Title:
COCRYSTAL OF ORLISTAT AND AMINO ACID, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
Document Type and Number:
WIPO Patent Application WO/2021/097650
Kind Code:
A1
Abstract:
The invention belongs to the technical field of medicines, and particularly relates to a cocrystal of orlistat and an amino acid, and a pharmaceutical composition comprising the same. The cocrystal formed by orlistat and L-proline, L-leucine or L-valine in an appropriate molar ratio has a high melting point of 95.3°C, 130.3°C and 103.5°C, respectively, which are all significantly higher than that of type II orlistat in the commercial orlistat capsules, so that the drying process in preparation of the active pharmaceutical ingredient and the preparation can be carried out at a higher temperature, which shortens the drying time, improves drying efficiency, and reduces drying energy consumption. In addition, when the resulting cocrystal is used as the raw material to prepare capsules, the obtained capsules has a higher dissolution rate of olitrolimus than that of Type II orlistat in the commercial orlistat capsules, and its action is faster than the latter.
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Inventors:
XIANG FEI (CN)
DU ZHIBO (CN)
PENG WEI (CN)
DU ZHIBO (CN)
PENG WEI (CN)
Application Number:
PCT/CN2019/119381
Publication Date:
May 27, 2021
Filing Date:
November 19, 2019
Export Citation:
Assignee:
ZHONGSHAN WANHAN PHARMACEUTICAL CO LTD (CN)
International Classes:
C07D305/12; A61K31/365; A61K31/401; A61P3/04; C07C227/42; C07C229/08; C07D207/16
Foreign References:
| CN106349192A | 2017-01-25 |
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