Cocrystal of progesterone and preparation method and use thereof
AssigneeNational Institutes for Food and Drug Control
InventorsLan He, Jing Xiong, Xiangxiang Wu, Xin Zhu, Zhonglin Lu, Yan Shi, Na Zhang, Yang Liu
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Abstract
The present invention relates to a cocrystal of progesterone, which is formed by the active ingredient progesterone and a cocrystal former which is selected from isophthalic acid, 4-formylbenzeneboronic acid and 3-nitrophthalic acid. The present invention also relates to the method for preparing the cocrystal of progesterone and use thereof for increasing the thickness of endometrium, improving progesterone's solubility or increasing progesterone's permeation rate.
Claims11
A cocrystal of progesterone, characterized in that the cocrystal of progesterone is formed by the active ingredient progesterone and a cocrystal former, which is selected from the group consisting of isophthalic acid, 4-formylbenzeneboronic acid, and 3-nitrophthalic acid;
- wherein when the cocrystal former is isophthalic acid, powder X-ray diffraction characteristic peaks of the resulting progesterone-isophthalic acid cocrystal, expressed as 2θ angles, appear at 6.56°, 10.96°, 13.14°, 16.17°, 19.76°, 20.32°, 21.04°, 22.20°, 24.17°, 26.45°, 28.05°, and 28.55°;
- wherein when the cocrystal former is 4-formylbenzeneboronic acid, powder X-ray diffraction characteristic peaks of the resulting progesterone-4-formylbenzeneboronic acid cocrystal, expressed as 2θ angles, appear at 9.04°, 10.55°, 12.64°, 13.44°, 15.53°, 16.48°, 16.99°, 18.22°, 19.11°, 19.66°, 20.70°, 21.18°, 22.12°, 23.48°, 24.68°, 26.63°, and 27.85°;
- wherein when the cocrystal former is 3-nitrophthalic acid, powder X-ray diffraction characteristic peaks of the resulting progesterone-3-nitrophthalic acid cocrystal, expressed as 2θ angles, appear at 9.08°, 13.01°, 13.39°, 13.78°, 15.88°, 16.55°, 18.78°, 19.29°, 20.87°, 23.34°, 26.27°, 27.33° and 29.79°.
Dependencies are inferred from the claim text.