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Docetaxel polymer micelle freeze-dried preparation and special solvent composition

A technology of docetaxel and polymer glue, applied in the field of medicine and chemical industry, can solve the problems of short validity period, difficult application and increased substance content of drugs, and achieve the effect of solving the problem of chemical stability and physical stability.

Active Publication Date: 2016-02-03
XINAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the contriver finds in further research, although above-mentioned method can improve the physical stability of docetaxel polymer micelle to a certain extent, but this arginine-docetaxel polymer micelle is accelerating (temperature 25 ±2°C) and long-term (6±2°C) stability studies, the content of related substances increased rapidly, resulting in a drug with a short validity period and difficult to be used in clinical practice
Therefore, it is necessary to study a docetaxel polymer micelle system that can solve both the physical stability of the docetaxel polymer micelle and the chemical stability of the docetaxel polymer micelle during long-term storage. Stability issues

Method used

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  • Docetaxel polymer micelle freeze-dried preparation and special solvent composition
  • Docetaxel polymer micelle freeze-dried preparation and special solvent composition
  • Docetaxel polymer micelle freeze-dried preparation and special solvent composition

Examples

Experimental program
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Effect test

Embodiment 1

[0019] Embodiment 1, the preparation of docetaxel polymer micelle freeze-dried preparation

[0020] Weigh 5g polyethylene glycol monomethyl ether-polylactic acid amphiphilic block copolymer (mPEG and PDLLA mass ratio is 40:60) and dissolve it in an appropriate amount of acetonitrile to obtain mPEG-PDLLA acetonitrile solution, and take another 1g docetaxel Docetaxel acetonitrile solution was prepared by dissolving in appropriate amount of acetonitrile, mPEG-PDLLA acetonitrile solution was mixed with docetaxel acetonitrile solution, acetonitrile was removed by rotary evaporation, so that docetaxel and mPEG-PDLLA formed a polymer gel, Then add 100 ml of water for injection, rotate to hydrate to form a polymer micelle solution, add a freeze-drying protective agent, add water to make up the volume, filter with a 0.22 μm microporous membrane, and freeze the filtrate to prepare docetaxel polymer glue Bundle of lyophilized preparations (1:5 mass ratio of docetaxel to mPEG-PDLLA).

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Embodiment 2

[0022] Embodiment 2, the preparation of docetaxel polymer micelle freeze-dried preparation

[0023] Weigh 5g of polyethylene glycol monomethyl ether-polylactic acid amphiphilic block copolymer (mPEG and PDLLA mass ratio of 50:50) and dissolve it in an appropriate amount of acetonitrile to obtain mPEG-PDLLA acetonitrile solution, and take another 1g of docetaxel Docetaxel acetonitrile solution was prepared by dissolving in appropriate amount of acetonitrile, mPEG-PDLLA acetonitrile solution was mixed with docetaxel acetonitrile solution, acetonitrile was removed by rotary evaporation, so that docetaxel and mPEG-PDLLA formed a polymer gel, Then add 100 ml of water for injection, rotate to hydrate to form a polymer micelle solution, add a freeze-drying protective agent, add water to make up the volume, filter with a 0.22 μm microporous membrane, and freeze the filtrate to prepare docetaxel polymer glue Bundle of lyophilized preparations (1:5 mass ratio of docetaxel to mPEG-PDLLA)...

Embodiment 3

[0025] Embodiment 3, the preparation of special solvent of docetaxel polymer micelle freeze-dried preparation - arginine aqueous solution

[0026] Dissolve 4g of arginine in 1000ml of water for injection, add 0.2g of activated carbon, make up to 2000ml with water, mix well, let stand for 20 minutes, first filter with a microporous membrane with a pore size of 0.45 μm, and then use a microporous filter with a pore size of 0.22 μm. The microporous membrane filter, the filtrate is divided into vials, plugged, capped, light inspection, packaging, namely the special solvent for docetaxel polymer micelle freeze-dried preparation - arginine aqueous solution.

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Abstract

The invention discloses a docetaxel polymer micelle freeze-dried preparation and special solvent composition. A docetaxel polymer micelle freeze-dried preparation comprises docetaxel, methoxy poly(ethylene glyeol)-poly(lactic acid) amphipathic block copolymer and freeze-drying protective additives, and a special solvent is an arginine aqueous solution. A clinical application mode of the composition includes that the special solvent is injected into the docetaxel polymer micelle freeze-dried preparation before use, and after redissolving, a stable polymer micelle solution is formed for use. The composition is capable of solving not only the problem of physical stability in redissolving of the docetaxel polymer micelle freeze-dried preparation but also the problem of chemical stability during long-term storage of the docetaxel polymer micelle freeze-dried preparation.

Description

technical field [0001] The invention belongs to the technical field of medicine and chemical industry, and relates to a composition composed of a polymer micelle freeze-dried preparation and its special solvent. Background technique [0002] Polymer micelles are drug-carrying systems developed in recent years for poorly soluble drugs. They have a core-shell structure, in which the core is a hydrophobic part and the shell is a hydrophilic part. The purpose of solubilization of poorly soluble drugs. Compared with commonly used solubilizers and cosolvents such as Tween 80, polyoxyethylene castor oil, etc., because the polymers used are all biodegradable materials, the safety is greatly improved. However, the stability of the existing drug-loaded polymer micelles is poor, and the drug is easily leaked from the polymer micelles, which affects the popularization and application of drug-loaded polymer micelles. [0003] Chinese patent application CN101972480A discloses a docetaxe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/337A61K47/34A61P35/00
Inventor 蒲道俊冯燕丽邹意琼余春梅陈兰杨秀丽李慧慧郑小锋
Owner XINAN PHARMA
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