Vascular targeting embolism sustained release agent of triple compound microsphere for antituberculosis drug, preparation method and applications thereof

A blood vessel targeting and anti-tuberculosis technology, which is applied in the direction of antibacterial drugs, suppository delivery, pharmaceutical formulations, etc., can solve the problems of non-uniform sustained release of drugs, non-uniform sustained release, tissue necrosis or damage, etc., to achieve Effects of prolonging drug action time, reducing toxicity, and easy operation

Active Publication Date: 2014-12-17
THE 309TH HOSPITAL OF CHINESE PEOPLES LIBERATION ARMY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Currently clinical anti-tuberculosis drugs are mainly oral and injection preparations, even injections are not ideal
Because the effective drug concentration cannot be obtained at the lesion site, the relatively uniform and sustained release cannot be obtained, and the obvious systemic toxicity and drug resistance during the application process greatly limit the application of the drug. A small number of embolization plus drug infusion therapy There are also the following defects: the drug can not be released relatively uniformly; when the local perfusion drug concentration is too high, the shock wave effect of the drug may cause local tissue necrosis or damage

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] Example 1 Preparation of anti-tuberculosis drug triple compound microsphere blood vessel targeted embolism slow-release agent:

[0061] 1. Reagent preparation:

[0062] 1. 10g / L (1% (W / V)) carrier solution:

[0063] Accurately weigh 10 grams of sodium alginate (or chitosan) powder, dissolve it with physiological saline or water for injection at a concentration ratio of 10 g / L to obtain a carrier solution, i.e. sodium alginate or chitosan solution;

[0064] 2. Drug solution:

[0065] ① Rifampicin solution:

[0066] Put 10 grams of rifampicin powder into a mortar, add 20ml of water for injection to grind and dissolve, then wash the mortar with 30ml of water for injection, mix and then sonicate for 10 minutes to obtain rifampicin solution;

[0067] ② Isoniazid solution:

[0068] Weigh 20 grams of isoniazid powder, add 50 ml of water for injection to dissolve, and obtain isoniazid solution;

[0069] ③Pyrazinamide (or moxifloxacin) solution:

[0070] Claim 40 grams of ...

Embodiment 2

[0101] Example 2: Preparation of anti-tuberculosis drug triple compound microsphere vascular targeted embolism slow release agent:

[0102] 1. Reagent preparation:

[0103] 1. 60g / L (6% (W / V)) carrier solution:

[0104] Accurately weigh 60 grams of sodium alginate (or chitosan) powder, dissolve it with physiological saline or water for injection at a concentration ratio of 60 g / L to obtain a carrier solution, i.e. sodium alginate or chitosan solution;

[0105] 2. Drug solution:

[0106] ① Rifampicin solution:

[0107] Put 10 grams of rifampicin powder into a mortar, add 20ml of water for injection to grind and dissolve, then wash the mortar with 30ml of water for injection, mix and then sonicate for 10 minutes to obtain rifampicin solution;

[0108] ② Isoniazid solution:

[0109] Weigh 20 grams of isoniazid powder, add 50 ml of water for injection to dissolve, and obtain isoniazid solution;

[0110] ③Pyrazinamide (or moxifloxacin) solution:

[0111] Claim 40 grams of pyr...

Embodiment 3

[0142] Example 3: Preparation of anti-tuberculosis drug triple compound microsphere vascular targeted embolism slow release agent:

[0143] 1. Reagent preparation:

[0144] 1. 20g / L carrier solution:

[0145] Accurately weigh 20 grams of sodium alginate (or chitosan) powder, dissolve it with physiological saline or water for injection at a concentration ratio of 20 g / L to obtain a carrier solution, i.e. sodium alginate or chitosan solution;

[0146] 2. Drug solution:

[0147] ① Rifampicin solution:

[0148] Put 20 grams of rifampicin powder in a mortar, add 40ml of water for injection to grind and dissolve, then wash the mortar with 60ml of water for injection, mix and then sonicate for 10 minutes to obtain rifampicin solution;

[0149] ② Isoniazid solution:

[0150] Weigh 40 grams of isoniazid powder, add 100 ml of water for injection to dissolve, and obtain isoniazid solution;

[0151] ③Pyrazinamide (or moxifloxacin) solution:

[0152] Claim 80 grams of pyrazinamide (o...

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Abstract

The invention relates to a vascular targeting embolism sustained release agent of a triple compound microsphere for an antituberculosis drug, a preparation method and applications thereof. The sustained release agent comprises a carrier and a drug, wherein the drug is encapsulated by the carrier, the carrier is selected from sodium alginate or chitosan, and the drug is a triple compound antituberculosis drug which comprises rifampin, isoniazide and pyrazinamide or moxifloxacin. Three antituberculosis drugs are employed as matrixes of a drug solution, sodium alginate or chitosan is used as a carrier solution, and a prepared solution is obtained by mixing the drug solution and the carrier solution. A polymer solution having the drug is enabled to be dispersed into droplets with certain particle sizes and to be sprayed into a curing liquid through a method of high voltage electrostatic droplets, and thus the microsphere for the antituberculosis drug are prepared in the presence of calcium ions. The embolism sustained release agent can be used in the drug for treating pulmonary tuberculosis, pulmonary tuberculosis massive hemoptysis, cavitary pulmonary tuberculosis, renal tuberculosis, osteoarticular tuberculosis, genital tubercolosis, thyroid tuberculosis, tuberculosis of cervical lymph nodes, pericardial tuberculosis, chest-wall tuberculosis and other in-vivo tuberculosises.

Description

technical field [0001] The present invention relates to a triple compound microsphere blood vessel targeting embolization sustained-release agent containing anti-tuberculosis drugs and its preparation method and application, in particular to a microsphere blood vessel cross-linked with various anti-tuberculosis active ingredients using sodium alginate as a carrier The targeted embolism slow-release agent, its preparation method and its application in interventional embolization therapy and the like belong to the field of medical embolization equipment. Background technique [0002] Tuberculosis is one of the major infectious diseases that seriously endanger human life and health, and my country is one of the 22 countries with a high burden of tuberculosis in the world. , about 150,000 people die from tuberculosis every year. Although great progress has been made in the treatment and immune prevention of tuberculosis, tuberculosis is still one of the major diseases that my cou...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496A61K31/4409A61K31/4965A61K31/4709A61K9/02A61K47/36A61P31/06
Inventor 敖国昆李新建张光宇洪宏
Owner THE 309TH HOSPITAL OF CHINESE PEOPLES LIBERATION ARMY
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