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Nimustine brain slow release implantation agent and its preparation method

A sustained-release implant, nimustine technology, applied in pharmaceutical formulations, medical preparations containing active ingredients, drug delivery, etc., can solve bone marrow suppression, liver and kidney function poisoning, gastrointestinal reactions, and cross-drug resistance And other issues

Inactive Publication Date: 2005-10-26
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these drugs will cause bone marrow suppression, toxicity to liver and kidney functions, and strong gastrointestinal reactions, and there is also cross-resistance between them.

Method used

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  • Nimustine brain slow release implantation agent and its preparation method
  • Nimustine brain slow release implantation agent and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] The weight ratio of nimustine to PLGA is 20:100.

[0035] The sustained-release polymer was a mixture of 60% PLGA (75:25) and dichloromethane solution.

[0036] Preparation steps:

[0037] Using W / O / W double emulsification-solvent evaporation method

[0038] (1) Accurately weigh 20 mg of nimustine into a 1.5 ml plastic centrifuge tube, add 20 μl of 16% gelatin aqueous solution, heat in a water bath at 60° C. to dissolve the drug completely, and serve as the inner water phase.

[0039] (2) Precisely weigh 0.1 g of PLGA and place it in a 1.5 ml plastic centrifuge tube, add 167 μl of dichloromethane to completely dissolve PLGA, and use it as the oil phase.

[0040](3) Add the oil phase to the inner water phase with a pipette gun, vortex mix, heat in a water bath at 60°C, and ultrasonically emulsify to obtain colostrum.

[0041] (4) Cool the colostrum to 18° C. in an ice-water bath, then add it to 40 ml of 4% polyvinyl alcohol 1788 aqueous solution, stir at 8000 rpm for ...

Embodiment 2

[0045] The weight ratio of nimustine to PLGA is 2:100, and the sustained-release polymer is a mixture of 5% PLGA (75:25) and dichloromethane solution. The preparation steps were as in Example 1, and the nimustine brain sustained-release implant was prepared.

Embodiment 3

[0047] The weight ratio of nimustine to PLGA is 5:100, and the slow-release polymer is a mixture of 10% PLGA (75:25) and dichloromethane solution. The preparation steps were as in Example 1, and the nimustine brain sustained-release implant was prepared.

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Abstract

A slow-releasing cerebral implant of nimustine for treating the cerebral malignant glioma and other cerebromas is prepared from nimustine and polylactate-hydroxyacetate copolymer (PLGA) through preparing slow-releasing microspheres, tabletting and sterilizing.

Description

technical field [0001] The invention relates to a novel pharmaceutical dosage form, in particular to a nimustine brain sustained-release implant for treating malignant glioma and a preparation method thereof. Background technique [0002] Malignant brain tumors are one of the leading causes of death from cancer. Gliomas, which account for half of primary brain tumors, are one of the most challenging types of brain tumors. In the past 30 years, the treatment effect of malignant glioma has not been significantly improved. Due to its infiltrative growth and unclear boundary with normal brain tissue, it is impossible to completely remove it by surgery, and recurrence often occurs after surgery. According to the American Brain Tumor Joint Research According to the statistics of the group, the median survival period (MTS) of malignant glioma treated with surgery alone is only 14 weeks, while the average survival period with radiotherapy after surgery is no more than one year. Th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506
Inventor 张翮高申陈建明邹豪管斐李国栋丁雪鹰俞媛
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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