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Slow released antituberculotic preparation

A slow-release preparation and anti-tuberculosis technology, applied in the field of anti-tuberculosis drug slow-release preparations, can solve the problems of difficulty in obtaining effective bactericidal concentration, side effects of increased doses, and unsatisfactory effects of multidrug-resistant tuberculosis, so as to facilitate drug application and reduce Effects of course of treatment, unique healing effect

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

[0115] 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 ofloxacin, 10mg capreomycin, 10mg ofloxacin and 10mg capreomycin respectively, re-shake and spray Microspheres for injection containing 10% ofloxacin, 10% capreomycin and 10% ofloxacin and 10% capreomycin were prepared by 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 slow-release injection in physiological saline in vitro is 20-30 days, and the drug release time in mice subcutaneous is about 40-50 days.

Embodiment 2

[0117] 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:

[0118] (a) 2-50% ofloxacin, ciprofloxacin or sparfloxacin in combination with 2-50% capreomycin;

[0119] (b) 2-50% ofloxacin, ciprofloxacin or sparfloxacin in combination with 2-50% sodium taurocholate or sodium taurodeoxycholate;

[0120] (c) 2-50% capreomycin in combination with 2-50% sodium taurocholate or sodium taurodeoxycholate; or

[0121] (d) Combination of 2-50% ofloxacin, ciprofloxacin or sparfloxacin with 2-50% capreomycin and 2-50% sodium taurocholate or sodium taurodeoxycholate .

Embodiment 3

[0123] 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 ciprofloxacin, 30mg capreomycin, 15mg ciprofloxacin and 15mg capreomycin to three containers respectively, re-shake and use spray drying method to prepare 30% ciprofloxacin, 30% capreomycin Injectable microspheres of ciprofloxacin, 15% ciprofloxacin and 15% capreomycin. 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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Abstract

The slow released antituberculotic preparation contains the composition of ofloxacin, ciprofloxacin or sparxacin, capreomycin, sodium taurocholate and / or deoxysodium taurocholate. The slow released antituberculotic preparation is slow released injection or slow released implanting agent. The 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, etc. and with 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 implanting agent is prepared through a certain process. The present invention has obvious unique treating effect on various kinds of intractable tuberulosis.

Description

(1) Technical field [0001] The invention relates to a slow-release preparation of 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 investment in ...

Claims

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Application Information

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IPC IPC(8): A61K38/04A61K9/10A61K31/496A61K31/5383A61K31/575A61K47/10A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61P31/06
Inventor 孙忠厚
Owner JINAN SHUAIHUA PHARMA TECH
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