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Rifapentine or Rifampicin microemulsion and suspension perfusate and injection and their preparation

A technology of rifapentine and rifampicin, which is applied in the field of broad-spectrum killing Mycobacterium tuberculosis antibiotic drug microemulsion solution, can solve the problem that there are not many effective treatment methods for refractory tuberculosis, and reduce economic burden and pain. , the effect of shortening the treatment period

Inactive Publication Date: 2005-06-22
WUHAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

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

[0024] Rifapentine or rifampicin microemulsion solution formula (weight percentage, following formula is the same):

[0025] Rifapentine or rifampicin 3.5

[0026] Lauroyl diethanolamine 8

[0027] Distilled water 88.5.

[0028] Preparation:

[0029] Accurately weigh rifapentine or rifampicin, lauroyl diethanolamine, place in a round-bottomed flask, add chloroform and shake, so that each component is fully dissolved, and a red transparent solution is formed. Water bath at 50°C, vacuumize, and distill to remove the solvent, so that the drug and emulsifier form a transparent red film on the bottle wall. Add a little distilled water to wet the film, stir to dissolve the film, then add distilled water to become a transparent solution. Pour out the solution, wash the flask several times with the remaining distilled water, combine the obtained solutions, and ultrasonically vibrate or grind to obtain a nearly transparent red solution, which is the rifapentine or rifampicin microe...

Embodiment 2

[0031] Rifapentine or rifampicin compound drug microemulsion formula:

[0032] Rifapentine or rifampicin 3.5

[0033] Ciprofloxacin 2

[0034] Lauroyl diethanolamine 8

[0035] Lidocaine 0.05

[0036] Distilled water 86.45.

[0037] Method of preparation:

[0038] Accurately weigh rifapentine or rifampicin, ciprofloxacin, lauroyl diethanolamine, and lidocaine and place them in a reactor, add chloroform and absolute ethanol, and oscillate to fully dissolve each component, forming a red transparent solution .

[0039] Water bath at 50°C, vacuumize, and distill off the solvent, so that the drug and emulsifier form a thin film on the wall of the vessel.

[0040] Add a little distilled water to wet the film, stir vigorously to dissolve the film, then add distilled water to become a translucent solution.

[0041] Pour out the solution, wash the reactor several times with the remaining distilled water, combine the obtained solutions, and ultrasonically oscillate or grind to ob...

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PUM

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Abstract

The invention relates to a microemulsion solution of broad-spectrum killing Mycobacterium tuberculosis antibiotics such as rifapentine (Dickfei) or rifampicin and a preparation method thereof. The rifapentine or rifampicin microemulsion for perfusion or injection is characterized in that: it is made up of rifapentine or rifampicin, lauroyldiethanolamine, distilled water, and the total weight percentage of each component is: Rifapentine or rifampicin 3.5, lauroyl diethanolamine 8, distilled water 88.5. The invention not only has a simple preparation method, but also has sustained and controlled release; the invention breaks through the limitation that rifapentine and other drugs are only used for oral administration, and creates rifapentine or rifampicin microemulsion solution perfusion solution and injection solution.

Description

technical field [0001] The invention relates to a microemulsion solution of broad-spectrum killing Mycobacterium tuberculosis antibiotics such as rifapentine (Dickfei) or rifampicin and a preparation method thereof. Background technique [0002] Rifapentine (Dickfell) or rifampicin is a class of broad-spectrum antibiotics that kill Mycobacterium tuberculosis, widely used in the treatment of tuberculosis and other tuberculosis. Because this type of drug is slightly soluble 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 or rifampicin is a widely used first-line drug in the clinical treatment of various tuberculosis. The solubility of rifapentine or rifampicin in water is extremely low, so far there are no reports on the preparation and clinical application of aqueous preparations and injections. At present, rifapentine or rifampicin dry powder ...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K9/107A61K31/496A61P31/06
Inventor 束家有广一平陈应夫刘志成张涛陈绪汉徐学文冯金海
Owner WUHAN UNIV
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