WO2022102457A1 - Comprimé à désintégration orale contenant de la linagliptine - Google Patents
Comprimé à désintégration orale contenant de la linagliptine Download PDFInfo
- Publication number
- WO2022102457A1 WO2022102457A1 PCT/JP2021/040258 JP2021040258W WO2022102457A1 WO 2022102457 A1 WO2022102457 A1 WO 2022102457A1 JP 2021040258 W JP2021040258 W JP 2021040258W WO 2022102457 A1 WO2022102457 A1 WO 2022102457A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- linagliptin
- orally disintegrating
- disintegrating tablet
- carmellose
- tablet
- Prior art date
Links
- 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 title claims abstract description 105
- 229960002397 linagliptin Drugs 0.000 title claims abstract description 105
- 239000006191 orally-disintegrating tablet Substances 0.000 title claims abstract description 65
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims abstract description 46
- 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 abstract description 46
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims abstract description 46
- 229950008138 carmellose Drugs 0.000 claims abstract description 46
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims abstract description 25
- 239000011575 calcium Substances 0.000 claims abstract description 25
- 229910052791 calcium Inorganic materials 0.000 claims abstract description 25
- 239000000654 additive Substances 0.000 claims abstract description 20
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- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims description 30
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 27
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Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
- C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Inorganic Chemistry (AREA)
- Endocrinology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
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- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Emergency Medicine (AREA)
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Abstract
La présente invention concerne : un comprimé à désintégration orale contenant de la linagliptine qui est capable de masquer suffisamment l'amertume ; et un procédé de production de celui-ci. Selon un mode de réalisation, la présente invention concerne un comprimé à désintégration orale contenant de la linagliptine contenant : de la linagliptine; et un additif comprenant au moins un élément choisi dans le groupe constitué par la carmellose calcique, la croscarmellose sodique, la carmellose et l'acide glycolique d'amidon sodique. L'additif peut également comprendre au moins un élément choisi dans le groupe constitué par la carmellose calcique, le sodium réticulé et la carmellose.
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PCT/JP2021/040258 WO2022102457A1 (fr) | 2020-11-10 | 2021-11-01 | Comprimé à désintégration orale contenant de la linagliptine |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2022192036A (ja) * | 2021-06-16 | 2022-12-28 | 日本ジェネリック株式会社 | リナグリプチン含有製剤及びリナグリプチン含有口腔内崩壊性錠剤 |
Citations (5)
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WO2013161823A1 (fr) * | 2012-04-24 | 2013-10-31 | 第一三共株式会社 | Comprimé à désintégration orale et son procédé de production |
EP2848242A1 (fr) * | 2013-09-12 | 2015-03-18 | Sanovel Ilac Sanayi ve Ticaret A.S. | Formulations orodispersibles de Linagliptin |
CN105853382A (zh) * | 2016-05-19 | 2016-08-17 | 广州迈达康医药科技有限公司 | 一种利格列汀口崩片及其制备方法 |
JP2018530566A (ja) * | 2015-10-09 | 2018-10-18 | ヘクサル・アクチェンゲゼルシャフトHexal AG | 8−[(3r)−3−アミノ−1−ピペリジニル]−7−(2−ブチン−1−イル)−3,7−ジヒドロ−3−メチル−1−[4−メチル−2−キナゾリニル)メチル]−1h−プリン−2,6−ジオンまたは薬学上許容できるその塩を含有する医薬組成物 |
JP2020158435A (ja) * | 2019-03-26 | 2020-10-01 | 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 |
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2021
- 2021-11-01 JP JP2022561834A patent/JPWO2022102457A1/ja active Pending
- 2021-11-01 WO PCT/JP2021/040258 patent/WO2022102457A1/fr active Application Filing
Patent Citations (5)
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WO2013161823A1 (fr) * | 2012-04-24 | 2013-10-31 | 第一三共株式会社 | Comprimé à désintégration orale et son procédé de production |
EP2848242A1 (fr) * | 2013-09-12 | 2015-03-18 | Sanovel Ilac Sanayi ve Ticaret A.S. | Formulations orodispersibles de Linagliptin |
JP2018530566A (ja) * | 2015-10-09 | 2018-10-18 | ヘクサル・アクチェンゲゼルシャフトHexal AG | 8−[(3r)−3−アミノ−1−ピペリジニル]−7−(2−ブチン−1−イル)−3,7−ジヒドロ−3−メチル−1−[4−メチル−2−キナゾリニル)メチル]−1h−プリン−2,6−ジオンまたは薬学上許容できるその塩を含有する医薬組成物 |
CN105853382A (zh) * | 2016-05-19 | 2016-08-17 | 广州迈达康医药科技有限公司 | 一种利格列汀口崩片及其制备方法 |
JP2020158435A (ja) * | 2019-03-26 | 2020-10-01 | 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 |
Non-Patent Citations (1)
Title |
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NAKAGAWA, TOMOYA ET AL.: "Drug Development Research with Taste Sensor, Part 2: Taste Masking and Formulation Development of Donepezil Hydrochloride OD Tablets", PHARM TECH JAPAN, vol. 28, no. 3, 1 January 2012 (2012-01-01), JP , pages 511 - 517, XP009536655, ISSN: 0910-4739 * |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2022192036A (ja) * | 2021-06-16 | 2022-12-28 | 日本ジェネリック株式会社 | リナグリプチン含有製剤及びリナグリプチン含有口腔内崩壊性錠剤 |
JP7210794B2 (ja) | 2021-06-16 | 2023-01-23 | 日本ジェネリック株式会社 | リナグリプチン含有製剤及びリナグリプチン含有口腔内崩壊性錠剤 |
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