WO2014167439A1 - Compositions pharmaceutiques à libération modifiée de topiramate ou de sels de celui-ci - Google Patents

Compositions pharmaceutiques à libération modifiée de topiramate ou de sels de celui-ci Download PDF

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Publication number
WO2014167439A1
WO2014167439A1 PCT/IB2014/060054 IB2014060054W WO2014167439A1 WO 2014167439 A1 WO2014167439 A1 WO 2014167439A1 IB 2014060054 W IB2014060054 W IB 2014060054W WO 2014167439 A1 WO2014167439 A1 WO 2014167439A1
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WO
WIPO (PCT)
Prior art keywords
topiramate
components
release
pharmaceutical composition
salts
Prior art date
Application number
PCT/IB2014/060054
Other languages
English (en)
Inventor
Girish Kumar Jain
Venkataramana NAIDU
Atul Patil
Original Assignee
Wockhardt Limited
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 Wockhardt Limited filed Critical Wockhardt Limited
Priority claimed from IN1157MU2013 external-priority patent/IN2013MU01157A/en
Priority claimed from IN1156MU2013 external-priority patent/IN2013MU01156A/en
Publication of WO2014167439A1 publication Critical patent/WO2014167439A1/fr

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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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants

Definitions

  • the present invention relates to modified release pharmaceutical compositions of topiramate or salts thereof.
  • a modified release pharmaceutical composition of topiramate can be formed.
  • the composition may provide extended and specific release of topiramate or salts thereof to achieve therapeutically effective plasma concentration over a period of 24 hours to treat epileptic conditions when administered to a patient in need thereof.
  • the invention also includes process of preparing such composition.
  • Topiramate is a sulfamate-substituted monosaccharide approved in the US for use as an antiepileptic agent, as an adjuvant therapy for patients with partial onset seizures or primary generalized tonic-clonic seizures and marketed under the trade name of Topamax ® . Topiramate has been also approved for the prophylaxis treatment of migraine headache. Chemically, topiramate is 2,3:4,5 Di-O-isopropylidene-p-D-fructopyranose sulfamate and has the following structural formula:
  • Topamax ® an IR dosage form
  • Topamax ® an IR dosage form
  • a peak in plasma concentrations of the drug and the fluctuations associated with the peaks and valleys of blood plasma levels of the drug causing undesirable effects.
  • it is associated with severe side-effects including somnolence, dizziness, ataxia, speech disorders and related speech problems, psychomotor slowing, abnormal vision, difficulty with memory, paresthesia, diplopia, renal calculi (kidney stones), hepatic failure, pancreatitis, renal tubular acidosis, acute myopia and secondary angle closure glaucoma.
  • administration of the medicament in this manner is cumbersome and patients can forget to take their medication in a timely manner.
  • the extended release of drug can be achieved either by coating the composition with release modifying substance or by dispersing drug in a matrix comprising one or more release modifying substance.
  • the drug is released over a period of time in the gastrointestinal tract upon dissolution or erosion of the matrix.
  • Extended-release dosage forms comprising a matrix system are conveniently prepared as compressed tablets.
  • drugs having relatively high solubility in water for example a solubility of about 5 mg/ml or greater, present challenges to the formulator wishing to provide an extended-release dosage form and the higher the solubility the greater are the challenges.
  • US Patent No. 7,125,560 discloses a pharmaceutical composition in the form of core particles containing topiramate with sugar spheres as diluent wherein the core particles are coated with a taste mask coating.
  • US Patent Nos. 7,61 1 ,728 and 7,351 ,695 discloses osmotic release pharmaceutical composition of topiramate and acceptable salts thereof.
  • US Patent No. 6,923,988 teaches the pharmaceutical compositions which can be used for improved delivery of hydrophilic or hydrophobic pharmaceutical active ingredients by encapsulating the composition with different combinations of pharmaceutical active ingredients, hydrophilic surfactant, lipophilic surfactants and triglycerides.
  • U.S. Patent No. 4,590,062 discloses a compressed product containing an active produced by dry blending with a matrix combination of a hydrophobic polymer (e.g. ethylcellulose) and a wax, fatty acid, neutral lipid or combination thereof.
  • a hydrophobic polymer e.g. ethylcellulose
  • U.S. Patent Application No. US 20090004281 discloses a modified release multiparticulate osmotic delivery system for oral administration.
  • the composition includes an osmotic subcoat applied to core that includes at least one drug in combination with at least one pharmaceutically acceptable excipient.
  • U.S. Patent Application No. US 20080131501 discloses a pharmaceutical composition which provides enhanced immediate release formulations of topiramate, in which 80% of the active ingredient is released in the period of time of not more than 30 min.
  • the inventors of the present invention have surprisingly found that by using two different types of components of topiramate in the composition, at least one of it being in the form of a matrix of topiramate and release modifying substances, the resulting composition may exhibit release of topiramate over a 24 hour period and/or reduce or eliminate the side effects associated with peaking and fluctuating plasma levels of topiramate.
  • composition of the present invention relates to modified release pharmaceutical compositions comprising at least two types of components, wherein at least one type of the component comprises a matrix of topiramate or salts thereof and one or more release modifying substances.
  • the component of the composition comprising said matrix exhibits sustained release of topiramate or salts thereof.
  • the composition may provide extended and specific release of topiramate or salts thereof to achieve therapeutically effective plasma concentration over a period of 24 hours to treat epileptic conditions when administered to a patient in need thereof.
  • a modified release pharmaceutical composition comprising at least two types of components, each comprising topiramate or salts thereof, wherein at least one type of the component comprises a matrix of topiramate or salts thereof with one or more release modifying substances and optionally one or more pharmaceutically acceptable excipients.
  • a modified release pharmaceutical composition comprising at least two types of components, each comprising topiramate or salts thereof, wherein at least one type of the component is uncoated and comprises a matrix of topiramate or salts thereof with one or more release modifying substances.
  • a modified release pharmaceutical composition comprising at least two types of components, each comprising topiramate or salts thereof, wherein at least one type of the component comprises a matrix of topiramate or salts thereof with one or more release modifying substances and it exhibits sustained release of topiramate or salts thereof.
  • a modified release pharmaceutical composition comprising at least two types of components, each comprising topiramate or salts thereof, wherein at least one type of the component comprises a matrix of topiramate or salts thereof with one or more release modifying substances and dimension of at least one type of the component is more than 1 .0 mm.
  • a modified release pharmaceutical composition comprising at least two types of components, each comprising topiramate or salts thereof, wherein at least one type of the component comprises a matrix of topiramate or salts thereof with one or more release modifying substances comprises ethyl cellulose, methacrylic acid copolymer, hydroxypropyl cellulose or hydroxypropyl methylcellulose, bees wax, carnauba wax or combination thereof.
  • a modified release pharmaceutical composition comprising at least two types of components, each comprising topiramate or salts thereof exhibits sustained release of topiramate or salts thereof, wherein the first type of the component comprises a matrix of topiramate or salts thereof with one or more release modifying substances and the second type of component exhibits either immediate release or sustained release of topiramate or salts thereof.
  • a modified release pharmaceutical composition comprising at least two types of components, each comprising topiramate or salts thereof, wherein first type of the component comprises a matrix of topiramate or salts thereof with one or more release modifying substances and the second type of the component is coated with one or more hydrophilic and/or hydrophobic coating substances.
  • the hydrophobic release controlling substances preferably polymers are pH dependent or pH independent.
  • a modified release pharmaceutical composition comprising at least two types of components, each comprising topiramate or salts thereof, wherein the first type of the component comprises a matrix of topiramate or salts thereof with one or more release modifying substances and the second type of component is coated with about 1 % to 70% w/w of hydrophilic or hydrophobic coating substances by total weight of another component.
  • a modified release pharmaceutical composition comprising at least two types of components, each comprising topiramate or salts thereof, wherein at least one type of the component comprises a matrix of topiramate or salts thereof with one or more release modifying substances and the components are in the form of pellets, granules, compressed units or combination thereof.
  • a modified release pharmaceutical composition comprising at least two types of components, each comprising topiramate or salts thereof, wherein at least one type of the component is in the form of pellets and comprises a matrix of topiramate or salts thereof with one or more release modifying substances.
  • a modified release pharmaceutical composition comprising at least two types of components, each comprising topiramate or salts thereof, wherein the first type of the component comprises a matrix of topiramate or salts thereof with one or more release modifying substances and the second type of the component comprises inert carriers, preferably in the form of cores, are sequentially coated with one or more topiramate and rate modifying polymer layers at different levels.
  • the inert carrier used in the present invention includes, but are not limited to, a group consisting of cellulose spheres, silicon dioxide, starch and sugar spheres.
  • the amount of the inert carrier in the composition ranges from about 20% to about 95% w/w, and preferably from about 30% to about 90% w/w of the composition.
  • Topiramate is introduced to the inert carrier by techniques known to one skilled in the art such as drug layering, powder coating, extrusion/spheronization, roller compaction or dry/wet granulation.
  • the introduction method is drug layering by spraying a suspension of topiramate and a binder onto the inert carrier.
  • a modified release pharmaceutical composition comprising at least two types of components, each comprising topiramate or salts thereof, wherein at least one type of the component comprises a matrix of topiramate or salts thereof with one or more release modifying substances and exhibits release of more than 80% of topiramate or salts thereof within a period of 24 hours, preferably 16 hours and more preferably 8 hours.
  • a process of preparing the modified release pharmaceutical composition comprises the steps of: (a) mixing topiramate and one or more release modifying substances, optionally with one or more pharmaceutical excipients;
  • step (b) granulating the mixture prepared in step (a) to form topiramate extended release components
  • step (e) granulating the mixture prepared in step (d) to form topiramate immediate release components
  • a modified release pharmaceutical composition comprising at least two types of components, each comprising topiramate or salts thereof, wherein at least one type of the component comprises a matrix of topiramate or salts thereof with one or more release modifying substances and the dosage form retains at least 90% w/w of the potency of topiramate or salt thereof when stored at 40°C and 60% relative humidity for 3 months.
  • the release modifying substances which can be used may be selected from the group consisting of hydrophilic agents (e.g. water-soluble polymers), lipophilic agents (water-insoluble polymers) and inert matrix agents, wherein the hydrophilic agents are selected from the group of pharmaceutical excipients which generate a gel in contact with water, including cellulose derivatives such as hydroxypropyl methyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, methyl cellulose and the like; noncellulose polysaccharides such as galactomannanes, guar gum, carob gum, gum arabicum, alginates, pectins, and the like; polyvinylpyrrolidone; polyvinylacetate polymers and copolymers; acrylic acid polymers and copolymers, polyethylene oxide and mixtures thereof; the lipophilic agents are selected from the group consisting of waxes such as white wax, bees wax, carnauba wax and the like; fatty acids and alcohols such as stearic
  • thermoplastic polymers which are insoluble and indigestible in the gastrointestinal fluids, such as polyvinyl chloride, polyethylene, vinyl acetate/vinyl chloride copolymers, polymethylmethacrylates, polyamides, silicones, ethyl cellulose, polystyrene, and mixtures thereof.
  • topiramate refers to not only topiramate per se, but also its other pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable hydrates, pharmaceutically acceptable enantiomers, pharmaceutically acceptable derivatives, pharmaceutically acceptable polymorphs and pharmaceutically acceptable prodrugs thereof.
  • modified release used throughout the specification shall apply to dosage forms, matrices, particles, coatings, portions thereof, or compositions that alter the release of an active ingredient in any manner.
  • Types of modified release include controlled, prolonged, sustained, extended, delayed, and the likes.
  • matrix used throughout the specification refers to the dispersion of drug within one or more release modifying substances and optionally one or more pharmaceutical excipients.
  • component used throughout the specification refers to mini-tablet, tablet, pellet, bead or granule prepared by standard methods known to the person skilled in the art, including but not limited to compression, granulation, spray coating, and extrusion/spheronization.
  • pellets used throughout the specification refers, but not limited to a carrier for pharmacologically active ingredients. Methods of manufacturing pellets for pharmaceutical use in both conventional (immediate release) and extended release single dosage forms include, but not limited to, extrusion/spheronization.
  • the modified release pharmaceutical composition comprises at least two types of components, at least one type of the component, being uncoated, comprises a matrix of topiramate or salts thereof with one or more release modifying substances and optionally one or more pharmaceutically acceptable excipients.
  • the release modifying substances comprises one or more of ethyl cellulose, methacrylic acid copolymer, hydroxypropyl cellulose or hydroxypropyl methylcellulose, bees wax, carnauba wax or combination thereof.
  • the uncoated component comprising matrix of topiramate or salts thereof with one or more release modifying substances of the modified release pharmaceutical composition exhibits release of more than 80% of topiramate or salts thereof within a period of 24 hours, preferably 16 hours and more preferably 8 hours
  • the dimension of at least one type of the component is more than 1 .0 mm.
  • the modified release pharmaceutical composition comprising at least two types of components, one comprising matrix of topiramate or salts thereof and one or more release modifying substances that exhibits sustained release and the second type of component exhibits either immediate release or sustained release of topiramate or salts thereof.
  • the second type of component of the modified release pharmaceutical composition is coated with one or more hydrophilic and/or hydrophobic coating substances.
  • another type of component of the modified release pharmaceutical composition is coated with about 1 % to 70%w/w of hydrophilic or hydrophobic coating substances by total weight of another component.
  • the components in the modified release pharmaceutical composition are in the form of one or more pellets, granules, compressed units (e.g. tablets, mini-tablets) or combination thereof.
  • the modified release pharmaceutical composition in accordance with the present invention retains at least 90% w/w of the potency of topiramate or salt thereof when stored at 25°C and 40% relative humidity or at 40°C and 25% relative humidity for 3 months.
  • the modified release composition of the present invention can be prepared by methods known to the person skilled in the art.
  • the composition comprises plurality of uncoated units.
  • the uncoated units can be prepared by various methods known to the person skilled in the art, such as extrusion, wet granulation, and dry granulation, followed by compression or slugging.
  • the process of preparing the modified release pharmaceutical composition comprises steps of:
  • step (b) granulating the mixture prepared in step (a) to form topiramate extended release components
  • step (e) granulating the mixture prepared in step (d) to form topiramate immediate release components
  • the modified release pharmaceutical composition of the present invention may be developed in the form a capsule, a tablet, a caplet and a mini-tablet.
  • the dosage form is in the form of a capsule.
  • composition of the present invention may comprise one or more pharmaceutically acceptable excipients selected from, but not limited to, diluent, binder, disintegrant, glidant, lubricant, stabilizing agent, and flavoring agents.
  • pharmaceutically acceptable excipients includes a pharmaceutically acceptable material, composition or vehicle, suitable for administering an active pharmaceutical ingredient. Each excipient should be “acceptable” in the sense of being compatible with the other ingredients of the formulation and not injurious to the patient. Excipients include diluents, binders, disintegrants, glidants, lubricants, flavoring, and others.
  • Diluents increase the bulk of a solid pharmaceutical composition.
  • Exemplary diluents for solid compositions include, but are not limited to, microcrystalline cellulose, microfine cellulose, lactose, starch, pregelatinized starch, calcium carbonate, calcium sulfate, sugar, dextrates, dextrin, dextrose, dibasic calcium phosphate dihydrate, tribasic calcium phosphate, kaolin, magnesium carbonate, magnesium oxide, maltodextrin, mannitol, polymethacrylates, potassium chloride, powdered cellulose, sodium chloride, sorbitol and talc.
  • Solid pharmaceutical compositions that are compressed may include excipients whose functions include helping to bind the active ingredient and other excipients together after compression.
  • binders for solid pharmaceutical compositions include, but are not limited to, acacia, alginic acid, carbomer, carboxymethylcellulose sodium, dextrin, ethyl cellulose, gelatin, guar gum, hydrogenated vegetable oil, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, liquid glucose, magnesium aluminum silicate, maltodextrin, methylcellulose, polymethacrylates, povidone, pregelatinized starch, sodium alginate and starch.
  • Disintegrants increase the dissolution rate of a compacted solid pharmaceutical composition in the patient's stomach, for example.
  • Exemplary disintegrants include, but are not limited to, alginic acid, carboxymethylcellulose calcium, carboxymethylcellulose sodium, colloidal silicon dioxide, croscarmellose sodium, crospovidone, guar gum, magnesium aluminum silicate, methyl cellulose, microcrystalline cellulose, polacrilin potassium, powdered cellulose, pregelatinized starch, sodium alginate, sodium starch glycolate and starch.
  • Glidants can be added to improve the flowability of a non-compacted solid composition and to improve the accuracy of dosing.
  • exemplary excipients that may function as glidants include, but not limited to, colloidal silicon dioxide, magnesium trisilicate, powdered cellulose, starch, talc and tribasic calcium phosphate.
  • a lubricant can be added to the composition to reduce adhesion and ease the release of the product from the dye.
  • exemplary lubricants include, but are not limited to, magnesium stearate, calcium stearate, glyceryl monostearate, glyceryl palmitostearate, hydrogenated castor oil, hydrogenated vegetable oil, mineral oil, polyethylene glycol, sodium benzoate, sodium lauryl sulfate, sodium stearyl fumarate, stearic acid, talc and zinc stearate.
  • the present invention further provides a method of treating epileptic conditions by administering the patient in need thereof the modified release composition of topiramate or salts thereof as substantially described throughout the specification.
  • First (Extended release beads) component of topiramate was prepared by mixing topiramate, HPMC, polyvinylpyrrolidone, ethyl cellulose, methyl methacrylic acid methyl methacrylate polymer dispersion in a mixture of isopropyl alcohol and methylene dichloride. The mixture was granulated to form granules. The granules were then lubricated with magnesium stearate.
  • the second component (Immediate release pellets) was formed by dispersing topiramate in hydroxypropyl methylcellulose solution that contains vitamin E TPGS, Polyoxyl hydrogenated castor oil and sodium lauryl sulfate. The resulting dispersion was then sprayed on to sugar spheres using a fluid bed processor to achieve a desired drug load.
  • the first (Extended release Beads) and second components (Immediate release Pellets) were then filled in to hard gelatin capsules.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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Abstract

La présente invention concerne des compositions pharmaceutiques à libération modifiée de topiramate ou de sels de celui-ci. En particulier, la présente invention concerne des compositions pharmaceutiques à libération modifiée comprenant au moins deux types de composant, au moins un type du composant comprenant une matrice de topiramate ou de sels de celui-ci et une ou plusieurs substances modifiant la libération. La composition peut produire une libération prolongée et spécifique de topiramate ou sels de celui-ci de manière à obtenir une concentration plasmatique et thérapeutiquement efficace sur une période de 24 heures pour traiter des affections épileptiques lorsque qu'elle est administrée à un patient nécessitant cela. L'invention concerne en outre un procédé de préparation d'une telle composition.
PCT/IB2014/060054 2013-03-26 2014-03-22 Compositions pharmaceutiques à libération modifiée de topiramate ou de sels de celui-ci WO2014167439A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IN1157/MUM/2013 2013-03-26
IN1156/MUM/2013 2013-03-26
IN1157MU2013 IN2013MU01157A (fr) 2013-03-26 2014-03-22
IN1156MU2013 IN2013MU01156A (fr) 2013-03-26 2014-03-22

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WO2014167439A1 true WO2014167439A1 (fr) 2014-10-16

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110638791A (zh) * 2019-10-31 2020-01-03 浙江普利药业有限公司 托吡酯缓释胶囊及其制备方法

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US4590062A (en) 1984-04-16 1986-05-20 Tech Trade Corp. Dry direct compression compositions for controlled release dosage forms
WO1999044581A2 (fr) * 1998-03-04 1999-09-10 Ortho-Mcneil Pharmaceutical, Inc. Composition pharmaceutique de topiramate
WO2005065648A2 (fr) * 2003-12-29 2005-07-21 Alza Corporation, Inc., Nouvelles preparations de medicaments et formes posologiques de topiramate
US6923988B2 (en) 1999-11-23 2005-08-02 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US20060034927A1 (en) * 2004-08-04 2006-02-16 Gemma Casadevall Means of delivering drugs in an ascending zero order release pattern
US20060121112A1 (en) * 2004-12-08 2006-06-08 Elan Corporation, Plc Topiramate pharmaceutical composition
WO2008027557A2 (fr) * 2006-08-31 2008-03-06 Spherics, Inc. Compositions à base de topiramate et méthodes permettant d'en augmenter la biodisponibilité
US7351695B2 (en) 2002-02-15 2008-04-01 Ortho-Mcneil Pharmaceuticals, Inc. Topiramate salts and compositions comprising and methods of making and using the same
WO2008061226A2 (fr) * 2006-11-17 2008-05-22 Supernus Pharmaceuticals Inc. Formulations de topiramate à libération prolongée
US20080131501A1 (en) 2006-12-04 2008-06-05 Supernus Pharmaceuticals, Inc. Enhanced immediate release formulations of topiramate
US20090004281A1 (en) 2007-06-26 2009-01-01 Biovail Laboratories International S.R.L. Multiparticulate osmotic delivery system
US7611728B2 (en) 2003-09-05 2009-11-03 Supernus Pharmaceuticals, Inc. Osmotic delivery of therapeutic compounds by solubility enhancement
US20120128778A1 (en) * 2010-11-23 2012-05-24 Nipun Davar Compositions and methods for once-daily administration of a trilayer osmotic tablet

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Publication number Priority date Publication date Assignee Title
US4590062A (en) 1984-04-16 1986-05-20 Tech Trade Corp. Dry direct compression compositions for controlled release dosage forms
WO1999044581A2 (fr) * 1998-03-04 1999-09-10 Ortho-Mcneil Pharmaceutical, Inc. Composition pharmaceutique de topiramate
US7125560B2 (en) 1998-03-04 2006-10-24 Ortho-Mcneil Pharmaceutical, Inc. Pharmaceutical composition of topiramate
US6923988B2 (en) 1999-11-23 2005-08-02 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US7351695B2 (en) 2002-02-15 2008-04-01 Ortho-Mcneil Pharmaceuticals, Inc. Topiramate salts and compositions comprising and methods of making and using the same
US7611728B2 (en) 2003-09-05 2009-11-03 Supernus Pharmaceuticals, Inc. Osmotic delivery of therapeutic compounds by solubility enhancement
WO2005065648A2 (fr) * 2003-12-29 2005-07-21 Alza Corporation, Inc., Nouvelles preparations de medicaments et formes posologiques de topiramate
US20060034927A1 (en) * 2004-08-04 2006-02-16 Gemma Casadevall Means of delivering drugs in an ascending zero order release pattern
US20060121112A1 (en) * 2004-12-08 2006-06-08 Elan Corporation, Plc Topiramate pharmaceutical composition
WO2008027557A2 (fr) * 2006-08-31 2008-03-06 Spherics, Inc. Compositions à base de topiramate et méthodes permettant d'en augmenter la biodisponibilité
WO2008061226A2 (fr) * 2006-11-17 2008-05-22 Supernus Pharmaceuticals Inc. Formulations de topiramate à libération prolongée
US20080131501A1 (en) 2006-12-04 2008-06-05 Supernus Pharmaceuticals, Inc. Enhanced immediate release formulations of topiramate
US20090004281A1 (en) 2007-06-26 2009-01-01 Biovail Laboratories International S.R.L. Multiparticulate osmotic delivery system
US20120128778A1 (en) * 2010-11-23 2012-05-24 Nipun Davar Compositions and methods for once-daily administration of a trilayer osmotic tablet

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110638791A (zh) * 2019-10-31 2020-01-03 浙江普利药业有限公司 托吡酯缓释胶囊及其制备方法

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