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WO2001062229A1 - Produit therapeutique, son application et sa formulation - Google Patents

Produit therapeutique, son application et sa formulation Download PDF

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Publication number
WO2001062229A1
WO2001062229A1 PCT/US2001/005758 US0105758W WO0162229A1 WO 2001062229 A1 WO2001062229 A1 WO 2001062229A1 US 0105758 W US0105758 W US 0105758W WO 0162229 A1 WO0162229 A1 WO 0162229A1
Authority
WO
WIPO (PCT)
Prior art keywords
therapeutic
product
wav
eudragit
polyethylene glycol
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/US2001/005758
Other languages
English (en)
Inventor
Edward M. Rudnic
James D. Isbister
Donald J. Treacy, Jr.
Sandra E. Wassink
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.)
Advanced Pharma Inc
Original Assignee
Advanced Pharma Inc
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
Application filed by Advanced Pharma Inc filed Critical Advanced Pharma Inc
Priority to CA002400784A priority Critical patent/CA2400784C/fr
Priority to JP2001561296A priority patent/JP2003523378A/ja
Priority to EP20010914449 priority patent/EP1257255A4/fr
Priority to AU2001239838A priority patent/AU2001239838A1/en
Publication of WO2001062229A1 publication Critical patent/WO2001062229A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
    • 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
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Definitions

  • This invention relates to an therapeutic product, as well as the use and formulation thereof.
  • a wide va ⁇ ety of antibiotics, anti-fungal, anti-viral and anti-neoplastic agents have been used, and will be used, in order to treat a patient
  • such therapeutics can be administered by a repeated dosing of immediate release dosage forms, which results in poor compliance or as a controlled release formulation (slow release) at higher administered doses
  • the present invention is directed to providing for an improved therapeutic product
  • a pharmaceutical product which is comprised of at least two, preferably at least three, dosage forms, each comprised of at least one therapeutic agent and a pharmaceutically acceptable earner
  • dosage forms are formulated so that each of the dosage forms has a different release profile
  • therapeutic or “therapeutic agent” means an antibiotic, or an anti-fungal or an antiviral or an anti-neoplastic agent
  • a single or unitary therapeutic product that has contained therein at least two, preferably at least three therapeutic dosage forms, each of which has a different release profile, whereby the therapeutic contained in each of such dosage forms is released at different times.
  • the therapeutic product may be comprised of at least four different dosage forms, each of which starts to release the therapeutic contained therein at different times after administration of the therapeutic product.
  • the therapeutic product generally does not include more than five dosage forms with different release times.
  • the therapeutic product has an overall release profile such that when administered the maximum serum concentration of the total therapeutic released from the product is reached in less than twelve hours, preferably in less than eleven hours. In an embodiment, the maximum serum concentration of the total therapeutic released from the therapeutic product is achieved no earlier than four hours after administration.
  • one of the at least three dosage forms is an immediate release dosage form whereby initiation of release of the therapeutic therefrom is not substantially delayed after administration of the therapeutic product.
  • the second and third of the at least three dosage forms is a delayed dosage form (which may be a pH sensitive or a non-pH sensitive delayed dosage form, depending on the type of therapeutic product), whereby the therapeutic released therefrom is delayed until after initiation of release of the therapeutic from the immediate release dosage form.
  • the therapeutic release from the second of the at least two dosage forms achieves a C max (maximum serum concentration in the serum) at a time after the therapeutic released from the first of the at least three dosage forms achieves a C max in the serum, and the therapeutic released from the third dosage form achieves a C ma x in the serum after the C max of therapeutic released from the second dosage form.
  • C max maximum serum concentration in the serum
  • the second of the at least two dosage forms initiates release of the therapeutic contained therein at least one hour after the first dosage form, with the initiation of the release therefrom generally occurring no more than six hours after initiation of release of therapeutic from the first dosage form of the at least three dosage forms.
  • the immediate release dosage form produces a C ma ⁇ for the therapeutic released therefrom within from about 0.5 to about 2 hours, with the second dosage form of the at least three dosage forms producing a C maX for the therapeutic released therefrom in no more than about four hours.
  • the C maX for such second dosage form is achieved no earlier than two hours after administration of the therapeutic product; however, it is possible within the scope of the invention to achieve C ma ⁇ in a shorter period of time.
  • the therapeutic product may contain at least three or at least four or more different dosage forms.
  • the therapeutic released therefrom reaches a C max at a time later than the C ma ⁇ is achieved for the therapeutic released from each of the first and second dosage forms.
  • release of therapeutic from the third dosage form is started after initiation of release of therapeutic from both the first dosage form and the second dosage form.
  • C ma ⁇ for therapeutic released from the third dosage form is achieved within eight hours.
  • the therapeutic product contains at least four dosage forms, with each of the at least four dosage forms having different release profiles, whereby the therapeutic released from each of the at least four different dosage forms achieves a C max at a different time.
  • C max for all the therapeutic released from the therapeutic product is achieved in less than twelve hours, and more generally is achieved in less than eleven hours.
  • the therapeutic product is a once a day product, whereby after administration of the therapeutic product, no further product is administered during the day; i.e., the preferred regimen is that the product is administered only once over a twenty-four hour period.
  • the preferred regimen is that the product is administered only once over a twenty-four hour period.
  • a single dosage therapeutic product comprised of at least three therapeutic dosage forms each having a different release profile is an improvement over a single dosage therapeutic product comprised of an therapeutic dosage form having a single release profile.
  • Each of the dosage forms of therapeutic in a pharmaceutically acceptable carrier may have one or more therapeutics of the same type (for example, one or more antibiotics; one or more anti-viral agents, etc.) and each of the dosage forms may have the same therapeutic or different therapeutics, each of the same type (the same or different antibiotics; the same or different anti- virals, etc.).
  • the fourth of the at least four dosage form may be a sustained release dosage form or a delayed release dosage form. If the fourth dosage form is a sustained release dosage form, even though C max of the fourth dosage form of the at least four dosage forms is reached after the C max of each of the other dosage forms is reached, therapeutic release from such fourth dosage form may be initiated prior to or after release from the second or third dosage form.
  • the therapeutic product of the present invention may be formulated for administration by a variety of routes of administration.
  • the therapeutic product may be formulated in a way that is suitable for topical administration; administration in the eye or the ear; rectal or vaginal administration; as nose drops; by inhalation; as an injectable; or for oral administration.
  • the therapeutic product is formulated in a manner such that it is suitable for oral administration.
  • the at least two different dosage forms may be formulated for topical administration by including such dosage forms in an oil-in-water emulsion, or a water-in-oil emulsion.
  • the immediate release dosage form is in the continuous phase
  • the delayed release dosage form is in a discontinuous phase.
  • the formulation may also be produced in a manner for delivery of three dosage forms as hereinabove described.
  • an oil-in-water-in-oil emulsion with oil being a continuous phase that contains the immediate release component, water dispersed in the oil containing a first delayed release dosage form, and oil dispersed in the water containing a third delayed release dosage form.
  • the therapeutic product may be formulated for use in the eye or ear or nose, for example, as a liquid emulsion.
  • the dosage form may be coated with a hydrophobic polymer whereby a dosage form is in the oil phase of the emulsion, and a dosage form may be coated with hydrophilic polymer, whereby a dosage form is in the water phase of the emulsion.
  • the therapeutic product with at least three different dosage forms with different release profiles may be formulated for rectal or vaginal administration, as known in the art. This may take the form of a cream or emulsion, or other dissolvable dosage form similar to those used for topical administration.
  • the therapeutic product may be formulated for use in inhalation therapy by coating the particles and micronizing the particles for inhalation.
  • the therapeutic product is formulated in a manner suitable for oral administration.
  • each of the dosage forms may be used as a pellet or a particle, with a pellet or particle then being formed into a unitary pharmaceutical product, for example, in a capsule, or embedded in a tablet, or suspended in a liquid for oral administration.
  • each of the dosage forms of the product may be formulated as a tablet, with each of the tablets being put into a capsule to produce a unitary therapeutic product.
  • therapeutic products may include a first dosage form in the form of a tablet that is an immediate release tablet, and may also include two or more additional tablets, each of which provides for a delayed release of the therapeutic, as hereinabove described, whereby the C max of the therapeutic released from each of the tablets is reached at different times, with the C max of the total therapeutic released from the therapeutic product being achieved in less than twelve hours.
  • the formulation of an therapeutic product including at least three dosage forms with different release profiles for different routes of administration is deemed to be within the skill of the art from the teachings herein.
  • the time of release can be controlled by the concentration of therapeutics in the coating and/or the thickness of the coating.
  • the immediate release dosage form of the product generally provides from about 20% to about 50% of the total dosage of therapeutic to be delivered by the product, with such immediate release dosage forms generally providing at least 25% of the total dosage of the therapeutic to be delivered by the product.
  • the immediate release dosage form provides from about 20% to about 30% of the total dosage of therapeutic to be delivered by the product; however, in some cases it may be desirable to have the immediate release dosage form provide for about 45% to about 50%) of the total dosage of therapeutic to be delivered by the product.
  • each of the delayed release dosage forms may provide about equal amounts of therapeutic; however, they may also be formulated so as to provide different amounts.
  • each of the dosage forms contains the same therapeutic; however, each of the dosage forms may contain more than one therapeutic.
  • the immediate release component provides from 20% to 35% (preferably 20% to 30%), by weight, of the total therapeutic; where there is three delayed release components, the immediate release component provides from 15% to 30%, by weight, of the total therapeutic; and where there are four delayed release components, the immediate release component provides from 10% to 25%, by weight, of the total therapeutic.
  • the first delayed release component (the one released earlier in time) provides from 30% to 60%, by weight, of the total therapeutic provided by the two delayed release components with the second delayed release component providing the remainder of the therapeutic.
  • the earliest released component provides 20% to 35% by weight of the total therapeutic provided by the three delayed release components
  • the next in time delayed release component provides from 20% to 40%, by weight, of the therapeutic provided by the three delayed release components and the last in time providing the remainder of the therapeutic provided by the three delayed release components.
  • the earliest delayed release component provides from 15% to 30%, by weight
  • the next in time delayed release component provides from 15% to 30%
  • the next in time delayed release component provides from 20% to 35%, by weight
  • the last in time delayed release component provides from 20% to 35%, by weight, in each case of the total therapeutic provided by the four delayed release components.
  • the immediate release portion of this system can be a mixture of ingredients that breaks down quickly after administration to release the therapeutic. This can take the form of either a discrete pellet or granule that is mixed in with, or compressed with, the other three components.
  • the materials to be added to the therapeutics for the immediate release component can be, but are not limited to, microcrystalline cellulose, com starch, pregelatinized starch, potato starch, rice starch, sodium carboxymethyl starch, hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxyethylcellulose, ethylcellulose, chitosan, hydroxychitosan, hydroxymethylatedchitosan, cross-linked chitosan, cross-linked hydroxymethyl chitosan, maltodextrin, mannitol, sorbitol, dextrose, maltose, fructose, glucose, levulose, sucrose, polyvinylpyrrolidone (PVP), acrylic acid derivatives (Carbopol, Eudragit, etc.), polyethylene glycols, such a low molecular weight PEGs (PEG2000- 10000) and high molecular weight PEGs (Polyox) with molecular weights above 20,000 daltons
  • ingredients in this system may be useful to have other ingredients in this system to aid in the dissolution of the drug, or the breakdown of the component after ingestion or administration.
  • These ingredients can be surfactants, such as sodium lauryl sulfate, sodium monoglycerate, sorbitan monooleate, sorbitan monooleate, polyoxyethylene sorbitan monooleate, glyceryl monostearate, glyceryl monooleate, glyceryl monobutyrate, one of the non-ionic surfactants such as the Pluronic line of surfactants, or any other material with surface active properties, or any combination of the above.
  • surfactants such as sodium lauryl sulfate, sodium monoglycerate, sorbitan monooleate, sorbitan monooleate, polyoxyethylene sorbitan monooleate, glyceryl monostearate, glyceryl monooleate, glyceryl monobutyrate, one of the non-ionic
  • These materials may be present in the rate of 0.05-15% (W/W).
  • compositions in this composition are the same immediate release unit, but with additional polymers integrated into the composition, or as coatings over the pellet or granule.
  • Materials that can be used to obtain a delay in release suitable for this component of the invention can be, but are not limited to, polyethylene glycol (PEG) with molecular weight above 4,000 daltons (Carbowax, Polyox), waxes such as white wax or bees wax, paraffin, acrylic acid derivatives (Eudragit), propylene glycol, and ethylcellulose.
  • PEG polyethylene glycol
  • Carbowax, Polyox polyethylene glycol
  • waxes such as white wax or bees wax
  • paraffin acrylic acid derivatives
  • acrylic acid derivatives Eudragit
  • propylene glycol and ethylcellulose
  • these materials can be present in the range of 0.5-25% (W/W) of this component.
  • the components in this composition are the same as the immediate release component, but with additional polymers integrated into the composition, or as coatings over the pellet or granule.
  • the kind of materials useful for this purpose can be, but are not limited to, cellulose acetate pthalate, Eudragit L, and other pthalate salts of cellulose derivatives.
  • These materials can be present in concentrations from 4-20% (W/W).
  • compositions in this composition are the same as the immediate release component, but with additional polymers integrated into the composition, or as coatings over the pellet or granule.
  • the kind of materials useful for this purpose can be, but are not limited to, ethylcellulose,hydroxypropylmethylcellulose,hydroxypropylcellulose, hydroxyethylcellulose, carboxymethylcellulose, methylcellulose, nitrocellulose, Eudragit R, and Eudragit RL, Carbopol, or polyethylene glycols with molecular weights in excess of 8,000 daltons.
  • These materials can be present in concentrations from 4-20% (W/W).
  • the units comprising the therapeutic composition of the present invention can be in the form of discrete pellets or particles contained in the capsule, or particles embedded in a tablet or suspended in a liquid suspension.
  • the therapeutic composition of the present invention may be administered, for example, by any of the following routes of administration: sublingual, transmucosal, transdermal, parenteral, etc., and preferably is administered orally.
  • the composition includes a therapeutically effective amount of the therapeutic, which amount will vary with the therapeutic to be used, the disease or infection to be treated, and the number of times that the composition is to be delivered in a day.
  • the composition is administered to a host in an amount effective for treating the disease or infection.
  • the therapeutic composition or product may be used for treating an infection in a host that is caused by bacteria or virus or fungus and may be used to treat cancer.
  • This system will be especially useful in extending the practial therapeutic activity for antibiotics with elimination half lives of less than 20 hours and more particularly with elimination half-lives of less than 12 hours, and will be particularly useful for those drugs with half-lives of 2-10 hours.
  • amphotericin B flucytosine, fluconazole, griseofulvin, miconazole nitrate, terbinafine hydrochloride, ketoconazole, itraconazole, undecylenic acid and chloroxylenol, ciclopirox, clotrimazole, butenafme hydrochloride, nystatin, naftifine hydrochloride, oxiconazole nitrate, selenium sulfide, econazole nitrate, terconazole, butoconazole nitrate, carbol- fuchsin, clioquinol, methylrosaniline chloride, sodium thiosulfate, sulconazole nitrate, terbinafine hydrochloride, tioconazole, tolnaftate, undecylenic acid and undecylenate salts
  • agents for the treatment of cancer that may be used in accordance with the invention: carboplatin, busulfan, cisplatin, thiotepa, melphalan hydrochloride, cyclophosphamide, ifosfamide, chlorambucil, mechlorethamine hydrochloride, carmustine, lomustine, streptozocin, polifeprosan 20, dexrazoxane, dronabinol, granisetron hydrochloride, fluconazole, erythropoietin, octreotide acetate, pilocarpine hydrochloride, etidronate disodium, pamidronate disodium, allopurinol sodium, amifostine, filgrastim, mesna, ondansetron hydrochloride, dolasetron mesylate, leucovorin calcium, sargramostim, levamisole hydrochloride, doxor
  • a regimen for treating a patient with a therapeutic agent wherein the therapeutic agent is administered by injection, with the daily dosage being delivered over a period that is less than eleven hours (which period is measured from the first injection), and wherein there are at least two delivery pulses, and no more than thirty-two delivery pulses during a period of less than eleven hours, and preferably a period of less than eight hours.
  • delivery pulses means and may be accomplished by at least two spaced injections with periods between such spaced injections wherein essentially no therapeutic agent is injected into the host or alternatively, between the spaced injections, therapeutic agent is continuously injected in an amount different than that which is injected in the spaced injections.
  • At least two delivery pulses can be achieved by continuous injection of the agent at one dosage, followed by continuous injection at a different dosage.
  • there can be an initial injection wherein the therapeutic agent is continuously administered over a period of time followed by an increase in the dosage of the therapeutic agent that is administered by injection over a period of time whereby in effect there are two delivery pulses even though there may be continuous administration of the therapeutic agent.
  • the spaced injections of the therapeutic agent in less than an eleven hour period, there is at least two spaced injections of the therapeutic agent and generally no more than thirty-two spaced injections of the therapeutic agent. There may or may not be a continuous injection of the agent between the spaced injections and if there is such a continuous injection, the dosage of the agent is less than or more than the spaced injections. In a preferred embodiment, there is no injection of agent between the spaced injections. In one preferred embodiment wherein there are spaced injections of the therapeutic agent, up to about sixty percent, and preferably up to about fifty percent of the dosage that is to be injected in a period of less than eleven hours is injected during the first four hours of such period.
  • the delivery pulses are accomplished by spaced injections of the therapeutic agent in a pharmaceutically acceptable carrier. There are at least two and no more than 32 spaced injections, all of which are delivered within 11 hours and preferably within 8 hours of the first injection.
  • the daily dosage is delivered within such eleven or eight hour period and the spaced injections provide for at least 75%, preferably at least 90% and more preferably at least 100% of the agent that is to be delivered.
  • the therapeutic agent may be injected by any procedures known in the art.
  • the therapeutic agent may be injected by use of a controlled pump of a type known in the art for injecting pharmaceutical products.
  • the regimen of the invention may be employed in a hospital wherein controlled injections are administered by use of a catheter.
  • Injections can be made into any body structure, organ or blood vessel, such as intravenous, intramuscular, subcutaneous, intradermal, intrathecal, intraperitoneal, intraarticular, intraocular, or other routes of injectable delivery.
  • distinct maximum serum concentration pulses of the therapeutic agent in the blood of the patient in a period of less than 11 hours.
  • distinct Cmax pulses occur in a period of less than eight hours and preferably within a period of six hours.
  • all of the Cmax pulses are achieved in a period of less than 1 1 hours, preferably less than eight hours, and such pulses provide the daily dosage of the therapeutic agent; i.e., the therapeutic agent is injected in at least two delivery pulses within eleven hours and there is no further administration over the remainder of a twenty-four hour period.
  • All or a portion of the delivery pulses of the therapeutic agent delivered by spaced injections may be the same or different dosages of the therapeutic agent.
  • each spaced injection provides at least 5% of the total daily dosage of the therapeutic agent.
  • each delivery pulse may include one or more different therapeutic agents (for example two or more different antibiotics), and each delivery pulse may contain the same or different therapeutic agents (for example, one delivery pulse may contain two or more antibiotics and one may contain only one of the two or more antibiotics).
  • the therapeutic agent is preferably an antibiotic or an anti-viral agent or an anti-fungal agent or an anti-neoplastic agent.
  • Formulate the composition by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a dry blend. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum over or forced-air oven.
  • a suitable pharmaceutical drier such as a vacuum over or forced-air oven.
  • the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Polyethylene glycol 4000 Polyethylene glycol 2000 10 Hydroxypropylcellulose 5
  • Clarithromycin 75% (W/W) Microcrystalline cellulose 15 Hydroxypropylcellulose 5 Croscarmellose sodium 5
  • Clarithromycin 75% (W/W) Polyethylene glycol 4000 10 Polyethylene glycol 2000 10 Hydroxypropylcellulose 5
  • Clarithromycin 75% (W/W) Polyethylene glycol 8000 20 Polyvinylpyrrolidone 5
  • Ciprofloxacin 75% (W/W) Microcrystalline cellulose 15 Hydroxypropylcellulose 5 Croscarmellose sodium 5
  • Ciprofloxacin 75% (W/W) Polyethylene glycol 4000 10 Polytheylene glycol 2000 10 Hydroxypropylcellulose 5
  • Polyethylene glycol 4000 Polyethylene glycol 2000 10 Hydroxypropylcellulose 5
  • Formulate the composition by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a hot melt process. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum over or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder
  • a suitable pharmaceutical drier such as a vacuum over or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Clarithromycin 75% (WAV) Polyethylene glycol 4000 10 Polyethylene glycol 2000 10 Eudragit RL 30D 5
  • Clarithromycin 80% (WAV) Polyethylene glycol 8000 10 Polyvinylpyrrolidone 5 Eudgragit R 30D 5
  • Ciprofloxacin 65% (WAV) Polyethylene glycol 4000 20 Hydroxypropylcellulose 10 Eudragit RL 30D 5
  • Ciprofloxacin 75% Microcrystalline cellulose 15 Hydroxypropylcellulose 5 Ethylcellulose 5
  • Ciprofloxacin 80% (WAV) Polyethylene glycol 4000 10 Polyethylene glycol 2000 5 Eudgragit RL 30D 5
  • Ciprofloxacin 75% (WAV) Polyethylene glycol 8000 20 Ethylcellulose 5
  • Formulate the ingredients by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a hot melt process. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum over or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder
  • a suitable pharmaceutical drier such as a vacuum over or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Microcrystalline cellulose 20 Cellulose Acetate Pthalate 15
  • Ciprofloxacin 75% Microcrystalline Cellulose 15 Hydroxypropylcellulose pthalate 10
  • Ciprofloxacin 70% (WAV) Polyethylene glycol 4000 20 Cellulose acetate pthalate 10
  • Microcrystalline cellulose 20 Cellulose acetate pthalate 10
  • Formulate the composition by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a hot melt process. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum over or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder
  • a suitable pharmaceutical drier such as a vacuum over or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Clarithromycin 80% (W/W) Polyethylene glycol 8000 10 Hydroxypropylmethylcellulose 5 Eudgragit RS 30D 5
  • Ciprofloxacin 75% (WAV) Hydroxyethylcellulose 10 Polyethylene glycol 4000 10 Hydroxypropylcellulose 5
  • Formulate the composition by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a dry blend. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum oven or forced-air oven.
  • a suitable pharmaceutical drier such as a vacuum oven or forced-air oven.
  • the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Polyethylene glycol 4000 Polyethylene glycol 2000 10 Hydroxypropylcellulose 5
  • Ketoconazole 65% (WAV) Microcrystalline cellulose 20 Hydroxypropylcellulose 10 Croscarmellose sodium 5
  • Ketoconazole 75% Microcrystalline cellulose 15 Hydroxypropylcellulose 5 Croscarmellose sodium 5
  • Ketoconazole 75% (W/W) Polyethylene glycol 4000 10 Polyethylene glycol 2000 10 Hydroxypropylcellulose 5
  • Ketoconazole 75% (WAV) Polyethylene glycol 8000 20 Polyvinylpyrrolidone 5
  • Polyethylene glycol 4000 Polytheylene glycol 2000 10 Hydroxypropylcellulose 5
  • Cirpofloxacin 75% Polyethylene glycol 8000 20 Polyvinylpyrrolidone 5
  • Formulate the composition by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a hot melt process. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum oven or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder
  • a suitable pharmaceutical drier such as a vacuum oven or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Ketoconazole 75% (WAV) Polyethylene glycol 4000 10 Polyethylene glycol 2000 10 Eudragit RL 30D 5
  • Ketoconazole 80% (W/W) Polyethylene glycol 8000 10 Polyvinylpyrrolidone 5 Eudgragit R 30D 5 Example 80:
  • Polyethylene glycol 4000 10 Polyethylene glycol 2000 5 Eudgragit RL 30D 5
  • Formulate the ingredients by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a hot melt process. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum oven or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder
  • a suitable pharmaceutical drier such as a vacuum oven or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Microcrystalline cellulose 20 Cellulose Acetate Pthalate 15
  • Microcrystalline cellulose 25 Cellulose Acetate Pthalate 10 Hydroxypropylmethylcellulose 10
  • Ketoconazole 70% (WAV) Eudragit L 30D 15 Hydroxypropylcellulose 10 Ethylcellulose 5
  • Ketoconazole 75% (WAV) Polyethylene glycol 2000 10 Eudragit L 30D 15
  • Formulate the composition by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a hot melt process. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum oven or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder
  • a suitable pharmaceutical drier such as a vacuum oven or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Ketoconazole 75% Polyethylene glycol 4000 10 Lactose 10 Eudragit RL 30D 5
  • Ketoconazole 80% (WAV) Polyethylene glycol 8000 10 Hydroxypropylmethylcellulose 5 Eudgragit RS 30D 5
  • Griseofulvin 75% (WAV) Hydroxyethylcellulose 10 Polyethylene glycol 4000 10 Hydroxypropylcellulose 5
  • Formulate the composition by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a dry blend. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum over or forced-air oven.
  • a suitable pharmaceutical drier such as a vacuum over or forced-air oven.
  • the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary table press.
  • Croscarmellose sodium 10 Example 116:
  • Polyethylene glycol 4000 Polyethylene glycol 2000 10 Hydroxypropylcellulose 5
  • Polyethylene glycol 4000 Polyethylene glycol 2000 10 Hydroxypropylcellulose 5
  • Valacyclovir 75% (WAV) Polyethylene glycol 4000 10 Polytheylene glycol 2000 10 Hydroxypropylcellulose 5
  • Cirpofloxacin 75% Polyethylene glycol 8000 20 Polyvinylpyrrolidone 5
  • Polyethylene glycol 4000 Polyethylene glycol 2000 10 Hydroxypropylcellulose 5
  • Formulate the composition by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a hot melt process. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum over or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder
  • a suitable pharmaceutical drier such as a vacuum over or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Valacyclovir 65% (WAV) Polyethylene glycol 4000 20 Hydroxypropylcellulose 10 Eudragit RL 30D 5
  • Valacyclovir 80% (WAV) Polyethylene glycol 4000 10 Polyethylene glycol 2000 5 Eudgragit RL 30D 5
  • Valacyclovir 75% Polyethylene glycol 8000 20 Ethylcellulose 5
  • Formulate the ingredients by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a hot melt process. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum over or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder
  • a suitable pharmaceutical drier such as a vacuum over or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Microcrystalline cellulose 20 Cellulose Acetate Pthalate 15
  • Microcrystalline cellulose 25 Cellulose Acetate Pthalate 10 Hydroxypropylmethylcellulose 10
  • Formulate the composition by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a hot melt process. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum over or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder
  • a suitable pharmaceutical drier such as a vacuum over or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Valacyclovir 75% (WAV) Hydroxyethylcellulose 10 Polyethylene glycol 4000 10 Hydroxypropylcellulose 5
  • Formulate the composition by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a dry blend. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum oven or forced-air oven.
  • a suitable pharmaceutical drier such as a vacuum oven or forced-air oven.
  • the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Polyethylene glycol 4000 Polyethylene glycol 2000 10 Hydroxypropylcellulose 5
  • Dexamethasone 65% (WAV) Microcrystalline cellulose 20 Hydroxypropylcellulose 10 Croscarmellose sodium 5
  • Dexamethasone 75% (WAV) Microcrystalline cellulose 15 Hydroxypropylcellulose 5 Croscarmellose sodium 5
  • Valrubicin 75% Microcrystalline cellulose 15 Hydroxypropylcellulose 5 Croscarmellose sodium 5
  • Polyethylene glycol 4000 Polytheylene glycol 2000 10 Hydroxypropylcellulose 5
  • Polyethylene glycol 4000 Polyethylene glycol 2000 10 Hydroxypropylcellulose 5
  • Formulate the composition by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a hot melt process. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum oven or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder
  • a suitable pharmaceutical drier such as a vacuum oven or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Dexamethasone 75% (WAV) Polyethylene glycol 4000 10 Polyethylene glycol 2000 10 Eudragit RL 30D 5
  • Dexamethasone 80% (WAV) Polyethylene glycol 8000 10 Polyvinylpyrrolidone 5 Eudgragit R 30D 5
  • Valrubicin 65% Polyethylene glycol 4000 20 Hydroxypropylcellulose 10 Eudragit RL 30D 5
  • Polyethylene glycol 4000 10 Polyethylene glycol 2000 5 Eudgragit RL 30D 5
  • Formulate the ingredients by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a hot melt process. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum oven or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder
  • a suitable pharmaceutical drier such as a vacuum oven or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Microcrystalline cellulose 20 Cellulose Acetate Pthalate 15
  • Microcrystalline cellulose 25 Cellulose Acetate Pthalate 10 Hydroxypropylmethylcellulose 10
  • Dexamethasone 70% (WAV) Eudragit L 30D 15 Hydroxypropylcellulose 10 Ethylcellulose 5
  • Dexamethasone 75% (W/W) Polyethylene glycol 2000 10 Eudragit L 30D 15
  • Formulate the composition by mixing the ingredients in a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder, in the presence of water or other solvent, or in a hot melt process. If water or other solvent was used, dry the blend in a suitable pharmaceutical drier, such as a vacuum oven or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • a suitable pharmaceutical mixer or granulator such as a planetary mixer, high-shear granulator, fluid bed granulator, or extruder
  • a suitable pharmaceutical drier such as a vacuum oven or forced-air oven. Allow the product to cool, the product may be sieved or granulated, and compressed using a suitable tablet press, such as a rotary tablet press.
  • Dexamethasone 75% (WAV) Polyethylene glycol 4000 10 Lactose 10 Eudragit RL 30D 5
  • composition of the aqueous Eudragit L30D-55 dispersion applied to the metronidazole matrix pellets is provided below in Table 2.
  • the TEC/talc suspension is then homogenized using a PowerGen 700 high shear mixer.
  • composition of the aqueous Eudragit® S 100 dispersion applied to the metronidazole matrix pellets is provided below in Table 3.
  • Part B is then added slowly to the polymer dispersion in Part A with a mild stirring.
  • 1.4 Coating Conditions for the Application of Aqueous Coating Dispersions The following coating parameters were used to coat matrix pellets with each of the Eudragit® L 30 D-55 and Eudragit® S 100 aqueous film coating.
  • Pellets are filled into size 00 hard gelatin capsules at a ratio of 30%: 30%: 40%:
  • the capsule is filled with the three different pellets to achieve a total dose of
  • composition of the Amoxicillin trihydrate matrix pellets provided in Table 4.
  • Table 4 Composition of Amoxicillin Matrix Pellets
  • composition of the aqueous Eudragit L30D-55 dispersion applied to the amoxicillin matrix pellets is provided below in Table 5.
  • the TEC/talc suspension is mixed using laboratory mixer.
  • composition of the aqueous Eudragit® S 100 dispersion applied to the Amoxicillin matrix pellets is provided below in Table 6.
  • Part B is then added slowly to the polymer dispersion in Part A with a mild stirring.
  • the fill weight should be adjusted to achieve a 500 mg dose tablet.
  • 232.2.1 Blend clarithromycin, silicified microcrystalline cellulose and lactose monohydrate using a Robot Coupe high shear granulator.
  • 232.2.2 Prepare the binder solution by adding the Polyoxyl to the purified water while stirring. After that is mixed, slowly add the hydroxypropyl methylcellulose and continue to stir until a solution is achieved.
  • composition of the aqueous Eudragit L30D-55 dispersion applied to the clarithromycin matrix pellets is provided below in Table 10.
  • the TEC/talc suspension is then homogenized using a PowerGen 700 high shear mixer.
  • composition of the aqueous Eudragit® S 100 dispersion applied to the clarithromycin matrix pellets is provided below in Table 11.
  • Part B is then added slowly to the polymer dispersion in Part A with a mild stirring.
  • SI 00 coated pellets in weight percentages of 30%:30%:40%, respectively to provide 250 mg. capsules.
  • composition of the metronidazole matrix pellets provided in Table 12.
  • composition of the aqueous Eudragit L30D-55 dispersion applied to the metronidazole matrix pellets is provided below in Table 13.

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Abstract

L'invention concerne un produit thérapeutique comprenant un premier dosage thérapeutique, un deuxième dosage thérapeutique et un troisième dosage thérapeutique, chacun de ces dosages contenant au moins un agent thérapeutique et un support pharmaceutiquement acceptable et ayant des profils de libération différents. Le produit thérapeutique atteint une Cmax en moins de douze heures environ et renferme un agent antibiotique, antifongique, antiviral et antinéoplasique.
PCT/US2001/005758 2000-02-24 2001-02-22 Produit therapeutique, son application et sa formulation Ceased WO2001062229A1 (fr)

Priority Applications (4)

Application Number Priority Date Filing Date Title
CA002400784A CA2400784C (fr) 2000-02-24 2001-02-22 Produit therapeutique, son application et sa formulation
JP2001561296A JP2003523378A (ja) 2000-02-24 2001-02-22 治療剤製品、その使用及び製剤形態
EP20010914449 EP1257255A4 (fr) 2000-02-24 2001-02-22 Produit therapeutique, son application et sa formulation
AU2001239838A AU2001239838A1 (en) 2000-02-24 2001-02-22 Therapeutic product, use and formulation thereof

Applications Claiming Priority (10)

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US18454600P 2000-02-24 2000-02-24
US60/184,546 2000-02-24
US68723600A 2000-10-13 2000-10-13
US68722900A 2000-10-13 2000-10-13
US68723500A 2000-10-13 2000-10-13
US68723700A 2000-10-13 2000-10-13
US09/687,229 2000-10-13
US09/687,235 2000-10-13
US09/687,237 2000-10-13
US09/687,236 2000-10-13

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WO2003037304A1 (fr) * 2001-11-02 2003-05-08 Wockhardt Limited Compositions a liberation controlee pour agents antimicrobiens macrolides
WO2003053450A1 (fr) * 2001-12-21 2003-07-03 Biopartners Gmbh Granulat de ribavirine pour la production de comprimes pellicules
WO2004096187A1 (fr) * 2003-04-29 2004-11-11 Pliva-Lachema A.S. Preparation pharmaceutique dont le principe actif est la ribavine, et son procede de fabrication
US20050019402A1 (en) * 2003-07-21 2005-01-27 Burnside Beth A. Antibiotic product, use and formulation thereof
US20050019401A1 (en) * 2003-07-21 2005-01-27 Burnside Beth A. Antibiotic product, use and formulation thereof
US20050019403A1 (en) * 2003-07-21 2005-01-27 Burnside Beth A. Antibiotic product, use and formulation thereof
JP2005538121A (ja) * 2002-08-02 2005-12-15 アドバンシス ファーマスーティカル コーポレイション 遅延放出抗ウイルス物質産物、その使用法と製剤
JP2006500344A (ja) * 2002-08-02 2006-01-05 アドバンシス ファーマスーティカル コーポレイション 抗生物質製剤、その使用法およびその作成方法
WO2005017804A3 (fr) * 2003-08-13 2006-03-23 Agilent Technologies Inc Methodes et systeme de decouverte de polytherapies
JP2007502294A (ja) * 2003-08-12 2007-02-08 アドバンシス ファーマスーティカル コーポレイション 抗生物質製剤、その使用法及び作成方法
JP2007504141A (ja) * 2003-08-29 2007-03-01 アドバンシス ファーマスーティカル コーポレイション 抗生物質製剤、その使用法及び作成方法
JP2007513869A (ja) * 2003-09-15 2007-05-31 アドバンシス ファーマスーティカル コーポレイション 抗生物質製剤、その使用法及び作成方法
WO2007084212A3 (fr) * 2006-01-19 2007-12-06 Dow Global Technologies Inc Composition biologiquement active contenant de l'éthylcellulose
WO2009049648A3 (fr) * 2007-10-17 2009-10-01 Pharmathen S.A. Composition pharmaceutique améliorée contenant un agent antiviral et procédé de préparation de celle-ci
EP1411921B2 (fr) † 2001-07-20 2010-08-18 Novartis AG Compositions pharmaceutiques contenant de la terbinafine et leur utilisation
US8303988B2 (en) 2000-10-13 2012-11-06 Shionogi Inc. Antifungal once-a-day product, use and formulation thereof
US8889187B2 (en) 2000-02-24 2014-11-18 Shionogi Inc. Once a day amoxicillin product comprising immediate and delayed release dosage forms

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Cited By (32)

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US8889187B2 (en) 2000-02-24 2014-11-18 Shionogi Inc. Once a day amoxicillin product comprising immediate and delayed release dosage forms
US8303988B2 (en) 2000-10-13 2012-11-06 Shionogi Inc. Antifungal once-a-day product, use and formulation thereof
EP1411921B2 (fr) † 2001-07-20 2010-08-18 Novartis AG Compositions pharmaceutiques contenant de la terbinafine et leur utilisation
WO2003037304A1 (fr) * 2001-11-02 2003-05-08 Wockhardt Limited Compositions a liberation controlee pour agents antimicrobiens macrolides
US7037523B2 (en) 2001-11-02 2006-05-02 Wockhardt Limited Controlled release compositions for macrolide antimicrobial agents
WO2003053450A1 (fr) * 2001-12-21 2003-07-03 Biopartners Gmbh Granulat de ribavirine pour la production de comprimes pellicules
AU2002229678B2 (en) * 2001-12-21 2006-09-28 Biopartners Gmbh Ribavirin granulate for producing coated tablets
EP1542656A4 (fr) * 2002-08-02 2011-05-25 Middlebrook Pharmaceuticals Inc Produit antibiotique, utilisation et formulation associees
JP2005538121A (ja) * 2002-08-02 2005-12-15 アドバンシス ファーマスーティカル コーポレイション 遅延放出抗ウイルス物質産物、その使用法と製剤
JP2006500344A (ja) * 2002-08-02 2006-01-05 アドバンシス ファーマスーティカル コーポレイション 抗生物質製剤、その使用法およびその作成方法
WO2004096187A1 (fr) * 2003-04-29 2004-11-11 Pliva-Lachema A.S. Preparation pharmaceutique dont le principe actif est la ribavine, et son procede de fabrication
JP2006528190A (ja) * 2003-07-21 2006-12-14 アドバンシス ファーマスーティカル コーポレイション 抗生物質製剤、その使用法及び作成方法
JP2006528189A (ja) * 2003-07-21 2006-12-14 アドバンシス ファーマスーティカル コーポレイション 抗生物質産物、その使用法および製剤
JP2006528185A (ja) * 2003-07-21 2006-12-14 アドバンシス ファーマスーティカル コーポレイション 抗生物質製剤、その使用法及び作成方法
US8425936B2 (en) * 2003-07-21 2013-04-23 Shionogi Inc. Antibiotic product, use and formulation thereof
US8313776B2 (en) * 2003-07-21 2012-11-20 Shionogi Inc. Antibiotic product, use and formulation thereof
US20050019403A1 (en) * 2003-07-21 2005-01-27 Burnside Beth A. Antibiotic product, use and formulation thereof
US20050019401A1 (en) * 2003-07-21 2005-01-27 Burnside Beth A. Antibiotic product, use and formulation thereof
US8313775B2 (en) * 2003-07-21 2012-11-20 Shionogi Inc. Antibiotic product, use and formulation thereof
US20050019402A1 (en) * 2003-07-21 2005-01-27 Burnside Beth A. Antibiotic product, use and formulation thereof
US20120213825A1 (en) * 2003-08-12 2012-08-23 Shionogi Inc. Antibiotic product, use and formulation thereof
JP2007502294A (ja) * 2003-08-12 2007-02-08 アドバンシス ファーマスーティカル コーポレイション 抗生物質製剤、その使用法及び作成方法
US9144548B2 (en) * 2003-08-12 2015-09-29 Shionogi Inc. Antibiotic product, use and formulation thereof
US8062672B2 (en) * 2003-08-12 2011-11-22 Shionogi Inc. Antibiotic product, use and formulation thereof
WO2005017804A3 (fr) * 2003-08-13 2006-03-23 Agilent Technologies Inc Methodes et systeme de decouverte de polytherapies
US8246996B2 (en) * 2003-08-29 2012-08-21 Shionogi Inc. Antibiotic product, use and formulation thereof
EP1658034A4 (fr) * 2003-08-29 2011-06-22 Middlebrook Pharmaceuticals Inc Produit antibiotique, son utilisation et sa formulation
JP2007504141A (ja) * 2003-08-29 2007-03-01 アドバンシス ファーマスーティカル コーポレイション 抗生物質製剤、その使用法及び作成方法
JP2007513869A (ja) * 2003-09-15 2007-05-31 アドバンシス ファーマスーティカル コーポレイション 抗生物質製剤、その使用法及び作成方法
WO2007084212A3 (fr) * 2006-01-19 2007-12-06 Dow Global Technologies Inc Composition biologiquement active contenant de l'éthylcellulose
US9198865B2 (en) 2006-01-19 2015-12-01 Dow Global Technologies Llc Biologically active composition comprising ethylcellulose
WO2009049648A3 (fr) * 2007-10-17 2009-10-01 Pharmathen S.A. Composition pharmaceutique améliorée contenant un agent antiviral et procédé de préparation de celle-ci

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JP5377465B2 (ja) 2013-12-25
EP1257255A4 (fr) 2008-07-30
EP1257255A1 (fr) 2002-11-20
CA2400784A1 (fr) 2001-08-30
JP2003523378A (ja) 2003-08-05

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