Methodc for preparing sub-micron gemfibrozil medicament powder

A gemfibrozil and submicron technology is applied in the field of preparing submicron ultrafine gemfibrozil pharmaceutical powder by a reactive crystallization method, and can solve the problems of large amount of surfactant and the like

Active Publication Date: 2007-12-05
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of this formula is that the amount of surfactant as non-pharmaceutical active ingredients is relatively large, about 1% to 4% (wt / wt)
There is no report on increasing the dissolution rate of gemfibrozil by micronization

Method used

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  • Methodc for preparing sub-micron gemfibrozil medicament powder
  • Methodc for preparing sub-micron gemfibrozil medicament powder
  • Methodc for preparing sub-micron gemfibrozil medicament powder

Examples

Experimental program
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Effect test

Embodiment 1

[0034] Weigh 0.16g of polyvinylpyrrolidone K30 and dissolve it in 100ml of aqueous hydrochloric acid solution with a concentration of 0.25mol / L. After it is completely dissolved, pour it into a reaction kettle and stir at a speed of 1000rpm. Then weigh 3.0 g of the gemfibrozil bulk drug and dissolve it in 100 ml of aqueous sodium hydroxide with a concentration of 0.15 mol / L to obtain a gemfibrozil bulk drug solution. The obtained bulk drug solution was quickly added into the reaction kettle, and the gemfibrozil drug was reacted and crystallized at 20° C. to obtain a suspension of gemfibrozil drug particles, and the stirring was continued for 30 minutes. Then filter and rinse the filter cake with deionized water. The obtained filter cake was put into a forced air drying oven at 40° C. to dry for more than 3 hours to obtain the dried gemfibrozil drug powder. Observation with electron scanning electron microscope, as shown in the scanning electron microscope photo in Figure 2, t...

Embodiment 2

[0036] Weigh 0.15 g of methylcellulose and dissolve it in 100 ml of aqueous hydrochloric acid solution with a concentration of 0.25 mol / L. After it is completely dissolved, pour it into a reaction kettle and stir at a speed of 10,000 rpm. Then weigh 3.0 g of the gemfibrozil bulk drug and dissolve it in 100 ml of aqueous sodium hydroxide with a concentration of 0.15 mol / L to obtain a gemfibrozil bulk drug solution. Quickly add the obtained raw material drug solution into the reaction kettle, so that the gemfibrozil drug is reacted and crystallized at 18° C. to obtain a suspension of gemfibrozil drug particles, continue to stir and age for 30 minutes, then filter, and use deionized water Rinse filter cake. Put the obtained filter cake into a beaker, add water with a weight equivalent to 5 times the weight of the wet filter cake, and redisperse the filter cake in water under the action of ultrasound to obtain a uniform suspension. The resulting suspension was poured into liquid ...

Embodiment 3

[0038] Weigh 0.39g of methylcellulose and dissolve it in 500ml of aqueous hydrochloric acid solution with a concentration of 0.05mol / L. After it is completely dissolved, pour it into a reaction kettle and stir at a speed of 2000rpm. Then weigh 2.6g of the gemfibrozil bulk drug and dissolve it in 100ml of sodium hydroxide solution with a concentration of 0.10mol / L to obtain the gemfibrozil bulk drug solution. Quickly add the obtained raw drug solution into the reaction kettle, make the gemfibrozil drug react and crystallize at 20° C. to obtain a suspension of gemfibrozil drug particles, continue to stir and age for 30 minutes, then filter, and use deionized water Rinse filter cake. The obtained filter cake is put into a quick drying apparatus for drying to obtain dry gemfibrozil drug powder. Observed by scanning electron microscope, gemfibrozil drug particles are spherical, with a particle size of 500nm-2μm and a narrow particle size distribution, as shown in the scanning elec...

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Abstract

The present invention is process of preparing gemfibrozil medicine powder, and belongs to the field of insoluble medicine micronizing technology. Through dissolving gemfibrozil medicine in water solution of sodium hydroxide, neutralizing and replacing with added water solution of hydrochloric acid containing surfactant to obtain suspension of gemfibrozil medicine, filtering, washing and drying, spheroid gemfibrozil medicine powder in submicron size is produced. The process is simple, low in cost and easy in industrial application, and the obtained gemfibrozil medicine powder has regular shape, narrow size distribution and high dispersivity. The present invention lays foundation for the industrial production and the new preparation form development of gemfibrozil medicine.

Description

technical field [0001] The invention relates to a method for preparing gemfibrozil drug powder, in particular to a method for preparing submicron ultrafine gemfibrozil drug powder by adopting a reaction crystallization method. Background technique [0002] Gemfibrozil (Gemfibrozil), the chemical name is 2,2-dimethyl-5-(2,5-xylyloxy)-pentanoic acid, and its structural formula is: [0003] [0004] It is a non-halogenated clofibrate lipid-lowering drug that can effectively reduce blood total cholesterol, total triglycerides, very low-density lipoprotein cholesterol and triglycerides, low-density lipoprotein cholesterol and triglycerides content, increase the concentration of high-density lipoprotein cholesterol. Therefore, it is widely used clinically to treat Fredrickson type IIa, type IIb, type III, type IV, type V hyperlipidemia and various coronary heart diseases, dyslipidemia and metabolic syndrome caused by diabetes. Gemfibrozil is currently on the market in the for...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/192A61P3/06
Inventor 陈建峰黄巧萍陈桂子王洁欣
Owner BEIJING UNIV OF CHEM TECH
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