Paclitaxel micelle preparation
A paclitaxel and micelle technology, applied in the field of paclitaxel micelle preparations, can solve the problems of increased difficulty in large-scale industrialization, complicated process conditions, etc., and achieve the effects of high safety, high blood stability and small particle size
Inactive Publication Date: 2015-04-15
POLYMERCHEM
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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.
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[0029] A paclitaxel micelle preparation can be obtained by a direct dissolution method, a dialysis method or a film hydration method. Preferably, the present invention is obtained by using a thin film hydration method, which includes the following steps.
[0030] 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 (CAS33069-62-4) is produced by Xi'an Ruilin Biotechnology Co., Ltd., with a purity greater than 95%. preparation;
[0031] 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.
[0032] ③The mixed membrane was placed in a water bath at 40-60°C until it became transparen...
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Abstract
The invention belongs to the technical filed of medicinal preparations, and concretely relates to a paclitaxel micelle preparation. The paclitaxel micelle preparation adopts mPEG-PLA-glutamic acid (methoxypolyethylene glycol-polylactide-glutamic acid) triblock copolymer as a micelle carrier. The average particle size of paclitaxel micelles is 21-41nm. The paclitaxel micelle preparation is prepared through a direct dissolution method, a dialysis method or a film hydration method. The mPEG-PLA-glutamic acid triblock copolymer with low toxicity is adopted as a micelle carrier, and no other auxiliary materials are needed in the micelle preparation, so the safety is high; the paclitaxel micelle preparation has high in vitro stability, the stable time of the paclitaxel micelles at room temperature exceeds 12h, and the stable time at a low temperature exceeds 168h; and the paclitaxel micelle preparation has the advantages of high blood stability, small particle size, and easy performance of the ERP effect.
Description
technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a paclitaxel micelle preparation. 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 assemble into microtubule dimers, there...
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IPC IPC(8): A61K9/10A61K47/34A61K31/337A61P35/00
Inventor 顾晓军滕鑫
Owner POLYMERCHEM