Novel cocrystals / molecular salts of metformin with oleoylethanolamide as an effective anti-diabetic + anti- obesity agent 机翻标题: 暂无翻译,请尝试点击翻译按钮。

公开号/公开日
WO2012090225 A2 2012-07-05 [WO201290225]WO2012090225 A3 2016-05-26 [WO201290225] / 2012-07-052016-05-26
申请号/申请日
2011WO-IN00903 / 2011-12-29
发明人
REDDY JAGGAVARAPU SATYANARAYANA;DANDELA RAMBABU;VISWANADHA GANESH SARASWATULA;NAGALAPALLI RAVIKUMAR;SOLOMON ANAND KAMALAKARAN;JAVED IQBAL;KRUTHIVENTI ANIL KUMAR;
申请人
NUTRACRYST THERAPEUTICS PRIVATE;
主分类号
IPC分类号
A01N-037/52A61K-031/155
摘要
(WO201290225) The present invention discloses novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide in fixed stoichiometric ratio at lower dosage, with improved residence time thereby increasing the bioavailability and efficacy, as anti- diabetic agent.  The invention further discloses a pharmaceutical composition comprising co- crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide with other antidiabetic agents.
机翻摘要
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地址
代理人
代理机构
;
优先权号
2010IN-DE03159 2010-12-29
主权利要求
(WO201290225) We Claim, 1. Novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts as API with oleoylethanolamide in fixed stoichiometric ratio, at lower dosage, with improved residence time, increased bioavailability and efficacy, as anti-diabetic agent. 2. Novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide as claimed in claim 1, wherein metformin and the oleoylethanolamide present in a molar ratio 1 : 1. 3. Novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide as claimed in claim 1, wherein the pharamaceutically acceptable salts of metformin comprises organic or inorganic salts. 4. Novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide as claimed in claim 3, wherein the inorganic or organic salts selected from phosphates, sulfates, hydrobromides, salicylates, maleates, benzoates, succinates, ethanesulfonates, fumarates, glycolate salts of metformin; p-chlorophenoxyacetic acid salt, pamoate, orotates, (4-chlorophenoxy) isobutyrates, clofibrate, acetylsalicylate, theophyllin-7-acetate, nicotinic acid, adamantoate, zinc-chlorophyll in, hydroxy acid salts such as salts of hydroxy aliphatic dicarboxylic acids selected from mesotartaric acid, tartaric acid, mesoxalic acids, and oxidized maleates; tannic acid, 3-methyl-pyrazole-5-carboxylic acids or other 5-member heterocycle carboxylic acids, as sulfamido aryloxyalkyl carboxylic acid, trimethoxy benzoic acid, dichloroacetic acid, salts of dibasic acids (2:1 molar ratio), preferably metformin (2:1) fumarate and metformin (2: 1) succinate. 5. Novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide as claimed in claim 1 , having characteristic peaks in a powder X-ray diffraction pattern at 16.2, 16.6, 17.9,24.6,28.4,29.0. 6. Novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide as claimed in claim 1 , having characteristic peaks in IR at -3296 cm-1, 3365cm-l , 3176cm- 1,1644cm- 1 , 1567cm-l, 1059cm-l . 7. Novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide as claimed in claim 1, exhibit DSC endotherm at 123°C and 205 °C. 8. A fixed dose pharmaceutical composition comprising co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide with other antidiabetic agents. 9. The fixed dose pharmaceutical composition as claimed in claim 8, wherein the antidiabetic agents selected from DPP-IV inhibitors, sulfonylureas, thiazolidinediones and alpha-glucosidase inhibitors. 10. The fixed dose pharmaceutical composition as claimed in claim 8, wherein DPP- 4 inhibitors selected from sitagliptin, vildagliptin, dutogliptin ,saxagliptin, linagliptin, gemigliptin and alogliptin. 11. The fixed dose pharmaceutical composition as claimed in claim 8, wherein sulfonylureas of first generation selected from carbutamide, acetohexamide, chlorpropamide, tolbutamide, tolazamide and second generation sulfonyl ureas selected from glipizide, gliclazide, glibenclamide, gliquidone, glycopyramide and glimepiride. 12. The fixed dose pharmaceutical composition as claimed in claim 8, wherein the thiazolidinediones selected from rosiglitazone and pioglitazone. 13. The fixed dose pharmaceutical composition as claimed in claim 8, wherein alpha- glucosidase inhibitors selected from acrabose. 14. A pharmaceutical composition comprising novel synergistic co-crystal of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide as claimed in claim 1, in association with one or more pharmaceutically acceptable carriers/excipients. 15. The pharmaceutical composition as claimed in claim 16, wherein said pharmaceutical composition may be formulated in oral dosage form such as tablets, powders, capsules, liquid dosage forms as well as parenteral dosage forms. 16. The pharmaceutical composition as claimed in claim 16, wherein said pharmaceutical composition may be administered as sustained, controlled, modified and immediate dosage forms. 17. Novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide as claimed in claim 1 , for the treatment of metabolic syndrome such as diabetes, obesity, elevated triglyceride and cholesterol levels. 18. Novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide as claimed in claim 1, wherein said pharmaceutical composition is prepared in the form of raw powders or granules dispersed in a suitable aqueous or non-aqueous liquid(s), pellets, beads, micro or nano particles, micro or a solvated powders, sachets, semisolids, an Injectable preparations, a tablets, a capsules or a suitable specific two- or three-dimensional matrix compositions. 19. Novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide as claimed in claim 1, wherein said pharmaceutical composition is a single layer or a bilayer tablet. 20. Novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide as claimed in claim 1, wherein said composition is prepared by dry granulation, wet granulation and / or direct compression using aqueous / Non aqueous solvent further fabricated into the single layer, bilayer, and multilayer and / or multicoated tablet dosage forms. 21. Novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide as claimed in claim 1, wherein said composition is prepared by homogenization, emulsification comprising o/w, w/o or multiple emulsion (s), hot-melt fusion, lyophilization and/or precipitation. 22. Use of novel synergistic pharmaceutical co-crystals of Metformin or its pharmaceutically acceptable salts and oleoylethanolamide for reducing diabetes, obesity, elevated triglyceride and cholesterol levels. 23. A method for treating diabetes, obesity, elevated triglyceride and cholesterol levels comprising administering an effective amount of the pharmaceutical composition to the subject suffering from said disease.
法律状态
(WO201290225) LEGAL DETAILS FOR WO2012090225  Actual or expected expiration date=2014-06-29    Legal state=DEAD    Status=LAPSED     Event publication date=2011-12-29  Event code=WO/APP  Event indicator=Pos  Event type=Examination events  Application details  Application country=WO WOIN2011000903  Application date=2011-12-29  Standardized application number=2011WO-IN00903     Event publication date=2012-07-05  Event code=WO/A2  Event type=Examination events  International application published with declaration under Article 17 (2) (a)  Publication country=WO  Publication number=WO2012090225  Publication stage Code=A2  Publication date=2012-07-05  Standardized publication number=WO201290225     Event publication date=2014-06-29  Event code=WO/EETL  Event type=Event indicating Not In Force  PCT Application validity period expired.    Event publication date=2016-05-26  Event code=WO/A3  Event indicator=Pos  Event type=Examination events  Later publication of ISR with revised front page  Publication country=WO  Publication number=WO2012090225  Publication stage Code=A3  Publication date=2016-05-26  Standardized publication number=WO201290225  LEGAL DETAILS FOR DESIGNATED STATE DE  Actual or expected expiration date=2013-07-01    Legal state=DEAD    Status=LAPSED   Corresponding cc:  Designated or member state=DE     Event publication date=2013-07-01  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
专利类型码
A2A3
国别省市代码
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