JP2017511350A5 - - Google Patents
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- Publication number
- JP2017511350A5 JP2017511350A5 JP2016562508A JP2016562508A JP2017511350A5 JP 2017511350 A5 JP2017511350 A5 JP 2017511350A5 JP 2016562508 A JP2016562508 A JP 2016562508A JP 2016562508 A JP2016562508 A JP 2016562508A JP 2017511350 A5 JP2017511350 A5 JP 2017511350A5
- Authority
- JP
- Japan
- Prior art keywords
- sitagliptin
- dosage form
- tannate complex
- oral dosage
- pharmaceutical composition
- 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.)
- Granted
Links
- MFFMDFFZMYYVKS-SECBINFHSA-N Sitagliptin Chemical compound C([C@H](CC(=O)N1CC=2N(C(=NN=2)C(F)(F)F)CC1)N)C1=CC(F)=C(F)C=C1F MFFMDFFZMYYVKS-SECBINFHSA-N 0.000 claims 11
- 229960004034 sitagliptin Drugs 0.000 claims 11
- 229920002253 Tannate Polymers 0.000 claims 8
- 239000006186 oral dosage form Substances 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 239000003826 tablet Substances 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 2
- 229920000591 gum Polymers 0.000 claims 2
- 239000012450 pharmaceutical intermediate Substances 0.000 claims 2
- 239000006188 syrup Substances 0.000 claims 2
- 235000020357 syrup Nutrition 0.000 claims 2
- 229940068682 Chewable Tablet Drugs 0.000 claims 1
- 101700062901 DPP Proteins 0.000 claims 1
- 102100012353 DPP4 Human genes 0.000 claims 1
- 101700039720 DPP4 Proteins 0.000 claims 1
- 239000001263 FEMA 3042 Substances 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 210000002784 Stomach Anatomy 0.000 claims 1
- 229940033123 Tannic Acid Drugs 0.000 claims 1
- LRBQNJMCXXYXIU-NRMVVENXSA-N Tannic acid Chemical compound OC1=C(O)C(O)=CC(C(=O)OC=2C(=C(O)C=C(C=2)C(=O)OC[C@@H]2[C@H]([C@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)[C@@H](OC(=O)C=3C=C(OC(=O)C=4C=C(O)C(O)=C(O)C=4)C(O)=C(O)C=3)O2)OC(=O)C=2C=C(OC(=O)C=3C=C(O)C(O)=C(O)C=3)C(O)=C(O)C=2)O)=C1 LRBQNJMCXXYXIU-NRMVVENXSA-N 0.000 claims 1
- 208000001072 Type 2 Diabetes Mellitus Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 230000036772 blood pressure Effects 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 239000007910 chewable tablet Substances 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 239000000796 flavoring agent Substances 0.000 claims 1
- 235000019634 flavors Nutrition 0.000 claims 1
- 239000008123 high-intensity sweetener Substances 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 235000013615 non-nutritive sweetener Nutrition 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000008188 pellet Substances 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 229920005862 polyol Polymers 0.000 claims 1
- 150000003077 polyols Chemical class 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 235000015523 tannic acid Nutrition 0.000 claims 1
- 229920002258 tannic acid Polymers 0.000 claims 1
Claims (15)
- タンニン酸シタグリプチン複合体。
- シタグリプチン含量が約25重量%から約75重量%である、請求項1に記載のタンニン酸シタグリプチン複合体。
- シタグリプチン含量が約29重量%から33重量%である、請求項2に記載のタンニン酸シタグリプチン複合体。
- タンニン酸に対するシタグリプチンの重量比が約3:1から約1:4である、請求項1に記載のタンニン酸シタグリプチン複合体。
- 重量比が約1:2である、請求項4に記載のタンニン酸シタグリプチン複合体。
- 治療的有効量の請求項1に記載のタンニン酸シタグリプチン複合体と不活性担体とを含む、医薬組成物。
- 治療的有効量の付加的な薬学的活性成分をさらに含む、請求項6に記載の医薬組成物。
- 治療的有効量の請求項1に記載のタンニン酸シタグリプチン複合体、薬学的に許容されるポリマーを含み、1または複数のポリオール、高強度甘味料、香味料を含んでもよい、医薬中間体。
- 請求項8に記載の医薬中間体を含む、経口剤形。
- 錠剤、カプセル、ペレットまたは散剤の形態である、請求項9に記載の経口剤形。
- ソフトチュー(soft chew)、薬用ガム、チュアブル錠、崩壊錠、シロップ、サッシェ(sachet)、経口フィルム、ゲルまたはリオスフェア(lyosphere)の形態である、請求項9に記載の経口剤形。
- 口内ではごくわずかな放出をし、且つ、胃内では即時放出をする、請求項9に記載の経口剤形。
- ソフトチュー、薬用ガム、経口フィルム、崩壊錠またはシロップである、請求項12に記載の経口剤形。
- 請求項1に記載のタンニン酸シタグリプチン複合体を含む、DPP−IVの阻害剤が適応される1または複数の疾患を処置、管理または予防するための医薬組成物。
- 前記疾患が、2型糖尿病、肥満または血圧である、請求項14に記載の医薬組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201461980641P | 2014-04-17 | 2014-04-17 | |
US61/980,641 | 2014-04-17 | ||
PCT/US2015/025504 WO2015160678A1 (en) | 2014-04-17 | 2015-04-13 | Sitagliptin tannate complex |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2017511350A JP2017511350A (ja) | 2017-04-20 |
JP2017511350A5 true JP2017511350A5 (ja) | 2017-11-24 |
JP6523328B2 JP6523328B2 (ja) | 2019-05-29 |
Family
ID=54324454
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2016562508A Active JP6523328B2 (ja) | 2014-04-17 | 2015-04-13 | タンニン酸シタグリプチン複合体 |
Country Status (12)
Country | Link |
---|---|
US (1) | US9833463B2 (ja) |
EP (1) | EP3131631B1 (ja) |
JP (1) | JP6523328B2 (ja) |
KR (1) | KR102351813B1 (ja) |
CN (1) | CN106456998B (ja) |
AU (1) | AU2015247921B2 (ja) |
BR (1) | BR112016023839A8 (ja) |
CA (1) | CA2945681A1 (ja) |
ES (1) | ES2932383T3 (ja) |
MX (1) | MX2016013588A (ja) |
RU (1) | RU2696588C2 (ja) |
WO (1) | WO2015160678A1 (ja) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TW201818969A (zh) * | 2016-10-19 | 2018-06-01 | 日商帝化製藥股份有限公司 | 在生體內之藥物溶出控制用組成物 |
US11096890B2 (en) | 2017-09-29 | 2021-08-24 | Merck Sharp & Dohme Corp. | Chewable dosage forms containing sitagliptin and metformin |
JP6839377B1 (ja) | 2020-03-30 | 2021-03-10 | 三菱電機株式会社 | エレベーター |
Family Cites Families (27)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO1997028149A1 (en) | 1996-02-02 | 1997-08-07 | Merck & Co., Inc. | Method for raising hdl cholesterol levels |
US5663415A (en) | 1996-06-28 | 1997-09-02 | Jame Fine Chemicals, Inc. | Process for preparing antihistamine tannates |
AR008789A1 (es) | 1996-07-31 | 2000-02-23 | Bayer Corp | Piridinas y bifenilos substituidos |
US6613942B1 (en) | 1997-07-01 | 2003-09-02 | Novo Nordisk A/S | Glucagon antagonists/inverse agonists |
AU749271B2 (en) | 1997-07-01 | 2002-06-20 | Agouron Pharmaceuticals, Inc. | Glucagon antagonists/inverse agonists |
JP2002534512A (ja) | 1999-01-15 | 2002-10-15 | ノボ ノルディスク アクティーゼルスカブ | 非ペプチドglp−1アゴニスト |
HUP0201033A3 (en) | 1999-05-17 | 2003-03-28 | Novo Nordisk As | Glucagon antagonists/inverse agonists, process for their preparation and their use |
PE20010612A1 (es) | 1999-09-28 | 2001-07-12 | Bayer Corp | Agonistas del receptor 3 (r3) del peptido activador de la adenilato ciclasa de la pituitaria y su uso farmacologico |
OA12622A (en) | 2001-06-11 | 2006-06-12 | Shire Biochem Inc | Thiophene derivatives as antiviral agents for flavivirus infection. |
UA74912C2 (en) | 2001-07-06 | 2006-02-15 | Merck & Co Inc | Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes |
US20030083354A1 (en) | 2001-10-26 | 2003-05-01 | Pediamed Pharmaceuticals, Inc. | Phenylephrine tannate and pyrilamine tannate salts in pharmaceutical compositions |
US20030114535A1 (en) | 2001-12-14 | 2003-06-19 | Jame Fine Chemicals, Inc. | Dextrochlorpheniramine tannate |
US6670370B1 (en) | 2001-12-14 | 2003-12-30 | Jame Fine Chemicals, Inc. | Dextromethorphan tannate |
JO2625B1 (en) * | 2003-06-24 | 2011-11-01 | ميرك شارب اند دوم كوربوريشن | Phosphoric acid salts of dipeptidyl betidase inhibitor 4 |
CN100457108C (zh) | 2003-09-02 | 2009-02-04 | 默克公司 | 一种二肽基肽酶iv抑制剂的磷酸盐新晶体 |
EP1667524A4 (en) | 2003-09-23 | 2009-01-14 | Merck & Co Inc | NOVEL CRYSTALLINE FORM OF A PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTASE-IV INHIBITOR |
EP1708571A4 (en) | 2004-01-16 | 2009-07-08 | Merck & Co Inc | NEW CRYSTALLINE SALTS OF A DIPEPTIDYLPEPTIDASE IV HEMMER |
US20050202050A1 (en) * | 2004-03-12 | 2005-09-15 | Kiel Jeffrey S. | Single tank process for preparing tannate liquid and semi-solid dosage forms |
EP1796671A4 (en) | 2004-09-15 | 2009-01-21 | Merck & Co Inc | AMORPHOUS FORM OF A PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR |
US20060270722A1 (en) * | 2005-05-31 | 2006-11-30 | Thornberry Nancy A | Combination of a dipeptidyl peptidase-IV inhibitor and a dual PPAR agonist for the treatment of diabetes and obesity |
WO2007035198A2 (en) * | 2005-07-25 | 2007-03-29 | Merck & Co., Inc. | Dodecylsulfate salt of a dipeptidyl peptidase-iv inhibitor |
US20090156579A1 (en) * | 2005-10-25 | 2009-06-18 | Hasegawa Philip A | Combination of a Dipeptidyl Peptidase-4 Inhibitor and an Anti-Hypertensive Agent for the Treatment of Diabetes and Hypertension |
NZ577623A (en) * | 2006-12-14 | 2011-05-27 | Teva Pharma | Tannate salt of rasagiline |
CN102026666B (zh) | 2007-12-11 | 2013-10-16 | 常山凯捷健生物药物研发(河北)有限公司 | 促胰岛素肽缀合物制剂 |
US8003672B2 (en) * | 2008-04-21 | 2011-08-23 | Merck Sharp & Dohme Corp. | CB-1 receptor modulator formulations |
EP2218721A1 (en) | 2009-02-11 | 2010-08-18 | LEK Pharmaceuticals d.d. | Novel salts of sitagliptin |
US9211263B2 (en) * | 2012-01-06 | 2015-12-15 | Elcelyx Therapeutics, Inc. | Compositions and methods of treating metabolic disorders |
-
2015
- 2015-04-13 CA CA2945681A patent/CA2945681A1/en not_active Abandoned
- 2015-04-13 MX MX2016013588A patent/MX2016013588A/es active IP Right Grant
- 2015-04-13 CN CN201580020211.4A patent/CN106456998B/zh active Active
- 2015-04-13 AU AU2015247921A patent/AU2015247921B2/en active Active
- 2015-04-13 EP EP15780045.9A patent/EP3131631B1/en active Active
- 2015-04-13 RU RU2016144695A patent/RU2696588C2/ru active
- 2015-04-13 US US15/302,211 patent/US9833463B2/en active Active
- 2015-04-13 WO PCT/US2015/025504 patent/WO2015160678A1/en active Application Filing
- 2015-04-13 KR KR1020167028345A patent/KR102351813B1/ko active IP Right Grant
- 2015-04-13 ES ES15780045T patent/ES2932383T3/es active Active
- 2015-04-13 BR BR112016023839A patent/BR112016023839A8/pt not_active Application Discontinuation
- 2015-04-13 JP JP2016562508A patent/JP6523328B2/ja active Active
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