Stable amorphous form of Resmetirom, characterized by data selected from amorphous form of Resmetirom is stable when exposed to specified relative humidity or relative humidity, X ray powder diffraction spectrum, or having specified purity by area percentage of high-performance liquid chromatography
	CHATURVEDI V K; KUMAR N; BHAVSAR J; KUMAR A
	2023-08-31
专利权人	MANKIND PHARMA LTD (MANK-Non-standard)
申请日期	2023-08-31
专利号	IN202311058349-A
成果简介	NOVELTY - Stable amorphous form of Resmetirom, characterized by data selected from (a) the amorphous form of Resmetirom is stable when exposed to a relative humidity of 75% at 40 °C or a relative humidity of 60% at 25 °C for a period of 12 months; (b) an X ray powder diffraction spectrum (XRPD); or (c) having a purity of about 99% or more by area percentage of high-performance liquid chromatography (HPLC). USE - Stable amorphous form of Resmetirom. ADVANTAGE - The method provides a simple process which comprises mixing a water insoluble Resmetirom and a water-soluble polymer together under no more than the usual agitation force with heating within the temperature region not melting them, making the water insoluble Resmetirom as amorphous in nature to yield a solid dispersion insuring very high solubility and bioavailability. The mixed-grinding technology, in which the water insoluble Resmetirom and the water-soluble polymer are mix-ground or roll-mixed without heating. It is considered that various factors arising from mechanical manipulation, such as lattice defect or lattice modulation, increases in specific surface area and surface energy and so on, enhances the activity of the solid phase to encourage transition of the Resmetirom to an amorphous state and, hence, dispersion of the Resmetirom in this amorphous state into the carrier. DETAILED DESCRIPTION - INDEPENDENT CLAIMS are included for: (1) a process for the preparation of stable amorphous compound, which involves (a) preparing a solution by dissolving the Resmetirom in solvents to obtain a solution; and (b) isolating the stable amorphous form of Resmetirom; and (2) a stable amorphous solid dispersion comprises Resmetirom, and pharmaceutically acceptable carriers selected from hydroxypropylmethyl cellulose, low-substituted hydroxypropylcellulose, hydroxyethyl cellulose, cellulose acetate phthalate, carboxy methyl ethyl cellulose, Eudragit(RTM: copolymer of poly(ethylacrylate, methyl-methacrylate, and chloro trimethyl-ammonioethyl methacrylate) (Grade: L100), povidone, polyvinylpyrrolidone (PVP), lactose, and/or sorbitol.
IPC 分类号	A61K-031/53 ; A61K-038/17 ; A61K-047/32 ; A61K-009/10 ; A61K-009/20
国家	印度
专业领域	医药卫生
语种	英语
成果类型	专利
文献类型	科技成果
条目标识符	http://119.78.100.226:8889/handle/3KE4DYBR/20598
专题	中国科学院新疆生态与地理研究所
作者单位	MANKIND PHARMA LTD (MANK-Non-standard)
推荐引用方式 GB/T 7714	CHATURVEDI V K,KUMAR N,BHAVSAR J,et al. Stable amorphous form of Resmetirom, characterized by data selected from amorphous form of Resmetirom is stable when exposed to specified relative humidity or relative humidity, X ray powder diffraction spectrum, or having specified purity by area percentage of high-performance liquid chromatography. IN202311058349-A[P]. 2023.

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