Slow released antituberculotic preparation

A tuberculosis, slow-release agent technology, applied in the field of anti-tuberculosis drug slow-release agents, can solve the problems of difficult to obtain effective bactericidal concentration, increased dosage, and unsatisfactory effect of multidrug-resistant tuberculosis

Inactive Publication Date: 2006-11-08
SHANDONG LANJIN PHARMA
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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
There will be many side effects if the dose is increased or the drug is taken for a long time

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] 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 100 ml of dichloromethane to each container, dissolve and mix well, add 10 mg rifampicin, 10 mg rifamycin, 10 mg rifampicin and 10 mg rifamycin respectively, re-shake and spray dry Microspheres for injection containing 10% rifampicin, 10% rifamycin and 10% rifampicin and 10% rifamycin were prepared by 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

[0100] 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:

[0101] (a) 2-40% rifampicin, rifamycin, rifapentine or utilbutin;

[0102] (b) 2-40% rifampicin in combination with 2-40% rifamycin, rifapentine or rifabutin;

[0103] (c) 2-40% rifamycin in combination with 2-40% rifapentine or rifabutin;

[0104] (d) Combination of 2-40% rifapentine and 2-40% urbutin.

Embodiment 3

[0106] 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 rifampicin, 30mg rifapentine, 15mg rifampicin and 15mg rifapentine into three containers respectively, shake up again and use spray drying method to prepare 30% rifampicin, 30% rifapentine 15% rifampicin and 15% rifapentine injection microspheres. 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 antituberculotic preparation is implanting agent or injection with slow releasing of medicine in the local tuberculosis focus to maintain the local effective medicine concentration while lowing the systemic toxicity. The slow released injection consists of slow released microsphere and solvent. The slow released microsphere consists of slow releasing supplementary material and antituberculotic selected from rifampicin, rifamycin, rifapentine and / or rifabutine. The solvent is special solvent containing suspending agent of carboxymethyl cellulose sodium, etc. and has viscosity of 100-3000 cp at 20-30 deg.c. The slow releasing supplementary material is selected from EVAc, PLA, PLGA, etc. The slow released preparation may be prepared with slow released microsphere. The present invention has obvious and unique treating effect on various kinds of intractable tuberculosis.

Description

(1) Technical field [0001] The invention relates to an anti-tuberculosis drug sustained-release agent, belonging to the technical field of drugs. Specifically, the invention provides a slow-release preparation containing 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 investment in related preventio...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/395A61K31/496A61K45/00A61K47/32A61K47/34A61K47/36A61K47/38A61K47/42
Inventor 孙娟
Owner SHANDONG LANJIN PHARMA
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