Taxol micelle preparation technology and product

A preparation process, the technology of paclitaxel, which is applied in the direction of drug combination, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of complicated process conditions and increased difficulty of large-scale industrialization, and achieve simple preparation process , good particle stability, and high blood stability

Pending Publication Date: 2019-09-06
POLYMERCHEM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Another disadvantage of the existing paclitaxel micelles is that the process conditions are more complicated, which increases the difficulty for large-scale industrialization
Some paclitaxel micelles contain a certain amount of ethanol, which still has certain cytotoxicity.

Method used

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  • Taxol micelle preparation technology and product
  • Taxol micelle preparation technology and product
  • Taxol micelle preparation technology and product

Examples

Experimental program
Comparison scheme
Effect test

Embodiment (1-7

[0025] A preparation process of paclitaxel micelle preparation adopts film hydration method, which includes the following steps.

[0026] ① Weigh the raw materials according to the different feeding ratios of paclitaxel and mPEG-PLA-glutamic acid (see Table 1). Among them, the raw material paclitaxel (CAS 33069-62-4) is produced by Xi'an Ruilin Biotechnology Co., Ltd., with a purity greater than 95%, mPEG-PLA-glutamic acid, and the process described in the patent number PCT-CN-2013000453 by the inventor self-preparation;

[0027] ② Put the above raw materials into the container, add organic solvents such as ethanol or acetonitrile until completely dissolved. Rotary evaporation at 30-50°C for 2h until the organic solvent evaporated to dryness, and vacuum drying at 10-60°C for >12h to remove residual organic solvent to obtain a polymer mixed film containing paclitaxel.

[0028] ③The mixed membrane was placed in a water bath at 40-60°C until it became transparent, then added ul...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a taxol micelle preparation technology and a product. The taxol micelle preparation technologyis simple in path and low in production cost. A prepared taxol micelle is high in stability in vitro and kept stable for over 12 hours at room temperature, and meets the requirements of drug treatment. Blood stability is high, particle sizes are small, and EPR (enhanced permeability and retention) effects are more easily exerted.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a paclitaxel micelle preparation process and product. Background technique [0002] The molecular formula of paclitaxel is: C 47 h 51 NO 14 , molecular weight 853.9, melting point 213-216 ℃, highly lipophilic, insoluble in water, is the first to be isolated from Taxus genus as a natural anticancer drug with high efficiency, low toxicity and broad spectrum. It is a complex natural secondary metabolite in Taxus plants, and its molecular structure is shown in the following formula. [0003] [0004] Paclitaxel is a microtubule-specific drug with high anti-cancer activity. Its sales volume ranks first among new anti-tumor drugs all the year round, and is increasing at a rate of 20%. [0005] In 1977, Horwit Z discovered that the anti-cancer mechanism of paclitaxel lies in its ability to bind to tubulin, promote tubulin polymerization and assembl...

Claims

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Application Information

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Patent Type & AuthorityApplications(China)
IPC IPC(8): A61K9/107A61K47/34A61K31/337A61K36/13A61P35/00
Inventor顾晓军滕鑫
OwnerPOLYMERCHEM