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Cetilistat solid dispersion and medicinal preparation prepared from the solid dispersion

A solid dispersion, the technology of new Lilistat, applied in the direction of drug combination, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of affecting drug efficacy, low bioavailability, Problems such as low solubility

Active Publication Date: 2016-07-27
BEIJING WINSUNNY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Neolistat has very low solubility in water. EP1897558 discloses that its solubility in water at 37°C does not exceed 10 mg / L. Therefore, when the poorly soluble Neolistat is administered orally, its bioavailability is inevitably low , affecting the efficacy of the drug

Method used

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  • Cetilistat solid dispersion and medicinal preparation prepared from the solid dispersion
  • Cetilistat solid dispersion and medicinal preparation prepared from the solid dispersion
  • Cetilistat solid dispersion and medicinal preparation prepared from the solid dispersion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Mix 120mg of Neolistat and 240mg of hydroxypropyl cellulose evenly, heat in an oil bath, raise the temperature to 120°C, the mixture melts into a viscous shape, and cool rapidly; crush the cooled mixture and pass through a 60-mesh sieve to obtain Solid dispersion.

Embodiment 2

[0061] Dissolve 120 mg neolistat and 120 mg copovidone in 150 ml acetone, and dry in vacuum to obtain a solid dispersion.

Embodiment 3

[0063] Mix 120mg of Neolistat, 300mg of hydroxypropyl cellulose, and 300mg of copovidone evenly, heat in an oil bath, and raise the temperature to 110°C. 60 mesh sieve to obtain a solid dispersion.

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PUM

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Abstract

The invention relates to cetilistat solid dispersion, and a medicinal preparation prepared from the solid dispersion. The cetilistat and one or both of the carriers hydroxypropyl cellulose and copovidone are prepared into a solid dispersion to significantly improve the solubility of the cetilistat, and overcome low solubility of cetilistat, so that the prepared medicinal preparation achieves good dissolution, and has increased bioavailability.

Description

technical field [0001] The invention relates to a solid dispersion of medicine for treating obesity and a pharmaceutical preparation thereof, in particular to a new lixistat solid dispersion and a pharmaceutical preparation thereof. 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 w...

Claims

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Application Information

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IPC IPC(8): A61K31/536A61K9/14A61K47/38A61K47/32A61P3/04
Inventor 马贵红陈彦瑶刘丽敏耿玉先产运霞
Owner BEIJING WINSUNNY PHARMA CO LTD