPP), and polyethylene terephthalate (A-PET). Alternatively, this may be a laminate produced by laminating with aluminum foil or the like (Patent Document 3) and, for example, various films including a barrier layer (such as a barrier packaging material including an oxygen absorbing barrier layer between polypropylene resins) or an aluminum laminate film (sometimes referred to as an aluminum blister foil) can be used for the container material and the lidding material. In view of the physical properties of isavuconazonium sulfate, packaging with an aluminum blister foil is preferred. [0045] One feature of the present invention is the size of the pocket in the blister packaging. The pocket provides space that can accommodate a No. 3 capsule (e.g. a Japanese Pharmacopoeia Capsule Standard No. 3 capsule preparation as defined in paragraph [0046]).
[0046] As mentioned above, hard capsules are generally further classified according to their size into 8 categories from large to small (No. 000, No. 00, No. 0, No. 1, No. 2, No. 3, No. 4, No. 5) (Non-Patent
Document 1). The size of the No. 3 capsule is listed as 5.8 mm (outer diameter) x total length after filling (15.9 mm) (Non-Patent Document 7). Including the tolerances, the No. 3 capsule is listed as having a size of 5.83 ± 0.06 mm (outer diameter) x 15.9 ± 0.30 mm (total length after filling) (Non-Patent Document 7). Therefore, the pocket in the blister packaging of the present invention is of a size that can accommodate a hard capsule preparation (which is to say, a Japanese Pharmacopoeia Capsule Standard No. 3 capsule preparation) having a size of 5.8 mm (outer diameter) x total length after filling (15.9 mm). For avoidance of any doubt, and as defined herein, the terms “No. 3 capsule”, “No. 3 capsule size”, “capsule size No. 3”, “No. 3” and “Capsule Standard No. 3” are synonymous with each other and refer to a hard capsule having the above-mentioned dimensions, i.e. 5.8 mm (outer diameter) x 15.9 mm (total length after filling), which preferably includes the above-mentioned tolerances. In terms of tolerances this means that the “No. 3 capsule”, “No. 3 capsule size”, “capsule size No. 3”, “No. 3” or “Capsule Standard No. 3” is a hard capsule having a size of 5.83 ± 0.06 mm (outer diameter) x 15.9 ± 0.30 mm (total length after filling). In some embodiments, the capsule preparation is in conformity with hard capsule preparations as described in the Japanese Pharmacopeia, in particular the 18th Edition dated 7 June 2021, i.e. it is not excluded by the description of capsule preparations in the Japanese Pharmacopeia, in particular the 18th Edition dated 7 June 2021. The terms “Japanese Pharmacopeia Capsule Standard No. 3” and “specified by Japanese Pharmacopeia Capsule Standard No. 3” refer to a hard capsule preparation of capsule size No. 3 which is in conformity with capsule preparations as described in the Japanese Pharmacopeia, in particular Japanese the 18th Edition dated 7 June 2021, i.e. it is not excluded from the description of hard capsule preparations in the Japanese Pharmacopeia, in particular the 18th Edition dated 7 June 2021.
[0047] The size of the pocket in the blister packaging of the present invention can be exemplified as follows.
[0048] (1) The major axis of the pocket containing the capsule preparation is 150 to 200% of the total length of 15.9 mm (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3). (2) The minor axis of the pocket containing the capsule preparation is 295 to 345% of the outer diameter of 5.8 mm (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3).
(3) The height of the pocket containing the capsule preparation is 100 to 150% of the outer diameter of 5.8 mm (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3).
[0049] For example, 150 to 200% of the total capsule length of 15.9 mm, 160 to 190% of the total capsule length of 15.9 mm, 165 to 185% of the total capsule length of 15.9 mm, or 170 to 180% of the total capsule length of 15.9 mm can be mentioned as preferred for the major axis of the pocket. Where the shape of that portion of the lidding material corresponding to the pocket accommodating one capsule preparation unit is generally rectangular or elliptical, the major axis of the pocket corresponds to the major axis of that rectangle or ellipse (Figure 1). (“Total capsule length” is the total capsule length after filling.)
[0050] For example, 295 to 345% of the outer capsule diameter of 5.8 mm, 305 to 335% of the outer capsule diameter of 5.8 mm, 310 to 330% of the outer capsule diameter of 5.8 mm, or 315 to 325% of the outer capsule diameter of 5.8 mm can be mentioned as preferred for the minor axis of the pocket. Where the shape of the portion of the lidding material corresponding to the pocket accommodating one capsule preparation unit is generally rectangular or elliptical, the minor axis of the pocket corresponds to the minor axis of that rectangle or ellipse (Figure 1).
[0051] In terms of the height of the pocket, for example, 100 to 150% of the outer capsule diameter of 5.8 mm, 100 to 130% of the outer capsule diameter of 5.8 mm, 100 to 120% of the outer capsule diameter of 5.8 mm, or 105 to 115% of the outer capsule diameter of 5.8 mm can be mentioned as preferred. The height of the pocket means the distance from the lidding material corresponding to a pocket accommodating one unit of capsule preparation to the top of the pocket (see Figure 1).
[0052] For example, (1) The major axis of the pocket containing the capsule preparation is 170 to 180% of the total length of 15.9 mm (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3).
(2) The minor axis of the pocket containing the capsule preparation is 315 to 325% of the outer diameter of 5.8 mm (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3). (3) The height of the pocket containing the capsule preparation is 105 to 115% of the outer diameter of 5.8 mm (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3).
[0053] Using the sizes described above as the size for the pocket in the blister pack can prevent an increase in water content in the capsule preparation accommodated therein during storage of said preparation. Alternatively, using the sizes described above for the size of the pocket in the blister pack can prevent decomposition of the isavuconazonium sulfate in the capsule preparation accommodated therein during storage of said preparation.
[0054] In addition to the pocket containing the capsule preparation, the blister pack may have a further pocket containing a desiccant. Preferably, the pocket containing the capsule preparation and the pocket containing the desiccant are spatially connected.
[0055] 3 , Capsule Preparation
One feature of the present invention is that the blister-packaged capsule preparation is a hard capsule (e.g. specified by Japanese Pharmacopoeia Capsule Standard No. 3 (see paragraph [0046])).
[0056] The Japanese Pharmacopoeia, which is sometimes also referred to as the Pharmacopoeia Law, is a nationally stipulated document published by the Ministry of Health, Labor and Welfare, which stipulates standards for the quality, purity, and strength of medications, and also lists methods for testing and determination of the efficacy of medications. Medications that meet said standards are sometimes referred to as "pharmaceutical products", and a list of these medications is also given in the Japanese Pharmacopoeia.
[0057] A capsule preparation is a preparation resulting from filling a capsule with a powdered or liquid medication or the like, or from encapsulating the same with a capsule membrane. The former is sometimes referred to as a hard capsule, and the latter is sometimes referred to as a soft capsule.
[0058] According to the Japanese Pharmacopoeia 18th Edition capsules are preparations enclosed in capsules or wrapped with capsule bases, intended for oral administration. Capsules are classified into hard capsules and soft capsules. Capsules are usually prepared by the following methods. Coloring agents, preservatives, etc. may be added to the capsule bases. [0059] Hard capsules : A homogeneous mixture of active substance(s) with diluents and other suitable excipients, or granules or formed masses prepared by a suitable method, are fdled into capsule shells as they are or after slight compression.
[0060] Soft capsules: Active substance(s) and suitable excipients (including solvents) are mixed, enclosed by a suitable capsule base such as gelatin plasticized by addition of glycerin, D-sorbitol, etc. and molded in a suitable shape and size.
[0061] Usually capsules meet the requirements of Uniformity of Dosage Units as described at paragraph 6.02 and meet the requirements of Dissolution Test or Disintegration Test as described at paragraphs 6.10 and 6.09 respectively of the Japanese Pharmacopoeia 18th Edition dated 7 June 2021.
[0062] Hard capsules are generally further classified according to their size into 8 categories from large to small (No. 000, No. 00, No. 0, No. 1, No. 2, No. 3, No. 4, No. 5) (Non-Patent Document 1). The size of the No. 3 capsule is listed as 5.8 mm (outer diameter) x total length after filling (15.9 mm) (Non-Patent Document 7). Including the tolerances, the No. 3 capsule is listed as having a size of 5.83 ± 0.06 mm (outer diameter) x 15.9 ± 0.30 mm (total length after filling) (Non-Patent Document 7).
[0063] The method for producing the capsule preparation is not particularly limited, and may be a conventional method. In general, capsule preparations can, for example, be produced by sieving various components such as active components, excipients, and disintegrants, then mixing, filling the mixture into capsules, and performing primary packaging such as blister packaging. A blister-packaged preparation (sometimes simply referred to as a blister sheet) can also be subjected to secondary packaging in which this is packaged in an individual box and sealed.
[0064] The capsules can likewise be produced by production techniques that are known per se. In general, capsules can be produced by way of dissolving capsule starting materials (for example, gelatine, hypromellose, titanium oxide) and the like in purified water or the like and stirring to make a uniform jelly, uniformly depositing the jelly on mold pins, drying the jelly on the mold pins, cutting, and temporary joining. The capsules can then be subjected to printing, inspection and packaging. Hard capsules may be made for example from hard gelatin or hydroxypropyl methylcellulose (HPMC). Both hard capsules and soft capsules are well known to the person skilled in the art and commercially available, such as the Capsugel™ range of capsules from Lonza, such as the Vcaps™ and Vcaps™ plus capsules.
[0065] The content of isavuconazonium sulfate contained in the hard capsule preparation (e.g. one specified by Japanese Pharmacopoeia Capsule Standard No. 3, see paragraph [0046]), is not particularly limited, but is exemplified by 10 to 200 mg, 30 to 150 mg, 50 to 100 mg, or 70 to 80 mg, and is preferably exemplified by 74.5 mg (40 mg in terms of isavuconazole).
[0066] The various components included in hard capsule preparations (e.g. those specified by Japanese Pharmacopoeia Capsule Standard No. 3 (see paragraph [0046])) can be exemplified by the components and compositional amounts shown in Table 1. Capsules can be produced using conventional methods, as described above, in accordance with Table 2 below.
Table 1
Figure imgf000015_0001
* Referred to as colloidal silicon dioxide in non-patent document 4
Table 2
Figure imgf000015_0002
[0067] 4, Preventing decomposition
In the present invention, preventing decomposition means preventing decreases in the content of isavuconazonium sulfate contained in the preparation in the course of storing the blister-packaged capsule preparation containing isavuconazonium sulfate according to the present invention, as compared to the content of isavuconazonium sulfate at the start of storage.
[0068] The content of isavuconazonium sulfate contained in the preparation can be measured by a method such as LC/MS/MS.
[0069] Here, the storage conditions are not particularly limited, and refrigerated storage or room temperature storage may be used, and dark storage may also be used. Furthermore, in order to more clearly confirm changes over time in the content of isavuconazonium sulfate connected with undergoing storage, preparations can be stored under conditions adopted for long-term storage tests, accelerated tests, and severe tests, and changes in the preparations over time can be observed. These can, for example, be exemplified by storage conditions such as 25°C/60% relative humidity (RH) and 40°C/75% RH.
[0070] In respect of preventing decomposition, the period for which the preparation is stored is preferably 1 month or more, and 2 months or more, 3 months or more, or 6 months or more is preferred.
Furthermore, sometimes other modes for the period for which the preparation is stored may preferably be exemplified by 9 months or more, 12 months or more, 18 months or more, 24 months or more, or 30 months or more.
[0071] 5, Preventing an increase in water content
In the present invention, preventing an increase in water content means preventing an increase in water content contained in the filling composition of the preparation, the capsule, and/or the overall preparation, after the start of storage, in the course of storing the blister-packaged capsule preparation containing isavuconazonium sulfate according to the present invention, as compared to the water content contained in the filling composition of the preparation, the capsule, and/or the overall preparation at the start of storage.
[0072] A person skilled in the art can easily measure the water content of the filling composition of the preparation, capsule, or the overall preparation. Although the measurement method is not particularly limited, this can, for example, be exemplified by the loss-on-drying test method and Karl Fischer method.
[0073] Here, the storage conditions are not particularly limited, and refrigerated storage or room temperature storage may be used, and dark storage may also be used. Furthermore, in order to more clearly confirm changes in the water content, preparations can be stored under conditions generally adopted for long-term storage tests, accelerated tests, and severe tests, and changes in the preparations over time can be observed. These can, for example, be exemplified by storage conditions such as 25°C/60% RH and 40°C/75% RH.
[0074] In respect of preventing increases in water content, the period for which the preparation is stored is preferably 1 month or more, and 2 months or more, 3 months or more, or 6 months or more is preferred. Furthermore, sometimes other modes for the period for which the preparation is stored may preferably be exemplified by 9 months or more, 12 months or more, 18 months or more, 24 months or more, or 30 months or more.
[0075] 6, Storage
The capsule preparation of the present invention is preferably stored in the state resulting from primary packaging in an aluminum blister pack. In addition, when the capsule preparation of the present invention undergoes primary packaging, it is preferable to enclose a desiccant together therewith for the purpose of reducing the effects of moisture in the air on the preparation. Although the type of desiccants is not particularly limited, this can, for example, be exemplified by silica gel, calcium oxide (quicklime), and silica-alumina gel-based compounds (montmorillonite, and the like). The amount of desiccant may be 10% or more, preferably 20% or more, 30% or more, or 50% or more of the content of isavuconazonium sulfate in the preparation.
[0076] The capsule preparation of the present invention can be secondarily packaged in an individual box, polyethylene bag, or the like, and it is preferable to enclose a desiccant in the secondary packaging as well.
[0077] The capsule preparation of the present invention may be stored at room temperature but is preferably stored refrigerated. The capsule preparation of the present invention is preferably stored in an environment with low air humidity and in a dark room.
[0078] Although the period for which the preparation is stored is not particularly limited, this is preferably 1 month or more, and 2 months or more, 3 months or more, or 6 months or more is preferred. Furthermore, sometimes other modes for the period for which the preparation is stored may preferably be exemplified by 9 months or more, 12 months or more, 18 months or more, 24 months or more, or 30 months or more.
[0079] 7, Use
Among other uses, the capsule preparation of the present invention can be used, for example, as a pharmaceutical preparation for treating fungal infections. That is to say, among other uses, by administering the preparation of the present invention to patients with fungal infections, it is possible to treat fungal infections. When administering the preparation of the present invention for the purpose of treating fungal infections, the administrative route, frequency of administration, the dose, and the subject of administration can be determined by a physician or the like.
[0080] In some embodiments the blister-packaged capsule preparation containing isavuconazonium sulfate, of the invention satisfies the following conditions (1) to (4):
(1) the capsule used in the capsule preparation is Japanese Pharmacopoeia Capsule Standard No. 3;
(2) the major axis of a pocket containing the capsule preparation is 150 to 200% of the total length of 15.9 mm specified by Japanese Pharmacopoeia Capsule Standard No. 3;
(3) the minor axis of the pocket containing the capsule preparation is 295 to 345% of the outer diameter of 5.8 mm specified by Japanese Pharmacopoeia Capsule Standard No. 3; and
(4) the height of the pocket containing the capsule preparation is 100 to 150% of the outer diameter of 5.8 mm specified by Japanese Pharmacopoeia Capsule Standard No. 3; wherein preferred dimensions of the pocket containing the capsule preparation are as described in paragraphs [0049], [0050] and [0051],
[0081] In some embodiments the blister-packaged capsule preparation containing isavuconazonium sulfate of the invention, satisfies the following conditions (1) to (4):
(1) the capsule used in the capsule preparation is of Japanese Pharmacopoeia Capsule Standard No. 3;
(2) the major axis of a pocket containing the capsule preparation is 170 to 180% of the total length of 15.9 mm specified by Japanese Pharmacopoeia Capsule Standard No. 3; (3) the minor axis of the pocket containing the capsule preparation is 315 to 325% of the outer diameter of 5.8 mm specified by Japanese Pharmacopoeia Capsule Standard No. 3; and
(4) the height of the pocket containing the capsule preparation is 105 to 115% of the outer diameter of 5.8 mm specified by Japanese Pharmacopoeia Capsule Standard No. 3.
Examples
[0082] Hereafter, examples will be given to describe the present invention in further detail. However, the present invention is not restricted by the following examples and can be embodied in any mode within a scope that does not depart from the gist of the present invention.
[0083] Example 1 : Production of Capsule Preparation 1
Capsule Preparation 1 containing isavuconazonium sulfate was produced by a method known per se. Here, the various components filled into the No. 3 capsules were as shown in Table 1 above, and the No. 3 capsule itself was produced using the components shown in Table 2, by way of a conventional method. [0084] Aluminum blister packaging was performed in a mode in which seven doses of the same preparation were packaged in one sheet. As shown in Figure 1, this pack was structured such that one dose of desiccant (25 mg) was packaged together with one dose of this preparation. That is to say, the structure was such that a pocket (recess) containing one dose of this preparation and a pocket (recess) containing one dose of the desiccant are spatially connected. The aluminum blister pack was produced by a conventional method.
[0085] Here, the major axis of the pocket containing this preparation was 177% of the total length of 15.9 mm . The minor axis of this pocket was 319% of the outer diameter of 5.8 mm . The height of this pocket was 108% of the outer diameter of 5.8 mm specified by No. 3.
[0086] Example 2: Evaluation of Capsule Preparation 1
(1) Method
The Capsule Preparation 1 produced in Example 1 was stored under conditions of 25°C/60% RH for 6 months. The content of isavuconazonium sulfate contained in the preparation was measured at the start of storage and 6 months after the start of storage. A relative value (%) with respect to the theoretical isavuconazonium sulfate content of 74.5 mg was used for the content. Measurement of isavuconazonium sulfate content was carried out using a validated high-performance liquid chromatography (HPLC) method.
[0087] (2) Results
Table 3
Figure imgf000020_0001
[0088] The decomposition rate is defined as the value (%) obtained by subtracting the isavuconazonium sulfate content after 6 months of storage from the isavuconazonium sulfate content at the start of storage, dividing the result by the isavuconazonium sulfate content at the start of storage, and multiplying by 100. [0089] Surprisingly, with the Capsule Preparation 1, it was found that decomposition of isavuconazonium sulfate during storage was found to be lower as compared with Capsule Preparation 2.
[0090] Comparative Example 1: Production of No. 3 Capsule Preparation 2
A capsule preparation containing isavuconazonium sulfate (Capsule Preparation 2) was produced by a method known per se. Here, the various components filled into the No. 3 capsules were as shown in Table 1 above, and the capsule itself was produced using the components shown in Table 2, by way of a conventional method. Capsule Preparation 2 was identical to Capsule Preparation 1.
[0091] Aluminum blister packaging was performed in a mode in which seven doses of the same preparation were packaged in one sheet. As shown in Figure 1, this pack was structured such that one dose of desiccant (25 mg) was packaged together with one dose of this preparation. That is to say, the structure was such that a pocket (recess) containing one dose of this preparation and a pocket (recess) containing one dose of the desiccant were spatially connected. The aluminum blister pack was produced by a conventional method.
[0092] Here, as differs from the case in Example 1, the major axis of the pocket containing the same preparation was 245% of the total length of 15.9 mm. The minor axis of the same pocket was 415% of the outer diameter of 5.8 mm. The height of the same pocket was 155% of the outer diameter of 5.8 mm. [0093] Comparative Example 2: Evaluation of Capsule Preparation 2
(1) Method The storage stability and the like of Capsule Preparation 2 were evaluated by way of the same methods as in Example 2.
[0094] (2) Results
Table 4
Figure imgf000021_0001
Industrial Applicability [0095] The capsule preparation of the present invention exhibits excellent physical properties. The present invention is extremely useful in the pharmaceutical industry.
[0096] References
Patent Document 1 JP 3787307 B
Patent Document 2 JP 5727972 B
Patent Document 3 JP 2019-135090 A
Non-Patent Document 1 Matsuyoshi & Co., Ltd.; online; retrieved December 9, 2021; internet <URL: https://www.matsuyoshi.co.jp/catalog-pdf/19/19-7805-00.pdf>
Non-Patent Document 2 Shionogi & Co., Ltd.; online; retrieved December 9, 2021; internet <URL: https://www.shionogi-ph.co.jp/news/2020/ll/1109.html>
Non-Patent Document 3 CRESEMBA® (isavuconazonium sulfate) 186 mg capsules PATIENT
EDUCATION (2020)
Non-Patent Document 4 CRESEMBA® pack insert (2015)
Non-Patent Document 5 PRODUCT MONOGRAPH INCLUDING PATIENT MEDICATION INFORMATION ' 'CRESEMBA™. AVIR Pharma Inc. (2018)
Non-Patent Document 6 CKD Technical Journal (2017) Vol. 3, pp. 2 to 7
Non-Patent Document 7 Technical Reference File Vcaps™ Capsules

Claims

Claims
1. A blister-packaged capsule preparation containing isavuconazonium sulfate, which satisfies the following conditions (1) to (4):
(1) the capsule used in the capsule preparation is Capsule Standard No. 3;
(2) the major axis of a pocket containing the capsule preparation is 150 to 200% of the total length of 15.9 mm;
(3) the minor axis of the pocket containing the capsule preparation is 295 to 345% of the outer diameter of 5.8 mm; and
(4) the height of the pocket containing the capsule preparation is 100 to 150% of the outer diameter of 5.8 mm.
2. The blister-packaged capsule preparation according to claim 1, wherein the capsule preparation satisfies the following conditions (1) to (4):
(1) the capsule used in the capsule preparation is Capsule Standard No. 3;
(2) the major axis of a pocket containing the capsule preparation is 170 to 180% of the total length of 15.9 mm;
(3) the minor axis of the pocket containing the capsule preparation is 315 to 325% of the outer diameter of 5.8 mm; and
(4) the height of the pocket containing the capsule preparation is 105 to 115% of the outer diameter of 5.8 mm.
3. The blister-packaged capsule preparation according to claim 1 or claim 2, wherein the blister pack is an aluminum blister pack.
4. A method for preventing decomposition of isavuconazonium sulfate during storage of a blisterpackaged capsule preparation containing isavuconazonium sulfate, characterized in that the capsule preparation is a capsule preparation that satisfies the conditions (1) to (4) as defined in claim 1.
5. The method according to claim 3, wherein the capsule preparation satisfies the conditions (1) to (4) as defined in claim 2.
6. The method according to claim 4 or claim 5, wherein the blister pack is an aluminum blister pack.
7. A method for preventing an increase in water content in a blister-packaged capsule preparation containing isavuconazonium sulfate during storage of said preparation, characterized in that the capsule preparation is a capsule preparation that satisfies the conditions (1) to (4) as defined in claim 1.
8. The method according to claim 7, wherein the capsule preparation satisfies the conditions (1) to (4) as defined in claim 2.
9. The method according to claim 7 or claim 8, wherein the blister pack is an aluminum blister pack.
10. The blister-packaged capsule preparation according to any one of claims 1 to 3, or the method according to any one of claims 4 to 9, wherein Capsule Standard No. 3 has a size of 5.83 ± 0.06 mm (outer diameter) x l5.9 ± 0.30 mm (total length after filling).
11. The blister-packaged capsule preparation according to any one of claims 1 to 3 and 10, or the method according to any one of claims 4 to 10, wherein the content of isavuconazonium sulfate contained in the capsule preparation is 10 to 200 mg.
12. The blister-packaged capsule preparation or the method according to claim 11, wherein the content of isavuconazonium sulfate contained in the capsule preparation is 70 to 80 mg.
13. The blister-packaged capsule preparation or the method according to claim 12, wherein the components included in the capsule preparation are as follows:
Figure imgf000024_0001
14. The blister-packaged capsule preparation according to any one of claims 1 to 3 and 10 to 13, or the method according to any one of claims 4 to 13, wherein the blister pack has a further pocket containing a desiccant, wherein the pocket containing the capsule preparation and the pocket containing the desiccant are spatially connected.
15. The blister-packaged capsule preparation according to any one of claims 1 to 3 and 10 to 14, or the method according to any one of claims 4 to 14, wherein the capsule used in the capsule preparation is a Japanese Pharmacopoeia Capsule Standard No. 3.
PCT/EP2023/063704 2022-11-01 2023-05-22 Blister-packaged capsule preparation containing isavuconazonium sulfate Ceased WO2024094329A1 (en)

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EPPCT/EP2022/087600 2022-12-22

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JP5727972B2 (en) 2012-07-04 2015-06-03 Ckd株式会社 Blister pack, blister pack manufacturing apparatus, and blister pack manufacturing method
JP2019135090A (en) 2018-02-05 2019-08-15 藤森工業株式会社 Complex film sheet and blister container
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EP0466068A2 (en) * 1990-07-10 1992-01-15 Mect Corporation Package
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US20100300924A1 (en) * 2007-08-30 2010-12-02 Avidiamed Gmbh Blister belt for receiving medical and/or pharmaceutical and/or food supplement products
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CKD TECHNICAL JOURNAL, vol. 3, 2017, pages 2 - 7
CRESEMBA® (ISAVUCONAZONIUM SULFATE) 186 MG CAPSULES PATIENT, 2020
CRESEMBA® PACK INSERT, 2015
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TECHNICAL REFERENCE FILE VCAPSTM CAPSULES

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