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1. WO2020004652 - FORMULATION CONTAINING EMRICASAN

Publication Number WO/2020/004652
Publication Date 02.01.2020
International Application No. PCT/JP2019/025945
International Filing Date 28.06.2019
IPC
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
38
Medicinal preparations containing peptides
04
Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
05
Dipeptides
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
08
Solutions
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9
Medicinal preparations characterised by special physical form
14
Particulate form, e.g. powders
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
02
Inorganic compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
08
containing oxygen
14
Esters of carboxylic acids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
26
Carbohydrates
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
30
Macromolecular compounds
34
Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
27
Drugs for disorders of the senses
02
Ophthalmic agents
A61K 38/05 (2006.01)
A61K 9/08 (2006.01)
A61K 9/14 (2006.01)
A61K 47/02 (2006.01)
A61K 47/14 (2017.01)
A61K 47/26 (2006.01)
CPC
A61K 38/05
A61K 47/02
A61K 47/14
A61K 47/26
A61K 47/34
A61K 9/08
Applicants
  • 学校法人同志社 THE DOSHISHA [JP/JP]; 京都府京都市上京区今出川通烏丸東入玄武町601番地 601, Gembu-cho, Karasuma-Higashi-iru, Imadegawa-dori, Kamigyo-ku, Kyoto-shi, Kyoto 6028580, JP
Inventors
  • 小泉 範子 KOIZUMI Noriko; JP
  • 奥村 直毅 OKUMURA Naoki; JP
Agents
  • 山本 秀策 YAMAMOTO Shusaku; JP
  • 森下 夏樹 MORISHITA Natsuki; JP
  • ▲駒▼谷 剛志 KOMATANI Takeshi; JP
  • 飯田 貴敏 IIDA Takatoshi; JP
  • 石川 大輔 ISHIKAWA Daisuke; JP
  • 山本 健策 YAMAMOTO Kensaku; JP
Priority Data
2018-12523429.06.2018JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) FORMULATION CONTAINING EMRICASAN
(FR) FORMULATION CONTENANT DE L'EMRICASAN
(JA) エムリカサンを含む製剤
Abstract
(EN)
The present disclosure provides a formulation having improved solubility and/or stability of emricasan. In one embodiment, the present disclosure provides a formulation containing (i) emricasan or a derivative thereof, or a pharmaceutically acceptable salt thereof, or a solvate thereof, (ii) a nonionic surfactant including a polyoxyethylene group, and (iii) a buffering agent that maintains the pH at about 4.5 to about 8.5. The present disclosure also provides a composition in the form of powder for preparing such a formulation at the time of use.
(FR)
La présente invention concerne une formulation ayant une solubilité et/ou une stabilité améliorées d'emricasan. Dans un mode de réalisation, la présente invention concerne une formulation contenant (i) de l'emricasan ou un dérivé de celui-ci, ou un sel pharmaceutiquement acceptable de celui-ci, ou un solvate de celui-ci, (ii) un tensioactif non ionique comprenant un groupe polyoxyéthylène, et (iii) un agent tampon qui maintient le pH à environ 4,5 à environ 8,5. La présente invention concerne également une composition sous forme de poudre pour préparer une telle formulation au moment de l'utilisation.
(JA)
本開示は、エムリカサンの可溶性および/または安定性が改善された製剤を提供する。一態様において、本開示は、(i)エムリカサンもしくはその誘導体、またはその薬学的に許容され得る塩、あるいはその溶媒和物と、(ii)ポリオキシエチレン基を含む非イオン性界面活性剤と、(iii)pHを約4.5~約8.5に維持する緩衝剤とを含む製剤を提供する。また、本開示は、このような製剤を用時調製するための粉末形態の組成物も提供する。
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