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Slow released compound antituberculotic preparation

A slow-release preparation and anti-tuberculosis technology, which is applied in the field of compound anti-tuberculosis drug slow-release preparations, can solve the problems of difficulty in obtaining effective bactericidal concentration, unsatisfactory effect of multidrug-resistant tuberculosis, and side effects of increasing doses, so as to achieve convenient drug application, Unique healing effect, effect of reducing course of treatment

Inactive Publication Date: 2006-11-08
JINAN SHUAIHUA PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, many new anti-tuberculosis drugs have shown good efficacy, but the effect on multidrug-resistant tuberculosis (MDR-TB) is not ideal
Because for many chronic lesions, especially local lesions, it is difficult to obtain an effective bactericidal concentration with the administration of conventional therapy
Increased dose or long-term use of drugs will have many side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0136] Put 90, 90 and 80 mg of polyphenylpropane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) at 20:80) copolymers into (A), (B) and (C) three Add 100ml of dichloromethane to each container, dissolve and mix well, add 10mg rifampicin, 10mg ethionamide, 10mg rifampicin and 10mg ethionamide respectively, re-shake and use Microspheres for injection containing 10% rifampicin, 10% ethionamide and 10% rifampicin and 10% ethionamide were prepared by spray-drying method. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 300cp-600cp (at 20°C-30°C). The drug release time of the sustained release injection in physiological saline in vitro is 15-20 days, and the drug release time in mice subcutaneous is about 30-40 days.

Embodiment 2

[0138] The method step of being processed into slow-release injection is identical with embodiment 1, but difference is that contained anti-tuberculosis active ingredient and weight percentage thereof are:

[0139] (a) rifampicin, rifamycin, rifapentine, or ributin in combination with isoniazid, pyrazinamide, ethambutol, or ammonium salicylate;

[0140] (b) rifampicin, rifamycin, rifapentine, or rifabutin in combination with streptomycin, kanamycin, amikacin, or amikacin;

[0141] (c) rifampicin, rifamycin, rifapentine, or a combination of rifabutin and ethionamide or prothionamide;

[0142] (d) combinations of isoniazid, pyrazinamide, ethambutol or sodium salicylate with streptomycin, kanamycin, amikacin or amikacin;

[0143] (e) isoniazid, pyrazinamide, ethambutol, or sodium salicylate in combination with ethionamide or prothione; or

[0144] (f) Combinations of streptomycin, kanamycin, amikacin or amikacin with ethionamide or prothione.

Embodiment 3

[0146] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65,000 into three containers (A), (B) and (C) respectively, and then add 100 ml of dichloromethane to each, dissolve and mix well , add 30mg rifapentine, 30mg prothionamide, 15mg rifapentine and 15mg prothionamide to three containers respectively, re-shake and prepare 30% rifapentine by spray drying method , 30% prothionamide, 15% rifapentine and 15% prothionamide microspheres for injection. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The viscosity of the injection is 300cp-600cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

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PUM

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Abstract

The slow released compound antituberculotic preparation contains at least one of rifampicin, pyrazinamide, kanamycin, isoniazide, rifapentine, etc. The slow released preparation is slow released injection or slow released implanting agent. The slow released injection consists of slow released microsphere and solvent, the slow released microsphere contains slow releasing supplementary material and antituberculotic, and the solvent is special solvent containing suspending agent carboxymethyl cellulose sodium and of viscosity of 100-3000 cp at 20-30 deg.c. The slow releasing supplementary material is EVAc, PLA, PLGA, sebacic acid copolymer, etc. The slow released compound antituberculotic preparation is set or injected into local tuberulosis focus to treat various kinds of intractable tuberulosis, and has medicine releasing period up to 30-40 days, less systemic toxicity and unique curative effect.

Description

(1) Technical field [0001] The invention relates to a slow-release preparation of compound anti-tuberculosis drugs, which belongs to the technical field of drugs. Specifically, the invention provides a slow-release preparation containing compound anti-tuberculosis drugs, mainly slow-release injections and slow-release implants. The slow-release agent is mainly applied locally, and can obtain and maintain an effective drug concentration in the local area of ​​the tuberculosis lesion. (2) Background technology [0002] Tuberculosis, represented by pulmonary tuberculosis, is a disease that seriously affects people's health. It is widespread all over the world and has killed hundreds of millions of people. People call it the white plague. There was a saying that "ten tuberculosis and nine deaths". With the advent of anti-tuberculosis drugs such as streptomycin, tuberculosis became a treatable disease. However, with people's ignorance of its severity, obvious insufficient inves...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/60A61K9/10A61K31/395A61K31/496A61K31/4965A61K45/00A61P31/06
Inventor 孔庆新
Owner JINAN SHUAIHUA PHARMA TECH
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