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Excipient-free lyophilized paclitaxel powder preparation and preparation method thereof

A technology of paclitaxel and freeze-dried powder, applied in freeze-dried delivery, powder delivery, anti-tumor drugs and other directions, can solve the problems of large particle size and complicated process, and achieve the effects of simple formula, good solubility and high safety

Inactive Publication Date: 2015-04-15
POLYMERCHEM
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Jing Xiabin and others disclosed a preparation method of paclitaxel freeze-dried powder in "Freeze-dried powder injection of paclitaxel polymer bonded drug and its preparation method" (patent application No. 200610016614), but its process is more complicated and needs to add a large amount of stabilizers and co-solvents, and the above-mentioned paclitaxel freeze-dried powder has a larger particle size after reconstitution, which is 100-150nm

Method used

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  • Excipient-free lyophilized paclitaxel powder preparation and preparation method thereof
  • Excipient-free lyophilized paclitaxel powder preparation and preparation method thereof
  • Excipient-free lyophilized paclitaxel powder preparation and preparation method thereof

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Embodiment (1-7

[0041] A paclitaxel freeze-dried powder preparation without excipients is prepared through the following steps.

[0042]① Weigh raw materials according to different feeding ratios (paclitaxel: mPEG-PLA-lysine). Among them, the raw material paclitaxel (CAS33069-62-4) is produced by Xi'an Ruilin Biotechnology Co., Ltd., with a purity greater than 95%, and the raw material mPEG-PLA-lysine is produced by the inventor according to the process described in the patent number PCT-CN-2013000453 Self-prepared;

[0043] ②Put the above-mentioned raw materials into a container, and add organic solvents such as ethanol or acetonitrile at a temperature of 15-45°C until they are completely dissolved. The dissolving process can adopt means such as stirring or shaking.

[0044] ③ Rotate the above solution at 30-50°C for 2 hours until the organic solvent evaporates to dryness. Then vacuum drying at 10-40° C. for > 12 hours to remove residual organic solvents to obtain a paclitaxel-containing ...

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Abstract

The invention belongs to the technical field of medicinal preparations, and relates to an excipient-free lyophilized paclitaxel powder preparation and a preparation method thereof. The lyophilized paclitaxel powder does not contain excipients, adopts paclitaxel as a medicinal effective component, and adopts mPEG- PLA-lysine as a matrix. The preparation method is simple; the excipient-free lyophilized paclitaxel powder preparation adopts mPEG-PLA-lysine with low cytotoxicityas as a carrier, and other auxiliary components are not needed, so the preparation has simple formula and high safety; the excipient-free lyophilized paclitaxel powder preparation has good solubility in water, can be rapidly re-dissolved in water, and has a highest concentration reaching 10mg / ml; and the re-dissolved lyophilized paclitaxel powder preparation has small average particle size, and easily performs an ERP effect.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a paclitaxel freeze-dried powder preparation without excipients and a preparation method thereof. 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, the molecular structure is shown in the figure below. [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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K9/19A61K31/337A61P35/00
Inventor 顾晓军滕鑫
Owner POLYMERCHEM
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