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Title:
SELF-MICROEMULSION COMPOSITION AND PREPARATION AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/088284
Kind Code:
A1
Abstract:
Disclosed is a self-microemulsion composition comprising, in percentage by mass, 0.5%-20% of a kinase inhibitor fat-soluble salt, 5%-70% of an oil phase, 5%-80% of an emulsifier and 0-50% of a co-emulsifier. The kinase inhibitor (such as cabozantinib) is prepared into a salt with significantly improved solubility, then the salt is used as an active component, and auxiliary materials such as an oil phase, an emulsifier and a co-emulsifier in a specific type and dosage ratio are selected, so that the prepared self-microemulsion composition of the kinase inhibitor (such as cabozantinib) has improved bioavailability and dissolution.

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Inventors:
YI MULIN (CN)
Application Number:
PCT/CN2022/132168
Publication Date:
May 25, 2023
Filing Date:
November 16, 2022
Export Citation:
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Assignee:
HUNAN HUIZE BIOPHARMA S&T CO LTD (CN)
International Classes:
A61K31/47; A61K9/107; A61K47/10; A61K47/14; A61K47/26; A61P35/00
Foreign References:
CN112516315A2021-03-19
CN112618488A2021-04-09
AU2020102909A42020-12-17
Other References:
WILLIAMS HYWEL D., FORD LEIGH, HAN SIFEI, TANGSO KRISTIAN J., LIM SHEA, SHACKLEFORD DAVID M., VODAK DAVID T., BENAMEUR HASSAN, POU: "Enhancing the Oral Absorption of Kinase Inhibitors Using Lipophilic Salts and Lipid-Based Formulations", MOLECULAR PHARMACEUTICS, AMERICAN CHEMICAL SOCIETY, US, vol. 15, no. 12, 3 December 2018 (2018-12-03), US , pages 5678 - 5696, XP093067581, ISSN: 1543-8384, DOI: 10.1021/acs.molpharmaceut.8b00858
MA, QIAOFANG; ZENG, JIA; SHA, KANG; WU, ZHENGHONG: "Research Progress of Oral Self-Microemulsifying Drug Delivery System", PROGRESS IN PHARMACEUTICAL SCIENCES, vol. 44, no. 6, 25 June 2020 (2020-06-25), CN , pages 466 - 475, XP009546400, ISSN: 1001-5094
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