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Anti-tuberculosis drug triple compound microsphere vascular targeted embolization sustained-release preparation and preparation method and use thereof

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

Active Publication Date: 2016-09-28
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

[0012] 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

[0061] Example 1 Preparation of anti-tuberculosis drug triple compound microsphere blood vessel targeted embolism slow-release agent:

[0062] 1. Reagent preparation:

[0063] 1. 10g / L (1% (W / V)) carrier solution:

[0064] 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;

[0065] 2. Drug solution:

[0066] ① Rifampicin solution:

[0067] 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;

[0068] ② Isoniazid solution:

[0069] Weigh 20 grams of isoniazid powder, add 50 ml of water for injection to dissolve, and obtain isoniazid solution;

[0070] ③Pyrazinamide (or moxifloxacin) solution:

[0071] Claim 40 grams of ...

Embodiment 2

[0102] Example 2: Preparation of anti-tuberculosis drug triple compound microsphere vascular targeted embolism slow release agent:

[0103] 1. Reagent preparation:

[0104] 1. 60g / L (6% (W / V)) carrier solution:

[0105] 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;

[0106] 2. Drug solution:

[0107] ① Rifampicin solution:

[0108] 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;

[0109] ② Isoniazid solution:

[0110] Weigh 20 grams of isoniazid powder, add 50 ml of water for injection to dissolve, and obtain isoniazid solution;

[0111] ③Pyrazinamide (or moxifloxacin) solution:

[0112] Claim 40 grams of pyraz...

Embodiment 3

[0143] Example 3: Preparation of anti-tuberculosis drug triple compound microsphere vascular targeted embolism slow release agent:

[0144] 1. Reagent preparation:

[0145] 1. 20g / L carrier solution:

[0146] 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;

[0147] 2. Drug solution:

[0148] ① Rifampicin solution:

[0149] 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;

[0150] ② Isoniazid solution:

[0151] Weigh 40 grams of isoniazid powder, add 100 ml of water for injection to dissolve, and obtain isoniazid solution;

[0152] ③Pyrazinamide (or moxifloxacin) solution:

[0153] Claim 80 grams of pyrazinamide (o...

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Abstract

The invention relates to a triple compound microsphere vascular targeted embolization sustained-release preparation containing an antituberculous drug as well as a preparation method and application of the preparation. The sustained-release agent comprises a carrier and drugs, wherein the drugs are coated with the carrier; the carrier is sodium alginate or chitosan, and the drugs are triple antituberculous compound drugs including rifampicin, isoniazid and pyrazinamide or moxifloxacin. The three antituberculous drugs are matrix drug solutions, the sodium alginate or chitosan is a carrier solution, the matrix drug solutions and the carrier solutiona are mixed to prepare a solution, the polymer solution containing drugs is dispersed into fogdrops with a certain diameter by adopting a high-voltage electrostatic droplet mode, and the fogdrops are sprayed into a solidifying liquid to prepare antituberculous drug microspheres under the action of calcium ions. The embolization sustained-release preparation can be used for treating tuberculosis, massive hemoptysis of pulmonary tuberculosis, tuberculosis cavity, renal tuberculosis, osteoarticular tuberculosis, genital tuberculosis, tuberculosis of thyroid gland, tuberculosis of cervical lymph nodes, tuberculosis of pericardium, tuberculosis of chest wall, pleural tuberculosis and other kinds of tuberculosis in a body.

Description

[0001] This application is an application number 201110053707.5, the application date is March 7, 2011, and the invention name is "anti-tuberculosis drug triple compound microsphere blood vessel targeted embolism slow-release agent and its preparation method and application" The divisional case of the invention patent application Apply. technical field [0002] 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 [0003] Tuberculosis is one of the major infectious diseases that s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496A61K9/16A61P31/06A61K31/4709A61K31/4409
CPCA61K9/0002A61K9/1652A61K31/4409A61K31/4709A61K31/496A61K2300/00
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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