Refapentine or rifampin liposome perfusate, injection and preparation process thereof

A technology of rifampicin lipid and rifapentine, applied in the field of liposome solution, can solve the problems of few effective treatment methods, difficult clinical treatment of pulmonary tuberculosis, insufficient dispersion of emulsion, etc. The effect of significant treatment effect and shortened treatment period

Inactive Publication Date: 2004-11-24
广一平 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] About the preparation of rifampicin microemulsion Microencapsulation 1995; 12 (4) 401 reported a method, dissolving rifampicin in Span 85 was prepared into an oil droplet suspension, which was used for the sterilization experiment of Mycobacterium tuberculosis. This emulsion The dispersion is not good enough, the stability is poor, and it has not been used clinically so far
There are also reports in China that rifampicin is prepared into microcapsules by using degradable polymer material polylactic acid and attempts to develop their use. Due to the complexity of the preparation, the resulting particle size is too large and the distribution is uneven, so it is difficult to be used as an injection or perfusion solution. Clinical treatment for tuberculosis
Chinese patent 98113445 reports that rifampicin, isoniazid and pyrazinamide composite preparations are used for the treatment of tuberculosis. Research content of pentin or rifampicin compound drug liposome perfusion solution and injection
[0005] At present, the incidence of tuberculosis in my country is on the rise, and there are not many drugs and effective treatments for refractory tuberculosis.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094] Rifapentine or rifampicin liposome microemulsion formula, the weight ratio of each component is:

[0095] Rifapentine / rifampicin 3.5

[0096] Lecithin 5.0

[0097] Cholesterol 3.0

[0098] Lauroyl diethanolamine 0.5

[0099] Distilled water 88.

[0100] Preparation:

[0101] Accurately weigh rifapentine (rifampicin), lecithin, cholesterol, and lauroyl diethanolamine and place them in a round-bottomed flask, add chloroform and absolute ethanol, and oscillate to fully dissolve each component to form a red transparent solution. Water bath at 50°C, vacuumize, and distill to remove the solvent, so that lecithin, cholesterol and drugs form a thin film on the bottle wall. Add a little distilled water to make the film wet and swell, stir quickly to make the film fall off and dissolve, add medical distilled water to become a translucent solution. The solution was poured out, and the flask was washed several times with the remaining distilled water. The resulting solutions we...

Embodiment 2

[0104] Rifapentine or rifampicin composite drug liposome microemulsion formula, the weight ratio of each component is:

[0105] Rifapentine / rifampicin 3.5

[0106] Ofloxacin 2.0

[0107] Lecithin 4.0

[0108] Cholesterol 3.0

[0109] Lauroyl diethanolamine 3.5

[0110] distilled water 84.

[0111] Preparation:

[0112] Accurately weigh rifapentine, ofloxacin, lecithin, cholesterol, and lauroyl diethanolamine into a round-bottomed flask, add chloroform and absolute ethanol, and oscillate to fully dissolve each component to form a red transparent solution. Water bath at 50°C, vacuumize, and distill to remove the solvent, so that lecithin, cholesterol and drugs form a thin film on the bottle wall. Add a little distilled water to make the film wet and swell, stir quickly to make the film fall off and dissolve, then add distilled water to become a translucent solution. The solution was poured out, and the flask was washed several times with the remaining distilled water. The...

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Abstract

The present invention is characterized by that it uses (by weight percentage) 1-22% of rifampin or rifapentine, 1-27% of lecithin, 1-18 % of cholesterol and 70-100 % of distilled water as main components, and adds emulsifier and auxiliary medicine so as to respectively obtain the rifapentine or rifampin liposome micro emulsion perfusate and injection and rifupentine or rifampin composite medicine liposome micro emulsion perfusate and injection. Said invention also provides their preparation method.

Description

technical field [0001] The present invention relates to the liposome solution of broad-spectrum killing Mycobacterium tuberculosis antibiotic medicine of rifapentine (Dickfei), rifampicin, specifically relate to rifapentine, rifampicin liposome solution and liposome microparticles Perfusion and injection of emulsion solution, perfusion and injection of rifapentine or rifampicin compound drug liposome solution and compound drug liposome microemulsion solution. Background technique [0002] Rifapentine (Dickfei) and rifampicin are a class of broad-spectrum antibiotics that kill Mycobacterium tuberculosis, and are widely used in the treatment of tuberculosis and other tuberculosis. Because this type of drug is insoluble in water, its application is greatly limited. So far, there is no injection for clinical treatment at home and abroad, and it can only be administered orally. [0003] Rifapentine and rifampicin are the first-line drugs widely used in the treatment of various t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/496A61P31/06
Inventor 广一平束家有陈绪汉张涛冯金海刘志成
Owner 广一平
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