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Cetilistat crystal

A new technology of lixistat and crystals, which is applied in the field of crystals for the treatment of obesity, can solve the problems affecting the bioavailability and absorption of drugs, and the difference in clinical drug effects, and achieve easy control, difficult crystal transformation, and good stability 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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  • Cetilistat crystal
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Take 300mg of Neolistat in a round-bottomed flask of appropriate volume, add 30mL of dichloromethane, stir and dissolve at 30°C, filter while hot to remove impurities, and spin-evaporate the obtained filtrate in a round-bottomed flask at a temperature of 40°C The obtained solid was dried in an oven to obtain 293 mg of Neolistat Crystal II with a yield of 97.7% and a purity of 99.6%.

[0035] After determination, the X-ray powder diffraction pattern of its obtained new lisstat crystal II is as follows: figure 1 As shown, where the 2θ angles are: 3.9±0.2°, 7.8±0.2°, 12.7±0.2°, 18.2±0.2°, 20.2±0.2°, 23.7±0.2°, 24.5±0.2°, 25.3±0.2° Characteristic peaks.

Embodiment 2

[0037] Take 500mg of Neolistat in a round-bottomed flask of appropriate volume, add 50mL of dichloromethane, stir and dissolve at 50°C, filter while hot to remove impurities, and spin-evaporate the obtained filtrate in a round-bottomed flask at a temperature of 42°C The obtained solid was dried in an oven to obtain 487 mg of Neolistat Crystal II with a yield of 97.4% and a purity of 99.9%. Its X-ray powder diffraction pattern data are with embodiment 1.

Embodiment 3

[0039] Take 400mg of Neolistat in a round-bottomed flask of appropriate volume, add 40mL of dichloromethane, stir and dissolve at 45°C, filter while hot to remove impurities, and spin-evaporate the obtained filtrate in a round-bottomed flask at a temperature of 43°C The obtained solid was dried in an oven to obtain 387 mg of Neolistat Crystal II with a yield of 96.8% and a purity of 99.9%. Its X-ray powder diffraction pattern data are with embodiment 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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Patent Type & Authority Applications(China)
IPC IPC(8): C07D265/26A61K31/536A61P3/04
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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