EA037498B1 - Фармацевтическая композиция, содержащая 8-[(3r)-3-амино-1-пиперидинил]-7-(2-бутин-1-ил)-3,7-дигидро-3-метил-1-[4-метил-2-хиназолинилметил]-1h-пурин-2,6-дион или его фармацевтически приемлемую соль - Google Patents
Фармацевтическая композиция, содержащая 8-[(3r)-3-амино-1-пиперидинил]-7-(2-бутин-1-ил)-3,7-дигидро-3-метил-1-[4-метил-2-хиназолинилметил]-1h-пурин-2,6-дион или его фармацевтически приемлемую соль Download PDFInfo
- Publication number
- EA037498B1 EA037498B1 EA201890744A EA201890744A EA037498B1 EA 037498 B1 EA037498 B1 EA 037498B1 EA 201890744 A EA201890744 A EA 201890744A EA 201890744 A EA201890744 A EA 201890744A EA 037498 B1 EA037498 B1 EA 037498B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- pharmaceutical composition
- linagliptin
- tablet
- hydrogen phosphate
- calcium hydrogen
- Prior art date
Links
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- 150000003839 salts Chemical class 0.000 title claims abstract description 45
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 title 1
- 229960002397 linagliptin Drugs 0.000 claims abstract description 127
- LTXREWYXXSTFRX-QGZVFWFLSA-N Linagliptin Chemical compound N=1C=2N(C)C(=O)N(CC=3N=C4C=CC=CC4=C(C)N=3)C(=O)C=2N(CC#CC)C=1N1CCC[C@@H](N)C1 LTXREWYXXSTFRX-QGZVFWFLSA-N 0.000 claims abstract description 121
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- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 71
- 239000000203 mixture Substances 0.000 claims description 41
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims description 40
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Classifications
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- A61K9/20—Pills, tablets, discs, rods
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- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
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- 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)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Diabetes (AREA)
- Inorganic Chemistry (AREA)
- Hematology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15189208 | 2015-10-09 | ||
| PCT/EP2016/073952 WO2017060398A1 (en) | 2015-10-09 | 2016-10-07 | Pharmaceutical composition containing 8-[(3r)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[4-methyl-2-quinazolinyl)methyl]-1h-purine-2,6-dione or a pharmaceutically acceptable salt thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201890744A1 EA201890744A1 (ru) | 2018-09-28 |
| EA037498B1 true EA037498B1 (ru) | 2021-04-05 |
Family
ID=54293102
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201890744A EA037498B1 (ru) | 2015-10-09 | 2016-10-07 | Фармацевтическая композиция, содержащая 8-[(3r)-3-амино-1-пиперидинил]-7-(2-бутин-1-ил)-3,7-дигидро-3-метил-1-[4-метил-2-хиназолинилметил]-1h-пурин-2,6-дион или его фармацевтически приемлемую соль |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10668073B2 (OSRAM) |
| EP (1) | EP3359136A1 (OSRAM) |
| JP (1) | JP6839708B2 (OSRAM) |
| CN (1) | CN108174596A (OSRAM) |
| AU (1) | AU2016335082A1 (OSRAM) |
| CA (1) | CA2998982A1 (OSRAM) |
| EA (1) | EA037498B1 (OSRAM) |
| WO (1) | WO2017060398A1 (OSRAM) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020009675A2 (en) | 2018-06-01 | 2020-01-09 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | Solid oral pharmaceutical compositions of linagliptin |
| CN110496129B (zh) * | 2018-11-23 | 2021-06-04 | 北京中医药大学 | 利拉利汀的抗肿瘤活性及其新用途 |
| JP7245694B2 (ja) * | 2019-03-26 | 2023-03-24 | エルメッド株式会社 | リナグリプチン含有医薬組成物及びその製造方法、並びにリナグリプチン含有医薬組成物の品質の向上方法 |
| WO2022102457A1 (ja) * | 2020-11-10 | 2022-05-19 | 沢井製薬株式会社 | リナグリプチン含有口腔内崩壊錠 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014026939A1 (en) * | 2012-08-13 | 2014-02-20 | Sandoz Ag | Stable pharmaceutical composition containing 8-[(3r)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1h-purine-2,6-dione or a pharmaceutically acceptable salt thereof |
| WO2014193528A1 (en) * | 2013-04-29 | 2014-12-04 | Anovel Pharmaceuticals, Llc | Amorphous dosage forms and methods |
| EP2848242A1 (en) * | 2013-09-12 | 2015-03-18 | Sanovel Ilac Sanayi ve Ticaret A.S. | Orally disintegrating formulations of Linagliptin |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101150449B1 (ko) | 2002-08-21 | 2012-06-01 | 베링거 잉겔하임 파르마 게엠베하 운트 코 카게 | 8-［3-아미노-피페리딘-1-일］-크산틴, 이의 제조방법 및 이를 포함하는 약제학적 조성물 |
| EP1852108A1 (en) | 2006-05-04 | 2007-11-07 | Boehringer Ingelheim Pharma GmbH & Co.KG | DPP IV inhibitor formulations |
| EA030606B1 (ru) | 2006-05-04 | 2018-08-31 | Бёрингер Ингельхайм Интернациональ Гмбх | Способы приготовления лекарственного средства, содержащего полиморфы |
| CN102256976A (zh) | 2008-12-23 | 2011-11-23 | 贝林格尔.英格海姆国际有限公司 | 有机化合物的盐形式 |
| US20120258170A1 (en) * | 2009-05-20 | 2012-10-11 | Nutracryst Therapeutics Private Limited | Pharmaceutical co-crystals of quercetin |
| WO2012152837A1 (en) | 2011-05-10 | 2012-11-15 | Sandoz Ag | Polymorph of linagliptin benzoate |
| CN103006663A (zh) * | 2011-09-23 | 2013-04-03 | 重庆药友制药有限责任公司 | 一种瑞舒伐他汀钙的药物组合物 |
| CN102631331A (zh) * | 2012-04-26 | 2012-08-15 | 北京哈三联科技股份有限公司 | 奥氮平口腔崩解片制剂及其制备方法 |
| WO2014184378A1 (en) * | 2013-05-16 | 2014-11-20 | Sandoz Ag | Tablet with increased drug load of odanacatib |
-
2016
- 2016-10-07 EA EA201890744A patent/EA037498B1/ru unknown
- 2016-10-07 CN CN201680058418.5A patent/CN108174596A/zh active Pending
- 2016-10-07 CA CA2998982A patent/CA2998982A1/en not_active Abandoned
- 2016-10-07 US US15/767,131 patent/US10668073B2/en not_active Expired - Fee Related
- 2016-10-07 AU AU2016335082A patent/AU2016335082A1/en not_active Abandoned
- 2016-10-07 EP EP16778023.8A patent/EP3359136A1/en not_active Withdrawn
- 2016-10-07 JP JP2018517867A patent/JP6839708B2/ja not_active Expired - Fee Related
- 2016-10-07 WO PCT/EP2016/073952 patent/WO2017060398A1/en not_active Ceased
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014026939A1 (en) * | 2012-08-13 | 2014-02-20 | Sandoz Ag | Stable pharmaceutical composition containing 8-[(3r)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1h-purine-2,6-dione or a pharmaceutically acceptable salt thereof |
| WO2014193528A1 (en) * | 2013-04-29 | 2014-12-04 | Anovel Pharmaceuticals, Llc | Amorphous dosage forms and methods |
| EP2848242A1 (en) * | 2013-09-12 | 2015-03-18 | Sanovel Ilac Sanayi ve Ticaret A.S. | Orally disintegrating formulations of Linagliptin |
Also Published As
| Publication number | Publication date |
|---|---|
| US20180243310A1 (en) | 2018-08-30 |
| JP2018530566A (ja) | 2018-10-18 |
| JP6839708B2 (ja) | 2021-03-10 |
| EP3359136A1 (en) | 2018-08-15 |
| AU2016335082A1 (en) | 2018-04-12 |
| US10668073B2 (en) | 2020-06-02 |
| CN108174596A (zh) | 2018-06-15 |
| EA201890744A1 (ru) | 2018-09-28 |
| WO2017060398A1 (en) | 2017-04-13 |
| CA2998982A1 (en) | 2017-04-13 |
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