Pharmaceutical formulations containing metformin 机翻标题: 暂无翻译,请尝试点击翻译按钮。

公开号/公开日
WO2007103563 A2 2007-09-13 [WO2007103563]WO2007103563 A3 2008-01-03 [WO2007103563] / 2007-09-132008-01-03
申请号/申请日
2007WO-US06055 / 2007-03-09
发明人
VISHNUPAD KRISHNA;
申请人
NEUROSCI;
主分类号
IPC分类号
A01N-047/28A61K-031/155A61K-031/17
摘要
(WO2007103563) Controlled delivery and instant release combination compositions of metformin or salts thereof and glimepiride and the process of making the same are disclosed.  Metformin and glimepiride are granulated with a binder and further dispersed in a rate-controlling matrix that results in a controlled release formulation that increases patient compliance.  In a further illustrative embodiment metformin and glimepiride are formulated in an instant release presentation using pharmaceutical excipients known in the art.
机翻摘要
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地址
代理人
代理机构
;
优先权号
2006US-60780944 2006-03-09
主权利要求
(WO2007103563) What is claimed: 1. A pharmaceutical composition comprising, a first active ingredient comprising a sulfonylurea or a pharmaceutically acceptable salt thereof as active ingredient, a second active ingredient a comprising biguamide or a pharmaceutically acceptable salt thereof as active ingredient as active ingredient. 2. The formulation as defined in claim 1 wherein said biguamide is metformin. 3. The formulation as defined in claim 2 wherein said sulfonylurea is glimepiride hydrochloride in an amount ranging from about lmg to about 8mg and, said metformin is present in an amount ranging from about 10 mg to about 4000 mg. 4. The formulation as defined in claim 2 which further comprises an extended release polymer having a predetermined rate of degradation. 5. The formulation as defined in claim 3, wherein said glimepiride hydrochloride and/or said metformin are present as biodegradable microspheres having a biodegradable shell coating and where said shell coating has a predetermined rate of degradation. 6. A method of administering glimepiride hydrochloride and metformin to a mammal, which comprises treating the mammal with the formulation defined in claim 2. 7. A method for producing a controlled release formulation, which comprises: (a) producing a first component comprising a biodegradable material having a predetermined rate of degradation to provide a predetermined delay in the time period of release of the contents destined to be enclosed by said component; (b) producing a second component comprising metformin and having a secondary layer comprising glimepiride hydrochloride partially enclosing said second component; and (c) combining said first and second component forming an extended release matrix allowing said metformin and glimepiride to be released in a therapeutically acceptable manner. 8. A method of producing a combined formulation of glimepiride hydrochloride and metformin, which comprises: (a) providing a therapeutic selected amount of metformin or a pharmaceutically acceptable salt thereof; and (b) providing a therapeutic selected amount of glimepiride or a pharmaceutically acceptable salt thereof; and combining said metformin and said glimepiride in a pharmaceutically acceptable binders and exceipents. 9. A method of treating diabetes mellitus in a patient in need thereof, which comprises administering to the patient the formulation of claim 2 wherein said active ingredients are each present in an therapeutically effective amount. 10. A pharmaceutical composition in a single integral unit consisting essentially of a therapeutically effective amount of glimepiride hydrochloride combined with a therapeutically effective amount of metformin. 11. A pharmaceutical composition in a single integral unit consisting essentially of a therapeutically effective amount of glimepiride hydrochloride combined with a therapeutically effective amount of buformin. 12. A method of treating diabetes mellitus in a patient in need thereof, which comprises, administering to the patient the integral composition of claim 10. 13. A method of treating diabetes mellitus in a patient in need thereof, which comprises, administering to the patient the integral composition of claim 11. 14. A method of treating diabetes mellitus in a patient in need thereof, which comprises, administering to the patient the composition of claim 1 wherein the biguamide is phenformin. 15. A method of treating diabetes mellitus in a patient in need thereof, which comprises, administering to the patient the composition of claim 1 wherein the biguamide is buformin. 16. A process for preparing an oral dosage form of metformin in combination with a sulfonylurea or a pharmaceutically acceptable salt thereof wherein the hardness of said oral dosage form is at least about 8kg/cm2comprising steps of (i) granulating metformin hydrochloride with about 0.1 to about 10% binder (ii) dispersing the resulting granules in one or more rate-controlling hydrophilic polymers; (iii) blending in a sulfonylurea; and (iv) compressing the composition so obtained into tablets of at least about 8kg/cm2 . 17. The process of claim 16 further comprising the step of adding about 0.5 % to about 4% of unbound metformin or pharmaceutically acceptable salt thereof wherein said unbound metformin is dispersed within said one or more rate-controlling hydrophilic polymers. 18. The process of claim 16 wherein said binder is selected from the group consisting of copovidone, polyvinyl pyrrolidone, hydroxy propyl methyl cellulose, hydroxy propyl cellulose, hydroxy ethyl cellulose, polyvinyl alcohol and sodium carboxy methyl cellulose. 19. The process of claim 16 wherein said binder copovidone. 20. The process of claim 16 further comprising the step of adding one or more tableting lubricants in an amount within the range of from about 0.2 to about 8% 21. The process of claim 16 said hydrophilic polymers is selected from the group consisting of Eudragit RS, Eudragit RL, xanthan gum, karaya gum, locust bean gum, guar gum, gelan gum, gum arabic, tragacanth, carrageenan, pectin, carboxymethyl cellulose, agar, alginic acid, sodium alginate polyvinylpyrrolidine, hydroxypropylcellulose, hydroxypropyl methyl cellulose, methyl cellulose, vinyl acetate copolymers, polyethylene oxide, methacrylic acid copolymers, maleic anhydride/methyl vinyl ether copolymers and derivatives and mixtures thereof. 22. The process of claim 16 wherein said hydrophilic polymers is selected from the group consisting of hydroxypropylmethyl cellulose 2208 USP , hydroxypropylmethylcellulose 2910 USP, sodium carboxy methylcellulose and mixtures thereof. 23. The process of claim 16 wherein said sulfonylurea is glimepiride hydrochloride in an amount ranging from about lmg to about 8mg and, said metformin is present in an amount ranging from about 10 mg to about 4000 mg.
法律状态
(WO2007103563) LEGAL DETAILS FOR WO2007103563  Actual or expected expiration date=2009-09-09    Legal state=DEAD    Status=LAPSED     Event publication date=2007-03-09  Event code=WO/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=WO WOUS2007006055  Application date=2007-03-09  Standardized application number=2007WO-US06055     Event publication date=2007-09-13  Event code=WO/A2  Event type=Examination events  International application published without international search report  Publication country=WO  Publication number=WO2007103563  Publication stage Code=A2  Publication date=2007-09-13  Standardized publication number=WO2007103563     Event publication date=2008-01-03  Event code=WO/A3  Event indicator=Pos  Event type=Examination events  Later publication of ISR with revised front page  Publication country=WO  Publication number=WO2007103563  Publication stage Code=A3  Publication date=2008-01-03  Standardized publication number=WO2007103563     Event publication date=2009-09-09  Event code=WO/EETL  Event type=Event indicating Not In Force  PCT Application validity period expired. LEGAL DETAILS FOR DESIGNATED STATE CA2645318  Actual or expected expiration date=2011-03-09    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=CA Corresponding appl: CA2645318  Application date in the designated or member state=2007-03-09   Application number in the designated or member state=2007CA-2645318 Corresponding cc:  Designated or member state=CA Corresponding pat: CA2645318  Publication stage code in the designated or member state=A1  Publication date in the designated or member state=2007-09-13   Publication number in the designated or member state=CA2645318    Event publication date=2008-09-09  Event code=WO/WWE  Event indicator=Pos  Event type=Entry into national phase  Wipo information: entry into national phase Corresponding cc:  Designated or member state=CA     Event publication date=2011-03-09  Event code=CA/STCHG  Patent Status changed by the national office Corresponding cc:  Designated or member state=CA  LEGAL DETAILS FOR DESIGNATED STATE DE  Actual or expected expiration date=2008-09-10    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=DE     Event publication date=2008-09-10  Event code=WO/NENP  Event type=Event indicating Not In Force  Non-entry into the national phase in: Corresponding cc:  Designated or member state=DE  LEGAL DETAILS FOR DESIGNATED STATE EP2001302  Actual or expected expiration date=2010-10-01    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=EP Corresponding appl: EP07752735  Application date in the designated or member state=2007-03-09   Application number in the designated or member state=2007EP-0752735 Corresponding cc:  Designated or member state=EP Corresponding pat: EP2001302  Publication stage code in the designated or member state=A2  Publication date in the designated or member state=2008-12-17   Publication number in the designated or member state=EP2001302    Event publication date=2007-11-07  Event code=WO/121  Event type=Designated states  EP: The EPO has been informed by wipo that ep was designated in this application Corresponding cc:  Designated or member state=EP     Event publication date=2011-05-18  Event code=EP/STCHG  Patent Status changed by the national office Corresponding cc:  Designated or member state=EP
专利类型码
A2A3
国别省市代码
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