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Nimustine brain slow release implantation agent and its preparation method

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

Inactive Publication Date: 2006-11-15
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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 1 g of PLGAO 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) Colostrum was cooled to 18° C. in an ice-water bath, then added to 40 ml of 4% polyvinyl alcohol 178 g aqueous solution, stirred at 8000 rpm ...

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 nimustine brain slow-release implant, consisting of nimustine and poly(lactic-co-glycolic acid) (PLGA), the weight ratio of nimustine to PLGA is 1:100 to 40:100, Nimustine sustained-release microspheres were prepared by double emulsification-solvent evaporation method, and the sustained-release microspheres were pressed into tablets, and sterilized to obtain nimustine brain sustained-release implants, which were locally implanted through the lesion to exert their full potential. The long-term and efficient inhibition of glioma solves the shortcomings and deficiencies of traditional systemic chemotherapy drugs such as difficulty in passing through the blood-brain barrier, low local concentration of drugs, severe systemic reactions, and short-term effect on tumors that affect curative effect. It avoids the blood-brain barrier The barrier directly increases the local drug concentration, prolongs the action time of chemotherapy drugs, and reduces the systemic side effects of drugs. It is used for the treatment of malignant glioma and other brain tumors.

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 Patents(China)
IPC IPC(8): A61K31/506A61K9/22A61P35/00
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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