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

A vascular targeting and anti-tuberculosis technology, used in antibacterial drugs, suppository delivery, pharmaceutical formulations, etc., can solve problems such as the inability of relatively uniform sustained release of drugs, inability to relatively uniform sustained release, tissue necrosis or damage, etc. The effect of prolonging the action time of the drug, reducing the toxicity and easy operation

Active Publication Date: 2012-09-19
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 vascular targeted embolization 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, and dissolve it in normal saline or water for injection at a concentration ratio of 10 g / L to obtain a carrier solution, namely sodium alginate or chitosan solution;

[0064] 2. Drug solution:

[0065] ①Rifampicin solution:

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

[0067] ②Isoniazid solution:

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

[0069] ③Pyrazinamide (or moxifloxacin) solution:

[0070] Weigh 40 ...

Embodiment 2

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

[0102] 1. Reagent preparation:

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

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

[0105] 2. Drug solution:

[0106] ①Rifampicin solution:

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

[0108] ②Isoniazid solution:

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

[0110] ③Pyrazinamide (or moxifloxacin) solution:

[0111] Weig...

Embodiment 3

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

[0143] 1. Reagent preparation:

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

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

[0146] 2. Drug solution:

[0147] ①Rifampicin solution:

[0148] Weigh 20 grams of rifampicin powder into a mortar and add 40ml of water for injection to grind and dissolve, then wash the mortar with 60ml of water for injection, and then ultrasonicate for 10 minutes after mixing to obtain a rifampicin solution;

[0149] ②Isoniazid solution:

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

[0151] ③Pyrazinamide (or moxifloxacin) solution:

[0152] 80 grams of pyrazi...

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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 invention relates to a triple compound microsphere vascular targeted embolization slow-release agent containing anti-tuberculosis drugs and a preparation method and application thereof, in particular to a microsphere vascular cross-linked with various anti-tuberculosis active ingredients using sodium alginate as a carrier The invention relates to a targeted embolization sustained-release agent, a preparation method thereof, and applications in interventional embolization therapy and the like, belonging to the field of medical embolization devices. 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. The number of tuberculosis patients ranks second in the world, and the existing pulmonary tuberculosis patients account for 1 / 4 of the total number of patients in the world. , about 150,00...

Claims

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Application Information

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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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