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Cetilistat crystal

A new Lilistat and crystal technology, applied in the field of crystals for obesity drugs, can solve problems such as affecting drug bioavailability and absorption, clinical efficacy differences, etc. Effect

Inactive Publication Date: 2016-10-19
BEIJING WINSUNNY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Different crystals of the same drug may be significantly different in appearance, solubility, melting point, dissolution rate, etc., and different crystals have different solubility and dissolution rates, which affect the bioavailability and absorption of the drug, resulting in differences in clinical efficacy

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Take 1ml of triethylamine and 19ml of dichloromethane and mix well, add 300mg of neolipristal, stir to dissolve at 50℃, filter to remove impurities while hot, and obtain a bright yellow clear solution, then add 20ml of methanol to mix well, and seal the resulting solution It was placed at 25°C for crystallization, and the solid was filtered out and dried to obtain 286 mg of neolipristal crystal I with a yield of 95.3% and a purity of 99.9%.

[0040] After determination, the X-ray powder diffraction pattern of the new lipristal crystal I obtained is as follows figure 1 As shown, it has the following X-ray powder diffraction data:

[0041]

Embodiment 2

[0043] Take 2ml of triethylamine and 18ml of acetone and mix well, add 300mg of neolipristal, stir to dissolve at 40℃, filter while hot to remove impurities, and obtain a bright yellow clear solution, then add 30ml of acetonitrile to mix well, and place the resulting solution sealed in It was allowed to stand for crystallization at 40°C, and the solid was filtered and dried to obtain 262 mg of neolipristal crystal I, with a yield of 87.3% and a purity of 99.7%. The X-ray powder diffraction pattern data is the same as that of Example 1.

Embodiment 3

[0045] Take 3ml of triethylamine and 17ml of dioxane and mix well, add 300mg of neolipristal, stir to dissolve at 50°C, filter while hot to remove impurities to obtain a bright yellow clear solution, then add 40ml of water to mix well, and the resulting solution It was sealed and placed at 20°C for crystallization, and the solid was filtered out and dried to obtain 269 mg of neolipristal crystal I, with a yield of 89.7% and a purity of 99.6%. The X-ray powder diffraction pattern data is the same as that of Example 1.

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Abstract

The present invention relates to a cetilistat crystal, which has good solubility and good stability, and is not easily subjected to crystal transition. The invention further provides a preparation method of the cetilistat crystal, wherein the method has characteristics of good reproducibility, easy condition control, high crystal yield, high crystal purity, and industrialized large-scale production.

Description

technical field [0001] The invention relates to a crystal of a medicine for treating obesity, in particular to a crystal of Neolistat. Background technique [0002] Obesity is a chronic disease manifested by excess body fat tissue or an excessively high ratio of adipose tissue to other soft tissues. WHO defines obesity in adults: BMI [body mass index: weight / height squared (kg / m 2 )] at 25-29.9 is overweight, 30 is obese, and 40 is severely obese. With the improvement of living standards, the proportion of obese people in the total population of the society is increasing, and the prevalence of obesity is three times that of 20 years ago. The proportion of obese patients with metabolic syndrome such as diabetic lipid metabolism disorder is as high as 7.68%, and the risk of tumors is also increased. Numerous US and European studies have shown that mortality from obesity varies with BMI. A BMI greater than 32 can double the mortality rate. Obesity reduces life expectancy by ...

Claims

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Application Information

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IPC IPC(8): C07D265/26A61K31/536A61P3/04
CPCC07D265/26
Inventor 林国良周浩辉吴尧耿玉先产运霞李泳
Owner BEIJING WINSUNNY PHARMA CO LTD
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