WO2010103544A4 - A novel sustained release composition of compounds selected from the class of centrally acting muscle relaxants - Google Patents
A novel sustained release composition of compounds selected from the class of centrally acting muscle relaxants Download PDFInfo
- Publication number
- WO2010103544A4 WO2010103544A4 PCT/IN2010/000137 IN2010000137W WO2010103544A4 WO 2010103544 A4 WO2010103544 A4 WO 2010103544A4 IN 2010000137 W IN2010000137 W IN 2010000137W WO 2010103544 A4 WO2010103544 A4 WO 2010103544A4
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- release
- sustained release
- oral sustained
- hours
- polymers
- Prior art date
Links
Classifications
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4453—Non condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
-
- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0007—Effervescent
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0065—Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—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
- 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
Abstract
Claims
29
STATEMENT UNDER ARTICLE 19
Present invention relates to oral gastro-retentive dosage forms comprising skeletal muscle relaxant which release active medicaments over period of 24 hours thereby achieving maximum absorption providing enhanced therapeutic effect in treatment of mucoskeletal disorders in mammals.
WO2009/013552 (D1) discloses tolperison hydrochloride containing pharmaceutical compositions with controllable release of active agent and process for preparation thereof. Controlled release pharmaceutical composition of D1 comprises multiple granule cores formed with natural anionic polymer and lipophilic excipient, hydrophilic matrix-forming excipient which surrounds the cores, and other pharmaceutically acceptable excipients. D1 does not specify the polymer systems used in the present invention to provide oral sustained release dosage form. The example 7 of D1 suggests that release test was carried for 8 hours and the same is also evident from figure 2. D1 clearly hints that 8 hour release is achieved. From the pattern of 80% in 8 hours, it cannot be speculated that rest of 20% release would be release for another 18 hours . or 16 hours. Neither there is any hint or teaching for therapeutic requirements in D1 for the drug release beyond 8 hours.
WO2004/032927 (D2), EP1 163902 (D3), US5252588 (D4) and EP 029541 1 (D5) relate to transdermal drug delivery systems which has different pharmacokinetics 30 than oral drug delivery route. None of these hints oral sustained release formulation with drug release upto 24 hour.
Accordingly claims 1 and its dependent claims are novel over D1 to D5.
D1 utilizes the formulation strategy as coating the granules with hydrogels which later are embedded in lipophilic excipients and finally compressed into tablet dosage form. The present process does not use such tedious, expensive and complicated procedures and is simple and easy to be industrially applied. Further D1 to D5 does not disclose oral sustained release formulations with drug release upto 24 hours. Accordingly claim 14 is novel. Further none of the prior art specifies the said coloring and coating for giving elegant appearance to the formulation as claimed in claim . Accordingly claim 18 is novel over prior art.
US2005/196451 (D6), an acknowledged prior art, utilizes different grades of Eudragit polymers for sustaining drug release upto 10 hours. D6 utilizes combinations of methacrylic acid polymers which are not cost effective. The release retardant polymers in D6 have different drug release pattern than polymers used in the present invention.
Accordingly prior art D1 to D6 does not motivate a person skilled in the art to arrive at a formulation with drug release upto 24 hours with judicial selection of polymers and its amounts employing simple process. Examples 15 to 19 discloses combinations of various polymer with actives in ratios 1 : 0.5 to 1 : 3, which gives the desired release profile. It is further submitted that claims are not characterized solely by release profile, rather they specify use of polymers in a defined ratio of 1 : 0.5 to 1 : 3.
However to emphasise the distinctness of present invention claims have been amended which may be regarded as amendment with Statement under Article 19.
Priority Applications (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2010800196712A CN102438597A (en) | 2009-03-09 | 2010-03-09 | A novel sustained release composition of compounds selected from the class of centrally acting muscle relaxants |
EP10740754A EP2405900A2 (en) | 2009-03-09 | 2010-03-09 | A novel sustained release composition of compounds selected from the class of centrally acting muscle relaxants |
EA201171109A EA201171109A1 (en) | 2009-03-09 | 2010-03-09 | NEW COMPOSITION OF THE DELAYED RELEASE OF COMPOUNDS SELECTED FROM THE CLASS OF MINORALEXANTS OF CENTRAL ACTION |
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IN522MU2009 | 2009-03-09 | ||
IN522/MUM/2009 | 2009-03-09 |
Publications (3)
Publication Number | Publication Date |
---|---|
WO2010103544A2 WO2010103544A2 (en) | 2010-09-16 |
WO2010103544A3 WO2010103544A3 (en) | 2011-04-07 |
WO2010103544A4 true WO2010103544A4 (en) | 2011-06-03 |
Family
ID=42728892
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/IN2010/000137 WO2010103544A2 (en) | 2009-03-09 | 2010-03-09 | A novel sustained release composition of compounds selected from the class of centrally acting muscle relaxants |
Country Status (5)
Country | Link |
---|---|
EP (1) | EP2405900A2 (en) |
CN (1) | CN102438597A (en) |
EA (1) | EA201171109A1 (en) |
GE (1) | GEP20135986B (en) |
WO (1) | WO2010103544A2 (en) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RU2012157127A (en) | 2010-07-06 | 2014-08-20 | Навифарм. Ко., Лтд. | PHARMACEUTICAL COMPOSITION CONTAINING DAPOXETINE FOR ORAL ADMINISTRATION WITH SLOW DELIVERY |
WO2012172413A1 (en) | 2011-06-16 | 2012-12-20 | Abbott Healthcare Pvt. Ltd. | Pharmaceutical composition comprising a combination of eperisone and diclofenac and process for preparing thereof |
KR101156054B1 (en) * | 2011-09-05 | 2012-06-20 | 주식회사 네비팜 | A stable and control-released pharmaceutical composition comprising eperisone |
KR101832842B1 (en) * | 2012-01-13 | 2018-02-27 | 한미약품 주식회사 | Pharmaceutical composition with an improved stability comprising eperisone or a pharmaceutically acceptable salt thereof and specific acidifying agent |
EP2875359A4 (en) | 2012-03-30 | 2015-08-19 | Charles R Drew University Of Medicine And Science | Compositions and methods for treating or preventing metabolic syndrome disorders |
CN102895206A (en) * | 2012-10-31 | 2013-01-30 | 中国药科大学 | Rhizoma bletillae polysaccharide gastric-floating tablet and preparation method and application thereof |
US20140271923A1 (en) | 2013-03-14 | 2014-09-18 | Christopher Brian Reid | Compositions & formulations for preventing and treating chronic diseases that cluster in patients such as cardiovascular disease, diabetes, obesity, polycystic ovary syndrome, hyperlipidemia and hypertension, as well as for preventing and treating other diseases and conditions |
KR101497354B1 (en) * | 2013-03-29 | 2015-03-02 | 초당약품공업 주식회사 | Slow release pharmaceutical composition having Eperisone as active ingredient |
CN103432093B (en) * | 2013-08-31 | 2015-03-25 | 西南大学 | Pridinol methanesulfonate matrix sustained-release tablet and preparation method thereof |
ES2582878T3 (en) * | 2013-09-12 | 2016-09-15 | Sanovel Ilac Sanayi Ve Ticaret A.S. | Pharmaceutical formulation comprising a combination of a muscle relaxant and an analgesic |
PL2848260T3 (en) * | 2013-09-12 | 2016-09-30 | Novel formulations of thiocolchicoside | |
RS54912B1 (en) * | 2013-09-12 | 2016-10-31 | Sanovel Ilac Sanayi Ve Ticaret As | Sustained release pharmaceutical formulations of thiocolchicoside |
CN104688709A (en) * | 2015-03-24 | 2015-06-10 | 北京世桥生物制药有限公司 | Fumaric acid quetiapine composition sustained-release tablet and preparing method thereof |
WO2018044020A1 (en) * | 2016-08-29 | 2018-03-08 | 초당약품공업 주식회사 | Method for preparing eperisone sustained release microsphere, and composite preparation of eperisone sustained release microsphere and aceclofenac |
TR201720293A2 (en) | 2017-12-13 | 2019-06-21 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Tolperisone and non-selective cox inhibitor combinations |
TR201720289A2 (en) * | 2017-12-13 | 2019-06-21 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Tolperizon and Selective COX-2 Inhibitor Combinations |
TR201819202A2 (en) * | 2018-12-12 | 2020-06-22 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | A COMBINATION CONTAINING ONE MULTIPLE SCLEROSIS AGENT AND AT LEAST ONE MUSCLE RELAXING AGENT |
TR201906487A1 (en) | 2019-04-30 | 2020-11-23 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | PHARMACEUTICAL COMPOSITIONS CONTAINING TOLPERISONE AND NIMESULIDE COMBINATIONS |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
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JPH0720866B2 (en) * | 1987-05-15 | 1995-03-08 | 三生製薬株式会社 | Transdermal preparation containing eperisone or tolperisone or their salts |
JPS6485915A (en) | 1987-09-28 | 1989-03-30 | Eisai Co Ltd | Hypotensor |
US5252588A (en) * | 1990-04-27 | 1993-10-12 | Sekisui Kagaku Kogyo Kabushiki Kaisha | Percutaneously absorbable crosslinked polyvinylpyrrolidone eperisone or tolperisone preparation |
WO1992017166A1 (en) | 1991-04-08 | 1992-10-15 | Nippon Shinyaku Co., Ltd. | Capsule |
AT409083B (en) | 1999-04-01 | 2002-05-27 | Sanochemia Pharmazeutika Ag | PHARMACEUTICAL PREPARATION CONTAINING TOLPERISON FOR ORAL ADMINISTRATION |
US6753011B2 (en) | 2000-01-14 | 2004-06-22 | Osmotica Corp | Combined diffusion/osmotic pumping drug delivery system |
KR100433614B1 (en) * | 2000-06-16 | 2004-05-31 | 주식회사 태평양 | Transdermal Preparation Containing Hydrophilic or Salt-form Drug |
US6733781B2 (en) | 2000-12-06 | 2004-05-11 | Wyeth | Fast dissolving tablet |
US20040224012A1 (en) | 2001-10-05 | 2004-11-11 | Pichit Suvanprakorn | Topical application and methods for administration of active agents using liposome macro-beads |
KR100511492B1 (en) * | 2002-10-11 | 2005-08-31 | 주식회사 태평양 | Transdermal preparations comprising eperisone, tolperisone or salts thereof |
AT500144A1 (en) * | 2004-03-05 | 2005-11-15 | Sanochemia Pharmazeutika Ag | TOLPERISON-CONTAINING PHARMACEUTICAL PREPARATION WITH CONTROLLABLE ACTIVE INGREDIENTS FOR ORAL ADMINISTRATION |
US20060004050A1 (en) | 2004-07-02 | 2006-01-05 | Speicher Brian T | Compositions and methods for the prevention or treatment of pain and other nervous system disorders |
CN101002752A (en) * | 2005-09-26 | 2007-07-25 | 刘凤鸣 | Slow release preparation of tropyone |
MX2008013437A (en) | 2006-04-20 | 2009-03-06 | Sanochemia Pharmazeutika Ag | Method for administering tolperisone. |
HUP0700485A3 (en) * | 2007-07-23 | 2010-01-28 | Richter Gedeon Nyrt | Pharmaceutical composition with controlled release containing tolperisone |
-
2010
- 2010-03-09 WO PCT/IN2010/000137 patent/WO2010103544A2/en active Application Filing
- 2010-03-09 CN CN2010800196712A patent/CN102438597A/en active Pending
- 2010-03-09 GE GEAP201012409A patent/GEP20135986B/en unknown
- 2010-03-09 EP EP10740754A patent/EP2405900A2/en not_active Withdrawn
- 2010-03-09 EA EA201171109A patent/EA201171109A1/en unknown
Also Published As
Publication number | Publication date |
---|---|
WO2010103544A3 (en) | 2011-04-07 |
EP2405900A2 (en) | 2012-01-18 |
CN102438597A (en) | 2012-05-02 |
EA201171109A1 (en) | 2012-03-30 |
GEP20135986B (en) | 2013-12-10 |
WO2010103544A2 (en) | 2010-09-16 |
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