JP2009537478A - レパグリニドとメトホルミンを含む錠剤配合物 - Google Patents
レパグリニドとメトホルミンを含む錠剤配合物 Download PDFInfo
- Publication number
- JP2009537478A JP2009537478A JP2009510416A JP2009510416A JP2009537478A JP 2009537478 A JP2009537478 A JP 2009537478A JP 2009510416 A JP2009510416 A JP 2009510416A JP 2009510416 A JP2009510416 A JP 2009510416A JP 2009537478 A JP2009537478 A JP 2009537478A
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- Prior art keywords
- weight
- tablet
- repaglinide
- metformin
- binder
- 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.)
- Ceased
Links
- XZWYZXLIPXDOLR-UHFFFAOYSA-N metformin Chemical compound CN(C)C(=N)NC(N)=N XZWYZXLIPXDOLR-UHFFFAOYSA-N 0.000 title claims abstract description 113
- FAEKWTJYAYMJKF-QHCPKHFHSA-N GlucoNorm Chemical compound C1=C(C(O)=O)C(OCC)=CC(CC(=O)N[C@@H](CC(C)C)C=2C(=CC=CC=2)N2CCCCC2)=C1 FAEKWTJYAYMJKF-QHCPKHFHSA-N 0.000 title claims abstract description 85
- 229960002354 repaglinide Drugs 0.000 title claims abstract description 85
- 229960003105 metformin Drugs 0.000 title claims abstract description 79
- 239000007916 tablet composition Substances 0.000 title claims description 14
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- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 16
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- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 13
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical group O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 12
- 239000002706 dry binder Substances 0.000 claims description 12
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- VJHCJDRQFCCTHL-UHFFFAOYSA-N acetic acid 2,3,4,5,6-pentahydroxyhexanal Chemical compound CC(O)=O.OCC(O)C(O)C(O)C(O)C=O VJHCJDRQFCCTHL-UHFFFAOYSA-N 0.000 claims description 11
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- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims description 7
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- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 6
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- OETHQSJEHLVLGH-UHFFFAOYSA-N metformin hydrochloride Chemical compound Cl.CN(C)C(=N)N=C(N)N OETHQSJEHLVLGH-UHFFFAOYSA-N 0.000 claims description 6
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- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims description 4
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 4
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 4
- 239000004386 Erythritol Substances 0.000 claims description 4
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 claims description 4
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims description 4
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 4
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- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims description 4
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- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims description 3
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- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 claims description 2
- 229910052782 aluminium Inorganic materials 0.000 claims description 2
- 238000001035 drying Methods 0.000 claims description 2
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- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 2
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- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 58
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- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 2
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- FJQXCDYVZAHXNS-UHFFFAOYSA-N methadone hydrochloride Chemical compound Cl.C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 FJQXCDYVZAHXNS-UHFFFAOYSA-N 0.000 description 1
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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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
-
- 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
- A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- 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
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
- A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
-
- 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
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06009902 | 2006-05-13 | ||
| EP06121953 | 2006-10-09 | ||
| PCT/EP2007/054510 WO2007131930A1 (en) | 2006-05-13 | 2007-05-10 | Tablet formulation comprising repaglinide and metformin |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009537478A true JP2009537478A (ja) | 2009-10-29 |
| JP2009537478A5 JP2009537478A5 (enExample) | 2010-07-01 |
Family
ID=38293358
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009510416A Ceased JP2009537478A (ja) | 2006-05-13 | 2007-05-10 | レパグリニドとメトホルミンを含む錠剤配合物 |
Country Status (4)
| Country | Link |
|---|---|
| US (2) | US20090252790A1 (enExample) |
| EP (1) | EP2026787B1 (enExample) |
| JP (1) | JP2009537478A (enExample) |
| WO (1) | WO2007131930A1 (enExample) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2013510875A (ja) * | 2009-11-13 | 2013-03-28 | ブリストル−マイヤーズ スクイブ カンパニー | 速放性錠剤製剤 |
| JP2016535791A (ja) * | 2013-11-12 | 2016-11-17 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Cftr媒介性疾患の処置のための医薬組成物を調製する方法 |
| JP2018199674A (ja) * | 2017-05-29 | 2018-12-20 | 第一三共株式会社 | 認知症治療薬を含有する口腔内崩壊性錠剤 |
| US12065432B2 (en) | 2007-12-07 | 2024-08-20 | Vertex Pharmaceuticals Incorporated | Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101516347A (zh) * | 2006-09-29 | 2009-08-26 | 诺沃-诺迪斯克有限公司 | 包含二甲双胍和瑞格列奈的药物制剂 |
| FI20080355A0 (fi) * | 2008-05-09 | 2008-05-09 | Atacama Labs Oy | Prosessi metforminia käsittävien tablettien valmistamiseksi |
| CN101756971B (zh) * | 2008-10-09 | 2013-09-18 | 北京德众万全药物技术开发有限公司 | 一种盐酸二甲双胍瑞格列奈的口服固体药物组合物 |
| RU2482846C2 (ru) * | 2011-04-12 | 2013-05-27 | Открытое акционерное общество "Химико-фармацевтический комбинат "АКРИХИН" (ОАО "АКРИХИН") | Фармацевтическая противодиабетическая композиция и способ получения противодиабетической композиции |
| CN102319245B (zh) * | 2011-07-08 | 2014-07-09 | 杭州华东医药集团新药研究院有限公司 | 一种含有瑞格列奈和盐酸二甲双胍的组合物及其制备 |
| CN102283813B (zh) * | 2011-07-28 | 2017-05-24 | 万全万特制药江苏有限公司 | 一种含有瑞格列奈的药物组合物及其制备方法 |
| WO2013074049A1 (en) * | 2011-11-03 | 2013-05-23 | Mahmut Bilgic | Micronized metformin |
| WO2013077825A1 (en) * | 2011-11-23 | 2013-05-30 | Mahmut Bilgic | Preparation process for a formulation comprising metformin |
| CN103494816B (zh) * | 2013-09-29 | 2019-06-14 | 威海迪素制药有限公司 | 一种治疗糖尿病的药物组合物 |
| KR101545268B1 (ko) * | 2015-02-05 | 2015-08-20 | 보령제약 주식회사 | 정제 및 이의 제조방법 |
| CN105535980B (zh) * | 2015-12-24 | 2019-02-26 | 江苏豪森药业集团有限公司 | 稳定的瑞格列奈药物组合物及其制备方法 |
| TW201938147A (zh) * | 2017-12-18 | 2019-10-01 | 德商拜耳廠股份有限公司 | 阿卡波糖與甲福明之固定劑量組合錠劑配製物及其製法 |
| KR20220024559A (ko) * | 2019-06-17 | 2022-03-03 | 디에스엠 아이피 어셋츠 비.브이. | 분무 건조된 비타민 b12를 포함하는 고체 약학적 투여 형태 |
| JP7711052B2 (ja) | 2019-10-16 | 2025-07-22 | バイエル・アクチエンゲゼルシヤフト | アカルボースの改善された形成方法 |
| LT6874B (lt) | 2020-04-17 | 2021-12-10 | Lietuvos sveikatos mokslų universitetas | Valpro rūgšties ir dichloroacetato druskų derinio taikymas vėžio gydymui |
| GB2599950A (en) * | 2020-10-16 | 2022-04-20 | Zentiva Ks | Pharmaceutical compositions with low amounts of nitrosamine impurities and methods for producing the same |
| LT7129B (lt) | 2023-08-22 | 2025-03-25 | Lietuvos sveikatos mokslų universitetas | Natrio dichloroacetato ir valpro rūgšties druskų derinys, skirtas virusinėms ir bakterinėms infekcijoms, ir uždegiminėms ligoms gydyti |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030224046A1 (en) * | 2002-06-03 | 2003-12-04 | Vinay Rao | Unit-dose combination composition for the simultaneous delivery of a short-acting and a long-acting oral hypoglycemic agent |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3174901A (en) * | 1963-01-31 | 1965-03-23 | Jan Marcel Didier Aron Samuel | Process for the oral treatment of diabetes |
| FR2758459B1 (fr) * | 1997-01-17 | 1999-05-07 | Pharma Pass | Composition pharmaceutique de fenofibrate presentant une biodisponibilite elevee et son procede de preparation |
| AU7906898A (en) * | 1997-06-13 | 1998-12-30 | Novo Nordisk A/S | Novel niddm regimen |
| US6559188B1 (en) * | 1999-09-17 | 2003-05-06 | Novartis Ag | Method of treating metabolic disorders especially diabetes, or a disease or condition associated with diabetes |
| US6878749B2 (en) * | 1999-09-17 | 2005-04-12 | Novartis Ag | Method of treating metabolic disorders, especially diabetes, or a disease or condition associated with diabetes |
| US20010036479A1 (en) * | 2000-01-14 | 2001-11-01 | Gillian Cave | Glyburide composition |
| GB0003232D0 (en) * | 2000-02-11 | 2000-04-05 | Smithkline Beecham Plc | Novel composition |
| BRPI0206432A2 (pt) * | 2001-01-12 | 2016-10-25 | Sun Pharmaceutical Ind Ltd | métodos para administrar dois ou mais agentes terapêuticos ativos e para tratar diabetes melito ou sintomas associados com diabetes melito em um humano e sistema de liberação espaçada de medicamento |
| US20050054731A1 (en) * | 2003-09-08 | 2005-03-10 | Franco Folli | Multi-system therapy for diabetes, the metabolic syndrome and obesity |
| AU2006311601A1 (en) * | 2005-11-07 | 2007-05-18 | Elixir Pharmaceuticals, Inc. | Combinations of metformin and meglitinide |
-
2007
- 2007-05-10 JP JP2009510416A patent/JP2009537478A/ja not_active Ceased
- 2007-05-10 US US12/300,662 patent/US20090252790A1/en not_active Abandoned
- 2007-05-10 EP EP07728962.7A patent/EP2026787B1/en not_active Not-in-force
- 2007-05-10 WO PCT/EP2007/054510 patent/WO2007131930A1/en not_active Ceased
-
2011
- 2011-09-23 US US13/241,768 patent/US20120012499A1/en not_active Abandoned
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030224046A1 (en) * | 2002-06-03 | 2003-12-04 | Vinay Rao | Unit-dose combination composition for the simultaneous delivery of a short-acting and a long-acting oral hypoglycemic agent |
Non-Patent Citations (1)
| Title |
|---|
| JPN6012050090; 佐川良寿: 医薬品製剤技術 , 2002, pp.62-63, 株式会社シーエムシー出版 * |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12065432B2 (en) | 2007-12-07 | 2024-08-20 | Vertex Pharmaceuticals Incorporated | Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid |
| JP2013510875A (ja) * | 2009-11-13 | 2013-03-28 | ブリストル−マイヤーズ スクイブ カンパニー | 速放性錠剤製剤 |
| JP2015129142A (ja) * | 2009-11-13 | 2015-07-16 | アストラゼネカ・アクチエボラーグAstrazeneca Aktiebolag | 速放性錠剤製剤 |
| JP2016535791A (ja) * | 2013-11-12 | 2016-11-17 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Cftr媒介性疾患の処置のための医薬組成物を調製する方法 |
| JP2018199674A (ja) * | 2017-05-29 | 2018-12-20 | 第一三共株式会社 | 認知症治療薬を含有する口腔内崩壊性錠剤 |
| JP7023186B2 (ja) | 2017-05-29 | 2022-02-21 | 第一三共株式会社 | 認知症治療薬を含有する口腔内崩壊性錠剤 |
Also Published As
| Publication number | Publication date |
|---|---|
| US20090252790A1 (en) | 2009-10-08 |
| US20120012499A1 (en) | 2012-01-19 |
| EP2026787B1 (en) | 2013-12-25 |
| EP2026787A1 (en) | 2009-02-25 |
| WO2007131930A1 (en) | 2007-11-22 |
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