Sustained-release agent containing tuberculosis-resistance medicament

A tuberculosis and anti-tuberculosis technology, applied in the direction of antibacterial drugs, drug delivery, medical preparations containing active ingredients, etc., can solve problems such as difficulty in obtaining effective bactericidal concentration, increased dose side effects, and unsatisfactory effects of multidrug-resistant tuberculosis

Inactive Publication Date: 2008-09-03
JINAN KANGQUAN 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

[0110] Put 90, 90 and 80 mg of polystyrene (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) 20:80) copolymer into (A), (B) and (C) three Then add 100 ml of dichloromethane to each container. After dissolving and mixing, add 10m cycloserine, 10mg ofloxacin, 10mg cycloserine and 10mg ofloxacin respectively, shake well and use spray drying method Prepare injection microspheres containing 10% cycloserine, 10% ofloxacin, 10% cycloserine and 10% ofloxacin. Then the microspheres are suspended 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℃-30℃). The release time of the sustained-release injection in vitro in physiological saline is 15-20 days, and the release time under the skin of mice is about 30-40 days.

Embodiment 2

[0112] The process of processing into a sustained-release injection is the same as in Example 1, but the difference is that the anti-tuberculosis active ingredient and its weight percentage are:

[0113] (1) 5-40% cycloserine, ofloxacin, ciprofloxacin or sparfloxacin;

[0114] (2) A combination of 5-40% cycloserine and 5-40% ofloxacin, ciprofloxacin or sparfloxacin;

[0115] (3) A combination of 5-40% ofloxacin and 5-40% ciprofloxacin or sparfloxacin; or

[0116] (4) A combination of 5-40% ciprofloxacin and 5-40% sparfloxacin.

Embodiment 3

[0118] Put 70mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65000 into three containers (A), (B) and (C), and then add 100 ml of dichloromethane to each, dissolve and mix well , Respectively add 30mg cycloserine, 30mg ciprofloxacin, 15mg cycloserine and 15mg ciprofloxacin to three containers, shake well and spray dry to prepare 30% cycloserine, 30% ciprofloxacin, Microspheres for injection of 15% cycloserine and 15% ciprofloxacin. The dried microspheres were suspended in physiological saline containing 1.5% sodium carboxymethyl cellulose to prepare the corresponding suspension type sustained-release injection. The viscosity of the injection is 300cp-600cp (at 20℃-30℃). The release time of the sustained-release injection in physiological saline in vitro is 10-15 days, and the release time under the skin of mice is about 20-30 days.

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Abstract

The invention relates to a slow-release implant or a slow-release injection containing antituberculotic drug(s), which can be locally placed on or injected into tuberculosis foci to slowly release the antituberculotic drug(s), so as to effectively obtain and keep effective drug concentration at local foci and at the same time reduce the systemic toxicity of the drug. The slow-release injection comprises slow-release microspheres and a solvent, wherein the slow-release microspheres comprise slow-release adjuvants and antituberculotic drug(s) selected from cycloserine, ofloxacin, ciprofloxacin and / or sparfloxacin; the solvent is a special solvent containing a suspending agent; the suspending agent has viscosity of 100-3,000cp (at 20-30 DEG C) and is selected from sodium carboxymethyl cellulose, etc.; the slow release adjuvants are selected from EVAc, polifeprosan, polylactic acid (PLA), polys(lactic-co-glycolic acid) (PLGA), poly(erucic acid dimmer-sebacic acid or fumaric acid-sebacic acid) copolymers, etc.; and the slow-release implant can be made from the slow-release microspheres or by other methods. The inventive agent has distinct and unique therapeutic effect on refractory tuberculosis, such as multiple drugs resistant bacillus tuberculosis infection, tuberculoma, tuberculosis in lymph, joint, kidney, skin, intestine, mammary gland and genitalia, tuberculous osteomyelitis, fistulous tract, and cavermous pulmonary tuberculosis.

Description

(1) Technical field [0001] The invention relates to a slow-release agent containing anti-tuberculosis drugs, belonging to the technical field of medicines. Specifically, the present invention provides a sustained-release agent containing cycloserine and / or quinolone anti-tuberculosis drugs, which are mainly sustained-release injections and sustained-release implants. The sustained-release agent is mainly applied locally, which can obtain and maintain the effective drug concentration locally in the tuberculosis lesion. (2) Background technology [0002] Tuberculosis, represented by tuberculosis, is originally a disease that seriously affects people's health. It is widespread all over the world, killing hundreds of millions of people. It is called the white plague, and there was a saying of "ten tuberculosis and nine deaths". With the advent of antituberculosis drugs such as streptomycin, tuberculosis has become a treatable disease. However, with people neglecting its seriousness, ...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K9/16A61K31/5383A61K31/496A61K31/421A61K47/34A61K47/32A61K47/36A61K47/42A61K47/26A61K47/38A61P31/06
Inventor 孙忠厚
Owner JINAN KANGQUAN PHARMA TECH
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