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Rifapentine sustained-released microspheres and preparation method thereof

A technology of rifapentine and sustained-release microspheres, which can be applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. problem, to achieve the effect of good local curative effect, high drug loading, and strong effect

Active Publication Date: 2012-11-28
THE FIRST TEACHING HOSPITAL OF XINJIANG MEDICAL UNIVERCITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The products currently on the market are oral capsule preparations, which are widely distributed in the body after oral administration. Long-term use may cause liver function damage and bone marrow suppression in varying degrees, increasing the pain and economic burden of patients. Therefore, it cannot meet the current experimental requirements. needs and clinical applications

Method used

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  • Rifapentine sustained-released microspheres and preparation method thereof
  • Rifapentine sustained-released microspheres and preparation method thereof
  • Rifapentine sustained-released microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1, the preparation method of the rifapentine sustained-release microspheres is carried out according to the following steps: the first step, respectively weigh 0.108 g of rifapentine and 0.104 g of polylactic acid with a molecular weight of 10,000 to 50,000, and weigh Dissolve an appropriate amount of gelatin in heated distilled water to prepare a gelatin aqueous solution with a mass concentration of 0.5%. Dissolve polylactic acid in an organic solvent, that is, dichloromethane or trichloromethane. After dissolving in the solution of chloroform, this solution is used as the oil phase, and rifapentine is dissolved in the oil phase to form a colostrum solution; in the second step, the colostrum solution is first ultrasonically homogenized, and the ultrasonically homogenized The colostrum solution is added to the gelatin aqueous solution with a mass concentration of 0.5% to 1.5% under the stirring condition of 1300r / min to 1600r / min, and then emulsified to form a do...

Embodiment 2

[0025] Example 2, the preparation method of the rifapentine sustained-release microspheres is carried out according to the following steps: the first step, respectively weigh 0.103 g of rifapentine and 0.203 g of polylactic acid with a molecular weight of 10000 or 50000, and weigh Dissolve an appropriate amount of gelatin in heated distilled water to prepare a gelatin aqueous solution with a mass concentration of 0.5%. Dissolve polylactic acid in an organic solvent, that is, dichloromethane or trichloromethane. After dissolving in the solution of chloroform, this solution is used as the oil phase, and rifapentine is dissolved in the oil phase to form a colostrum solution; in the second step, the colostrum solution is first ultrasonically homogenized, and the ultrasonically homogenized The colostrum solution is added to the gelatin aqueous solution with a mass concentration of 0.5% or 1.5% under the stirring condition of 1300r / min or 1600r / min, and then emulsified to form a doub...

Embodiment 3

[0026] Example 3, the preparation method of the rifapentine sustained-release microspheres is carried out according to the following steps: the first step, respectively weigh 0.109 g of rifapentine and 0.307 g of polylactic acid with a molecular weight of 30000, and weigh an appropriate amount of gelatin Soluble in heated distilled water, and prepare a gelatin aqueous solution with a mass concentration of 0.5%. Dissolve polylactic acid in an organic solvent, that is, dichloromethane or chloroform, and wait for the polylactic acid to dissolve in an organic solvent, that is, dichloromethane or trichloromethane. After dissolving in the methane solution, the solution is used as the oil phase, and rifapentine is dissolved in the oil phase to form a colostrum solution; in the second step, the colostrum solution is ultrasonically homogenized, and the ultrasonically homogenized colostrum The solution is added to the gelatin aqueous solution with a mass concentration of 0.5% or 1.5% und...

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Abstract

The invention, relating to both the technical field of biology and medicine, discloses rifapentine sustained-released microspheres and a preparation method thereof. The rifapentine sustained-released microspheres disclosed herein have high drug loading capacity, good entrapment efficiency, and good sustained action by in vitro release test. The rifapentine sustained-released microspheres disclosed herein can be directly implanted into tuberculosis local focus to conduct regional continuous chemotherapy to let the tuberculosis focus position have large drug amount, high drug concentration, long duration, large effect, good local curative effect, little amount of the drug distributed to the whole body, and low plasma concentration, thus the curative effect is raised, and the effect of adverse reaction is significantly reduced, so that good treatment of patients (severe liver and kidney dysfunction, combination of a plurality of systemic diseases, severe malnutrition) who can not endure anti-tuberculosis chemotherapy can be achieved. The preparation method of the rifapentine sustained-released microspheres has the advantages of low cost, simple operation, and convenient, simple and repeatable method, and can generate huge economic benefits.

Description

technical field [0001] The invention not only relates to the field of biotechnology, but also belongs to the field of medicine technology, and relates to a rifapentine sustained-release microsphere and a preparation method thereof. Background technique [0002] Rifapentine (Rifapentine, RFT) is a new semi-synthetic rifamycin antibiotic, which is a cyclopentyl derivative of rifampicin. In 1998, the drug was approved by the US FDA for the treatment of tuberculosis. 47 h 64 N 4 o 12 , the molecular weight is 877.0429, and the structural formula is as follows: [0003] [0004] Because rifapentine has good fat solubility, it is almost insoluble in water, the plasma protein binding rate is 88% to 99%, and the half-life is 10-15h. Rifapentine has a broad-spectrum antibacterial effect, and can kill or inhibit microorganisms such as Mycobacterium tuberculosis, Bacillus leprae, certain viruses, Staphylococcus aureus and other Gram-positive bacteria and some Gram-negative bacte...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/496A61K47/34A61P31/06
Inventor 宋兴华罗兰折胜利温浩王建华丁俐文古丽再努尔·吐尔逊吕顺忠
Owner THE FIRST TEACHING HOSPITAL OF XINJIANG MEDICAL UNIVERCITY
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