[go: up one dir, main page]

WO2004047811A1 - Formulation a liberation controlee de tamsulosine ou de sels acceptables d'un point de vue pharmaceutique de celle-ci, utilisee dans le traitement des signes et des symptomes de l'hyperplasie prostatique benigne - Google Patents

Formulation a liberation controlee de tamsulosine ou de sels acceptables d'un point de vue pharmaceutique de celle-ci, utilisee dans le traitement des signes et des symptomes de l'hyperplasie prostatique benigne Download PDF

Info

Publication number
WO2004047811A1
WO2004047811A1 PCT/KR2003/000658 KR0300658W WO2004047811A1 WO 2004047811 A1 WO2004047811 A1 WO 2004047811A1 KR 0300658 W KR0300658 W KR 0300658W WO 2004047811 A1 WO2004047811 A1 WO 2004047811A1
Authority
WO
WIPO (PCT)
Prior art keywords
eudragit
methylmethacrylate
copolymer
tamsulosin
controlled release
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/KR2003/000658
Other languages
English (en)
Inventor
Ung Kil Jee
Sung Joo Hwang
Jin Kyu Park
Kyung Lae Park
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.)
Centurion Inc
Original Assignee
Centurion 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 Centurion Inc filed Critical Centurion Inc
Priority to AU2003219573A priority Critical patent/AU2003219573A1/en
Publication of WO2004047811A1 publication Critical patent/WO2004047811A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • 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
    • A61K9/5005—Wall or coating material
    • A61K9/5015—Organic compounds, e.g. fats, sugars
    • 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
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

Definitions

  • the present invention relates, in general, to a controlled release formulation of tamsulosin or pharmaceutically acceptable salts thereof for treating benign prostatic hyperplasia. More specifically, the present invention relates to a controlled release formulation for treatment of benign prostatic hyperplasia comprising tamsulosin or pharmaceutically acceptable salts thereof as an effective ingredient, characterized in that a controlled release type solid dispersion simply prepared by a spray drying process is granulated and coated, thereby accurately controlling initial release profiles; and a method of preparing the same.
  • tamsulosin was firstly disclosed in Japanese Patent Laid-open Publication No. Sho. 56-110665, together with pharmaceutically acceptable salts thereof.
  • the chemical name of tamsulosin represented by the following Formula 1 is (R)(-)-5-[2-[[2-(o- ethoxyphenoxy)ethyl]amino]propyl]-2-methoxybenzenesulfoneamide: Formula 1
  • Tamsulosin or salts thereof are known to be an antagonist of O ⁇ A adrenoceptors.
  • tamsulosin hydrochloride tamsulosin HC1
  • functions as an o receptor blocker in the urethra and the prostate region and also decreases pressure of prostate regions in urethra inner pressure curves, to improve benign prostatic hyperplasia due to prostatomegaly [UROLOGY 58 (Suppl 6 A): 42-48, 2001].
  • Korean Patent Laid-open Publication No. 02-0016944 discloses a therapeutic agent of lower urinary tract diseases comprising tamsulosin or pharmaceutically acceptable salts thereof as an effective ingredient.
  • Lower urinary tract disease is regarded as a kind of benign prostatic hyperplasia symptom caused by functional obstruction of lower urinary tracts of males as well as females. As such, it is noted that disorders of nerves controlling lower urinary tract and organic obstruction of the urethra are not included in . the above urinary tract disease category. Females are often afflicted with lower urinary tract diseases.
  • Lower urinary tract disease is caused by dysuria, sclerosis or obstruction of neck of the urinary bladder, urethra syndrome, detrusor-sphincter coordinated insufficiency, unstable bladder, chronic prostatitis, chronic cystitis, prostatalgia, Hinman's syndrome, Fowler's syndrome, psychogenic benign prostatic hyperplasia, benign prostatic hyperplasias due to drug and aging, etc.
  • tamsulosin hydrochloride for treatment of benign prostatic hyperplasia is orally administered in the amount of 0.2-0.4 mg/day [UROLOGY 58 (Suppl 6A) : 42-48, 2001], and preferable administration form is a controlled release formulation which is continuously released.
  • Commercially available Harnal ® capsule (containing 0.2 mg of tamsulosin HC1) sold by Yamanouchi Pharmaceutical Co., Ltd.
  • FLOMAXTM capsule containing 0.4 mg of tamsulosin HC1) sold by Boeringer Ingelheim are known as a controlled release dosage form administered once per day.
  • the above water-insoluble polymer is used in the form of aqueous dispersion, aqueous emulsion or water-containing organic solvent, and examples thereof include acrylate polymers or copolymers, or cellulose derivatives [e.g., commercially available Eudragit L30D-55 (methacrylic acid copolymer LD), Eudragit E30D (ethylacrylate methylmethacrylate copolymer emulsion),
  • Aquacoat ECD-30 aqueous ethyl cellulose dispersion
  • granular formulation is prepared from the above materials by use of a centrifugal fluid granulating machine, after which such granules are filled into capsules.
  • the above method is disadvantageous in terms of non-uniform release profiles, for example, high initial release rates and low release rates after 4-5 hours, therefore resulting in very difficult release control.
  • an object of the present invention is to provide a controlled release formulation of tamsulosin or pharmaceutically acceptable salts thereof for treatment of benign prostatic hyperplasia, simply prepared by a spray drying process.
  • Another object of the present invention is to provide a controlled release formulation of tamsulosin or pharmaceutically acceptable salts thereof for treatment of benign prostatic hyperplasia, capable of accurately controlling initial release profiles by adjusting a coating amount upon coating following granulating the formulation.
  • a further object of the present invention is to provide a method of preparing a controlled release formulation of tamsulosin or pharmaceutically acceptable salts thereof for treatment of benign prostatic hyperplasia, as a granular dosage form having controlled initial release profiles.
  • a controlled release formulation of tamsulosin or pharmaceutically acceptable salts thereof for treatment of benign prostatic hyperplasia comprising tamsulosin or pharmaceutically acceptable salts thereof; and a dissolution controlling agent of the tamsulosin or pharmaceutically acceptable salts thereof, including an acrylate polymer (containing copolymers, hereinafter the same), a cellulose derivative or mixtures thereof, and a poloxamer.
  • a controlled release formulation of tamsulosin or pharmaceutically acceptable salts thereof for treating benign prostatic hyperplasia comprising a first release controlling system including tamsulosin or pharmaceutically acceptable salts thereof, and a dissolution controlling agent of the tamsulosin or pharmaceutically acceptable salts thereof including an acrylate polymer, a cellulose derivative or mixtures thereof, and a poloxamer; and a second release controlling system including the first release controlling system coated with a coating agent having at least a second dissolution controlling agent.
  • the present invention provides a method of preparing a controlled release formulation of tamsulosin or pharmaceutically acceptable salts thereof for treating benign prostatic hyperplasia, comprising the following steps of: mixing a solution of tamsulosin or pharmaceutically acceptable salts thereof in a solvent, with another solution of a first dissolution controlling agent of the tamsulosin or pharmaceutically acceptable salts thereof in another solvent, followed by spray drying the mixed solution, to prepare a solid dispersion, said first dissolution controlling agent including an acrylate polymer, a cellulose derivative or mixtures thereof, and a poloxamer; granulating the solid dispersion by addition of an excipient and a binder, to prepare granules; and coating the granules with a coating agent containing at least a second dissolution controlling agent in a suitable solvent.
  • a controlled release formulation for treating benign prostatic hype ⁇ lasia comprising tamsulosin or pharmaceutically acceptable salts thereof and a dissolution controlling agent, according to a primary embodiment of the present invention, below.
  • Tamsulosin or pharmaceutically acceptable salts thereof, preferably tamsulosin hydrochloride, is used in the safe dosage range not causing side effects when administered to humans.
  • Korean Patent Laid-open Publication No. 01-53221 discloses a preferable daily dosage.
  • an acrylate polymer is exemplified by commercially available polymethacrylate methylmethacrylate copolymer (Eudragit L-100), polyethylacrylate methylmethacrylate trimethylammonioethyl methacrylate chloride copolymer (Eudragit RL-100, RS-100), polymethacrylate ethylacrylate copolymer (Eudragit L30D-55), ethylacrylate methylmethacrylate trimethylammonioethyl methacrylate chloride copolymer (Eudragit RL30D), ethylacrylate methylmethacrylate trimethylammonioethyl methacrylate chloride copolymer (Eudragit RS30D), or polyethylacrylate methylmethacrylate copolymer (Eudragit L-100), polyethylacrylate methylmethacrylate trimethylammonioethyl methacrylate chloride cop
  • examples of a cellulose derivative include aqueous ethyl cellulose dispersion (Aquacoat ECD-30, Surelease), or AnyCoat.
  • the dissolution controlling agent includes a poloxamer as a block copolymer of a series of ethylene oxide and propylene oxide, which is exemplified by ⁇ -hydro- ⁇ -hydroxypoly(oxyethylene)poly(oxypropylene) poly( ⁇ xyethylene) block copolymer.
  • the poloxamer is known to be polyethylene-propyleneglycol copolymer or polyoxyethylene-polyoxypropylene copolymer.
  • the poloxamer of the present invention contains 60-90 wt%; preferably
  • polyoxyethylene 70-80 wt% of polyoxyethylene.
  • the polyoxyethylene portion is hydrophilic but the polypropylene portion is hydrophobic. All poloxamers have similar chemical formulas, provided that only relative contents of propylene oxide and ethylene oxide in each chemical structure are different.
  • Examples of the poloxamer usable in the present invention include
  • Poloxamer 188 Poloxamer 188, Poloxamer 124, Poloxamer 237, Poloxamer 338, Poloxamer 407 and so on.
  • Poloxamer 188 is used. More detailed information related to poloxamers may be provided from Technical Bulletin available from
  • the above dissolution controlling agent is used in the form of powders, aqueous dispersion, aqueous emulsion, or water-containing organic solvent.
  • the dissolution controlling agent when being used as powders, is not specifically limited but is preferably used in the amount of 30 wt% or less.
  • the above controlling agent in case of using as the aqueous liquid forms, is not specifically limited but is preferably used in the amount of
  • a plasticizer is further added in the amount of 2-5 wt%, which is exemplified by polyethyleneglycol, propyleneglycol, glycerol, dimethylphthalate, dibutylphthalate, dibutylsebacate, triethylcitrate, tributylcitrate, triethylacetylcitrate, triacetin, castor oil, etc.
  • any one component selected from among acrylate polymers, cellulose derivatives, or mixtures thereof and the poloxamer component are mixed at a weight ratio of 10:1-10:3, preferably 10:1.
  • the controlled release formulation for treating benign prostatic hype ⁇ lasia is prepared by a general method using a spray drier. Specific preparation process is as follows.
  • Tamsulosin hydrochloride is dissolved in a suitable organic solvent.
  • the organic solvent is not specifically limited so long as it can dissolve tamsulosin hydrochloride.
  • the organic solvent is not specifically limited so long as it can dissolve tamsulosin hydrochloride.
  • the acrylate copolymer (at least one component selected from among Eudragit L- 100, Eudragit RS-100 and RL-100) is mixed with the poloxamer (e.g., Poloxamer 188) at a weight ratio of 10:1 ⁇ 10:3, preferably 10:1, and then is dissolved in a suitable organic solvent.
  • the usable organic solvent includes ethanol, acetone, dichloromethane, or mixtures thereof.
  • a weight ratio of the solvent to tamsulosin hydrochloride ranges from 50:1 to 150:1.
  • the mixed solution is spray dried at 55-60°C, to prepare a solid dispersion as a primary release controlling granular form.
  • the above solid dispersion according to the primary embodiment of the present invention may be selectively formulated to dosage forms of injection, powder, granule, tablet, suppository and the like.
  • a controlled release formulation of tamsulosin or pharmaceutically acceptable salts thereof for treating benign prostatic hype ⁇ lasia according to a secondary embodiment of the present invention, below.
  • the formulation according to the secondary embodiment of the present invention is in the granular form, based on granulation of the formulation according to the primary embodiment of the present invention.
  • various excipients and binders are pharmaceutically used.
  • the excipient is exemplified by CMC, calcium phosphate or lactose, and examples of the binder include polyvinylpyrrohdone
  • PNP cellulose derivatives such as methylcellulose, ethylcellulose, hydroxypropylcellulose or hydroxypropylmethylcellulose, alginic acid, sodium alginate, acacia, guar gum, polymethacrylate, gelatin aqueous solution, or mixtures thereof.
  • the prepared granules are coated with a coating agent consisting mainly of a second dissolution controlling agent, thereby realizing a two-step release controlling system.
  • the second dissolution controlling agent is composed of an acrylate polymer, a cellulose derivative, or mixtures thereof.
  • a controlling agent is selected from the group consisting of polymethacrylate methylmethacrylate copolymer (Eudragit L-100), polyethylacrylate methylmethacrylate trimethylammonioethyl methacrylate chloride copolymer (Eudragit RL-100, RS-100), polymethacrylate ethylacrylate copolymer (Eudragit L30D-55), ethylacrylate methylmethacrylate trimethylammonioethyl methacrylate chloride copolymer (Eudragit RL30D), ethylacrylate methylmethacrylate trimethylammonioethyl methacrylate chloride copolymer (Eudragit RS30D), polyethylacrylate methylmethacrylate copolymer (Eudragit ⁇ E30D),
  • a weight ratio of the second dissolution controlling agent constituting the coated layer to tamsulosin hydrochloride ranges from 10:1 to 100:1. If the weight ratio of the above controlling agent is less than 10, initial release rates become high. Meanwhile, if the ratio exceeds 100, dissolution rates become reduced. However, it should be noted that the present invention may be effective even though the amount of the dissolution controlling agent falls outside of the above range.
  • the coating agent may further comprise a fat component for accurate release control.
  • a fat component includes fatty alcohol, fatty acid ester, wax or mixtures thereof.
  • the fatty alcohol includes cetyl alcohol or cetostearyl alcohol.
  • the fatty acid ester includes fatty acid glycerol (Precirol AT05, Compritol 888 ATO, sold by Gattefosse).
  • the wax includes bees wax, or carnaubar wax.
  • a weight ratio of the above fat component to the tamsulosin component is in the range of 1 : 1 to 20: 1.
  • the second dissolution controlling agent and the fat component are mixed at a ratio of 10:1 ⁇ 10:3.
  • the solvent used for the coating agent is not specifically limited so long as it is capable of dissolving the acrylate copolymer and the fat component.
  • the solvent used for the coating agent is not specifically limited so long as it is capable of dissolving the acrylate copolymer and the fat component.
  • a coating process is performed by use of a known fluid bed coating machine, which is usable as a bottom spray system or a top spray system. Operation conditions of the fluid bed coating machine are described later.
  • tamsulosin hydrochloride 1 g was dissolved in 200 ml of ethanol, and 100 g of Eudragit L-100 or Eudragit RL and 10 g of Poloxamer 188 were dissolved in 500 ml of ethanol. Then, the two dissolved solutions were mixed together.
  • the mixed solution was spray dried to obtain a solid dispersion comprising fine powders.
  • 100 g of the solid dispersion was mixed with 540 g of CMC and 60 g of lactose as an excipient, and 900 ml of 5% gelatin aqueous solution as a binder, to prepare granules, which were then air dried.
  • a coating agent having a composition as shown in the following Table 1 was prepared. 500 g of the above granules were coated with the coating agent by use of a fluid bed coating machine (GLATT, Germany) under operation conditions shown in Table 2, below.
  • Example 2 100 g of the solid dispersion prepared from the above example 1 was mixed with 500 g of CMC as the excipient and 1000 ml of 5% PNP aqueous solution as the binder, and formulated to granules, which were then air dried.
  • [C] granules passed through No. 35 sieve the smallest size Of the above classified granules, 300 g of [A] granules were fluid bed coated with 240 ml of the coating agent of the above example 1.
  • Example 5 200 g of [C] granules obtained from the above example 2 were fluid bed coated with 240 ml of the coating agent of the above example 1.
  • Component Eudragit RL-100 10wt%, cetyl alcohol 2 wt% 100 g of the coated granules were uniformly mixed with 24.5 g of CMC- Ca and 500 mg of magnesium stearate, and formulated to tablets using a tableting machine.
  • tamsulosin is contained in the amount of 0.2 mg per each tablet.
  • coated granules and tablets were assayed for dissolution rates according to the following Experimental Example, in order to evaluate release properties.
  • test liquid was filtered with a 0.45 ⁇ m membrane filter, and dissolution rates of tamsulosin HC1 were quantitatively analyzed with HPLC under the following operation conditions given in Table 4, below. Six of each sample obtained in the above examples 1 through 6 were tested. The results are shown in Table 5, below.
  • a single tablet 250 mg, containing 0.2 mg of tamsulosin HCl was used as a unit dosage form, and subjected to the dissolution test.
  • the present invention provides a controlled release formulation of tamsulosin or pharmaceutically acceptable salts thereof for treatment of benign prostatic hype ⁇ lasia, simply prepared by a spray drying process.
  • a coating amount is adjusted, whereby initial release profiles of the above drug component can be accurately controlled.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Urology & Nephrology (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

L'invention concerne une formulation à libération contrôlée de tamsulosine ou de sels acceptables d'un point de vue pharmaceutique de celle-ci, utilisée dans le traitement de l'hyperplasie prostatique bénigne, avantageuse en ce qu'elle nécessite une préparation simple et présente des profils de libération initiale pouvant être précisément réglés par ajustement d'une quantité d'enrobage lors de la granulation et de l'enrobage de la formulation. Ladite formulation à libération contrôlée comprend de la tamsulosine ou des sels acceptables d'un point de vue pharmaceutique de celle-ci comme ingrédient actif, et un agent de régulation de la dissolution du composant de tamsulosine comprenant un polymère ou copolymère d'acrylate et un poloxamère. La formulation à libération contrôlée comprend, de plus, un premier système de contrôle de la libération contenant de la tamsulosine ou des sels acceptables d'un point de vue pharmaceutique de celle-ci, et un premier agent de régulation de la dissolution contenant un polymère ou copolymère d'acrylate et un poloxamère, et un second système de contrôle de la libération comprenant le premier système de contrôle de libération enrobé d'un agent d'enrobage contenant au moins un second agent de contrôle de la dissolution. L'invention concerne également un procédé de préparation d'une telle formulation à libération contrôlée.
PCT/KR2003/000658 2002-11-22 2003-04-02 Formulation a liberation controlee de tamsulosine ou de sels acceptables d'un point de vue pharmaceutique de celle-ci, utilisee dans le traitement des signes et des symptomes de l'hyperplasie prostatique benigne Ceased WO2004047811A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003219573A AU2003219573A1 (en) 2002-11-22 2003-04-02 Controlled release formulation of tamsulosin or pharmaceutically acceptable salts thereof for treatment of the signs and symptoms of benign prostatic hyperplasia

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020020073182A KR100592512B1 (ko) 2002-11-22 2002-11-22 탐술로신 또는 약제학적으로 허용되는 이의 염을활성성분으로 하는 서방성 배뇨장애 치료제
KR10-2002-0073182 2002-11-22

Publications (1)

Publication Number Publication Date
WO2004047811A1 true WO2004047811A1 (fr) 2004-06-10

Family

ID=32388202

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2003/000658 Ceased WO2004047811A1 (fr) 2002-11-22 2003-04-02 Formulation a liberation controlee de tamsulosine ou de sels acceptables d'un point de vue pharmaceutique de celle-ci, utilisee dans le traitement des signes et des symptomes de l'hyperplasie prostatique benigne

Country Status (4)

Country Link
JP (1) JP2004175781A (fr)
KR (1) KR100592512B1 (fr)
AU (1) AU2003219573A1 (fr)
WO (1) WO2004047811A1 (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005030179A1 (fr) * 2003-09-29 2005-04-07 Cj Corporation Formulations a liberation lente
WO2005053659A1 (fr) * 2003-12-03 2005-06-16 Natco Pharma Limited Preparation pharmaceutique amelioree contenant un sel de tamsulosine et procede de fabrication
WO2020208202A1 (fr) * 2019-04-11 2020-10-15 Add Advanced Drug Delivery Technologies Ltd. Procédé de production continue de granulés de principe actif
US11135242B2 (en) * 2016-07-06 2021-10-05 Calm Water Therapeutics Llc Bi-functional co-polymer use for ophthalmic and other topical and local applications

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20060093931A (ko) * 2005-02-23 2006-08-28 센츄론(주) 펠렛타입의 방출제어형 탐술로신 제제
KR100706036B1 (ko) * 2005-04-04 2007-04-11 대화제약 주식회사 염산 탐술로신 서방성 정제 및 그의 간단한 제조방법
US8216495B2 (en) * 2008-03-25 2012-07-10 Formac Pharmaceuticals N.V. Preparation method for solid dispersions
KR102027912B1 (ko) * 2011-02-15 2019-10-02 지엘팜텍주식회사 경구투여용 탐술로신 또는 이의 약제학적으로 허용되는 염을 포함하는 서방성 삼중정제

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4772475A (en) * 1985-03-08 1988-09-20 Yamanouchi Pharmaceutical Co., Ltd. Controlled-release multiple units pharmaceutical formulation
EP1064938A1 (fr) * 1999-06-28 2001-01-03 Sanofi-Synthelabo Formes pharmaceutiques à libération contrôlée avec au moins une impulsion temporelle
EP1088551A1 (fr) * 1998-06-26 2001-04-04 Yamanouchi Pharmaceutical Co. Ltd. Compositions medicinales destinees au traitement de l'insuffisance d'evacuation
WO2001037808A1 (fr) * 1999-11-23 2001-05-31 Lipocine, Inc. Excipients solides pour administration amelioree d'ingredients actifs contenus dans des compositions pharmaceutiques

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR0178099B1 (ko) * 1996-08-22 1999-03-20 정도언 방출제어형 이부프로펜 과립제 및 그의 제조방법
US7919119B2 (en) * 1999-05-27 2011-04-05 Acusphere, Inc. Porous drug matrices and methods of manufacture thereof

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4772475A (en) * 1985-03-08 1988-09-20 Yamanouchi Pharmaceutical Co., Ltd. Controlled-release multiple units pharmaceutical formulation
EP1088551A1 (fr) * 1998-06-26 2001-04-04 Yamanouchi Pharmaceutical Co. Ltd. Compositions medicinales destinees au traitement de l'insuffisance d'evacuation
EP1064938A1 (fr) * 1999-06-28 2001-01-03 Sanofi-Synthelabo Formes pharmaceutiques à libération contrôlée avec au moins une impulsion temporelle
WO2001037808A1 (fr) * 1999-11-23 2001-05-31 Lipocine, Inc. Excipients solides pour administration amelioree d'ingredients actifs contenus dans des compositions pharmaceutiques

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005030179A1 (fr) * 2003-09-29 2005-04-07 Cj Corporation Formulations a liberation lente
WO2005053659A1 (fr) * 2003-12-03 2005-06-16 Natco Pharma Limited Preparation pharmaceutique amelioree contenant un sel de tamsulosine et procede de fabrication
US11135242B2 (en) * 2016-07-06 2021-10-05 Calm Water Therapeutics Llc Bi-functional co-polymer use for ophthalmic and other topical and local applications
WO2020208202A1 (fr) * 2019-04-11 2020-10-15 Add Advanced Drug Delivery Technologies Ltd. Procédé de production continue de granulés de principe actif
CN114302711A (zh) * 2019-04-11 2022-04-08 埃德先进药物输送技术有限责任公司 连续制造有效成分颗粒的方法

Also Published As

Publication number Publication date
JP2004175781A (ja) 2004-06-24
KR100592512B1 (ko) 2006-07-03
AU2003219573A1 (en) 2004-06-18
KR20040045148A (ko) 2004-06-01

Similar Documents

Publication Publication Date Title
US6576260B2 (en) Sustained-release form of administration containing tramadol saccharinate
RU2240786C2 (ru) Пероральные лекарственные формы пролонгированного действия
US20230240994A1 (en) Medicament-containing hollow particle
BG63708B1 (bg) Лекарствени форми на трамадол
CN109562072B (zh) 包括含有盐酸坦索罗辛的缓释丸粒的具有受控的溶出度的用于口服给药的药物制剂
JP2002542208A (ja) 回腸胆汁酸輸送阻害剤化合物を含む回腸投与のための経口製剤
JP2010285445A (ja) 担体粒子に吸着されたｎｏ−供与ｎｓａｉｄ
JP2007507553A (ja) パントプラゾール多粒子処方
JP2006512358A (ja) タムスロシンの放出制御薬剤組成物
WO2004056336A2 (fr) Systemes d'administration de medicaments a unites multiples et a liberation controlee
US20110244033A1 (en) Tamsulosin pellets for fixed dose combination
JP4438268B2 (ja) 薬物顆粒の製造方法、および薬物顆粒、ならびにそれを用いた医薬製剤
WO2004047811A1 (fr) Formulation a liberation controlee de tamsulosine ou de sels acceptables d'un point de vue pharmaceutique de celle-ci, utilisee dans le traitement des signes et des symptomes de l'hyperplasie prostatique benigne
US20150140089A1 (en) Novel formulations of nitrofurans including nifurtimox with enhanced activity with lower toxicity
JP2009191034A (ja) 時限放出製剤
WO2005053659A1 (fr) Preparation pharmaceutique amelioree contenant un sel de tamsulosine et procede de fabrication
JP2009542669A (ja) ピペリジノアルカノールと充血除去剤の組み合わせを含んで成る医薬組成物
JP2007531727A (ja) Ｇａｂａｂ受容体アゴニストを含有する即時放出特性および／または制御放出特性を有する薬学的剤形
JP2007516282A (ja) 放出制御医薬製剤
JP2001002567A (ja) 水溶性薬物を含有する徐放性製剤
KR20060093931A (ko) 펠렛타입의 방출제어형 탐술로신 제제
CN101340894A (zh) 爆裂小丸
EA043575B1 (ru) Фармацевтическая композиция для перорального приема с контролируемой скоростью растворения, содержащая пеллеты с замедленным высвобождением, содержащие тамсулозина гидрохлорид
MX2008008167A (en) Bursting pellets

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NI NO NZ OM PH PL PT RO RU SC SD SE SG SK SL TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LU MC NL PT RO SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP

WWW Wipo information: withdrawn in national office

Country of ref document: JP