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Amphiphilic polymelphalan prodrug micelle and preparation method thereof

A melphalan and amphiphilic technology, which is applied in the field of amphiphilic polymelphalan prodrug micelles and its preparation, can solve the problems of high toxicity and side effects, and achieve low cost, controllable structure, and easy industrialization The effect of production

Active Publication Date: 2020-11-13
CHANGZHI MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, melphalan is highly toxic, especially systemic administration can easily cause a variety of toxic and side effects

Method used

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  • Amphiphilic polymelphalan prodrug micelle and preparation method thereof
  • Amphiphilic polymelphalan prodrug micelle and preparation method thereof
  • Amphiphilic polymelphalan prodrug micelle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] A preparation method of amphiphilic polymelphalan prodrug micelles, comprising the following steps:

[0031] Put 1mmol antineoplastic drug melphalan and 0.05mmol aminopolyethylene glycol monomethyl ether (molecular weight 2000) in a round bottom flask, add DCC and HOBT in equimolar ratio with melphalan, that is, melphalan and DCC , The mol ratio of HOBT is 1:1:1; Add anhydrous DMF and molecular sieve afterwards, the mass ratio of melphalan and anhydrous DMF is 1:40;

[0032] After two days of reaction in anhydrous and oxygen-free room temperature, the reaction solution was transferred to a dialysis bag. After three days of dialysis with DMF, DMF was changed three times during the period, and the dialysis was continued in pure water for two days, and the pure water was changed several times during the period.

[0033] After dialysis, freeze-dry to obtain amphiphilic polymelphalan prodrug micelles.

Embodiment 2

[0035] A preparation method of amphiphilic polymelphalan prodrug micelles, comprising the following steps:

[0036] Put 1mmol antineoplastic drug melphalan and 0.02mmol aminopolyethylene glycol monomethyl ether (molecular weight 2000) in a round bottom flask, add DCC and HOBT in equimolar ratio with melphalan, that is, melphalan and DCC , The mol ratio of HOBT is 1:1:1; Add anhydrous DMF and molecular sieve afterwards, the mass ratio of melphalan and anhydrous DMF is 1:50;

[0037] After two days of reaction in anhydrous and oxygen-free room temperature, the reaction solution was transferred to a dialysis bag. After three days of dialysis with DMF, DMF was changed three times during the period, and the dialysis was continued in pure water for two days, and the pure water was changed several times during the period.

[0038] After dialysis, freeze-dry to obtain amphiphilic polymelphalan prodrug micelles.

Embodiment 3

[0040] A preparation method of amphiphilic polymelphalan prodrug micelles, comprising the following steps:

[0041] Put 1mmol antineoplastic drug melphalan and 0.1mmol aminopolyethylene glycol monomethyl ether (molecular weight 2000) in a round bottom flask, add DCC and HOBT in equimolar ratio with melphalan, that is, melphalan and DCC , The mol ratio of HOBT is 1:1:1; Add anhydrous DMF and molecular sieve afterwards, the mass ratio of melphalan and anhydrous DMF is 1:30;

[0042] After two days of reaction in anhydrous and oxygen-free room temperature, the reaction solution was transferred to a dialysis bag. After three days of dialysis with DMF, DMF was changed three times during the period, and the dialysis was continued in pure water for two days, and the pure water was changed several times during the period.

[0043] After dialysis, freeze-dry to obtain amphiphilic polymelphalan prodrug micelles.

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Abstract

The invention provides an amphiphilic polymelphalan prodrug micelle and a preparation method thereof, and belongs to the technical field of preparation of pharmaceutical preparation. The method comprises the following steps: using melphalan and a polymer end-capping reagent as raw materials and DCC / HOBT or DCC / DMAP as a condensing agent, mixing, adding anhydrous DMF and a molecular sieve, and reacting at room temperature for 2 days under anhydrous and anaerobic conditions to obtain a reaction solution; dialyzing, purifying and freeze-drying the reaction solution to obtain an amphiphilic polymelphalan prodrug micelle, wherein the molar ratio of the melphalan to the polymer end-capping reagent is (10-50): 1, the molar ratio of the melphalan to the DCC to the HOBT is 1: 1: 1, or the molar ratio of the melphalan to the DCC to the DMAP is 1: 1: 0.2. The polymelphalan prodrug micelle capable of accurately regulating and controlling the drug loading rate is constructed by adopting a one-stepmethod, the operation is simple, the reaction temperature is relatively low, the cost is low, the structure is controllable, and the polymelphalan prodrug micelle is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of preparation of pharmaceutical preparations, and in particular relates to an amphiphilic polymelphalan prodrug micelle and a preparation method thereof. Background technique [0002] In today's rapid economic development, cancer is still one of the important diseases that seriously threaten human life and health. In the process of cancer treatment, rational drug use is required to avoid poisoning caused by excessively high blood drug concentration, or too low blood drug concentration has no therapeutic effect, resulting in slow and controlled release preparations, which is also the initial development stage of DDS. [0003] At present, the research purpose of drug delivery system (DDS) is to achieve the best therapeutic effect with the smallest dose with the appropriate dosage form and administration method. By increasing the drug loading rate, changing the distribution of chemotherapy drugs in vivo, and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/333A61K9/107A61K31/198A61K47/60A61P35/00
CPCC08G65/33396A61K31/198A61K9/1075A61K47/60A61P35/00Y02P20/55
Inventor 段晓郑金平苗聪秀张鑫宇吴钧宋丽华杨雪李常风
Owner CHANGZHI MEDICAL COLLEGE
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