Excipient-free lyophilized paclitaxel powder preparation and preparation method thereof
A technology of paclitaxel and freeze-dried powder, which is applied in the direction of freeze-dried delivery, powder delivery, antineoplastic drugs, etc. It can solve the problems of complex process and large particle size, and achieve the effect of good solubility, simple formula and high safety
Inactive Publication Date: 2015-04-15
POLYMERCHEM
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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
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[0042] A paclitaxel freeze-dried powder preparation without excipients is prepared through the following process.
[0043]① Weigh raw materials according to different feeding ratios (paclitaxel: mPEG-PLA-aspartic acid). 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-aspartic acid is produced by the inventor according to the process described in the patent number PCT-CN-2013000453 self-preparation;
[0044] 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.
[0045] 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 pac...
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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-aspartic acid as a matrix. The preparation method is simple; the excipient-free lyophilized paclitaxel powder preparation adopts mPEG-PLA-aspartic acid 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, and can be rapidly re-dissolved in water; 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, in particular to a paclitaxel freeze-dried powder preparation without excipients and a preparation method thereof. Background technique [0002] The molecular formula of paclitaxel is: C47H51NO14, the molecular weight is 853.9, and the melting point is 213-216°C. It is highly lipophilic and insoluble in water. It is a highly efficient, low-toxic and broad-spectrum natural anticancer drug isolated from Taxus genus first. . It is a complex natural secondary metabolite in the Taxus genus, the molecular structure is shown 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 tubulin polymeriza...
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Login to View More IPC IPC(8): A61K9/19A61K31/337A61K47/34A61P35/00
Inventor 顾晓军滕鑫
Owner POLYMERCHEM