Slow released compound antituberculotic preparation containing synergist

An anti-tuberculosis and synergistic technology, which is applied in the field of compound anti-tuberculosis drug sustained-release preparations, can solve the problems of difficulty in obtaining effective bactericidal concentration, increased dose side effects, unsatisfactory effects of multidrug-resistant tuberculosis, etc., and achieves convenient drug application, The effect of reducing the course of treatment, unique treatment effect

Inactive Publication Date: 2006-11-08
JINAN SHUAIHUA PHARMA TECH
View PDF8 Cites 3 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0123] 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 ofloxacin, 10 mg rifampicin and 10 mg ofloxacin respectively, re-shake and spray dry Microspheres for injection containing 10% rifampicin, 10% ofloxacin and 10% rifampicin and 10% ofloxacin were prepared by this 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

[0125] 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:

[0126] (a) 2-50% rifampicin, rifamycin, rifapentine or ributin with 2-50% cycloserine, ofloxacin, ciprofloxacin, sparfloxacin or curly Combinations of mycins;

[0127] (b) 2-50% streptomycin, kanamycin, amikacin or amikacin and 2-50% cycloserine, ofloxacin, ciprofloxacin, sparza A combination of star or capreomycin;

[0128] (c) 2-50% of isoniazid, pyrazinamide, ethambutol or sodium p-aminosalicylate and 2-50% of cycloserine, ofloxacin, ciprofloxacin, sparfloxacin or Combinations of capreomycin;

[0129] (d) 2-50% combination of rifampicin and pyrazinamide with 2-50% cycloserine, ofloxacin, ciprofloxacin, sparfloxacin or capreomycin;

[0130] (e) 2-50% of ethionamide or prothione in combination with 2-50% of cycloserine, ofloxacin, ciprofloxacin, sparfloxacin or capreo...

Embodiment 3

[0135] 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 ofloxacin, 15mg rifapentine and 15mg ofloxacin into three containers respectively, shake up again and use spray drying method to prepare 30% rifapentine, 30 % ofloxacin, 15% rifapentine and 15% ofloxacin 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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The slow released compound antituberculotic preparation containing synergist is implanting agent or slow released injection comprising slow released microsphere and solvent. The slow released microsphere consists of slow releasing supplementary material, at least one antituberculotic selected from rifampicin, isoniazid and pyrazinamide and at least one antituberculotic synergist selected from cycloserine, ofloxacin, ciprofloxacin, sparfloxacin and capreomycin. 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 compound antituberculotic preparation can release antituberculotic in the local tubercolosis part for 30-40 days so as to maintain the local effective medicine concentration while lowering systemic toxicity. 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 compound anti-tuberculosis drugs, which belongs to the technical field of drugs. Specifically, the present invention provides a slow-release preparation of a compound anti-tuberculosis drug containing a synergist, 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 and isoniazid, tuberculosis became a treatable disease. However, with people's ignorance of it...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K9/10A61K31/496A61K31/4965A61K31/7036A61K47/26A61K47/34A61K47/36A61K47/42A61P31/06
Inventor 孙娟
Owner JINAN SHUAIHUA PHARMA TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap