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Excipient-containing 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 large particle size and complicated process, and achieve the effect 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-containing lyophilized paclitaxel powder preparation and preparation method thereof
  • Excipient-containing lyophilized paclitaxel powder preparation and preparation method thereof
  • Excipient-containing lyophilized paclitaxel powder preparation and preparation method thereof

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Embodiment (1-7

[0037] A paclitaxel freeze-dried powder preparation containing excipients is prepared according to the following process steps.

[0038] 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 prepared by the inventor according to the patent No. PCT-CN-2013000453 Self-preparation process;

[0039] 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.

[0040] 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 paclitax...

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Abstract

The invention belongs to the technical field of medicinal preparations, and relates to an excipient-containing lyophilized paclitaxel powder preparation and a preparation method thereof. The preparation adopts paclitaxel as a medicinal effective component, adopts mPEG-PLA-aspartic acid as a matrix, and contains an excipient; and the excipient comprises one or more of lactose, mannitol, dextran, glycine and glucose. The preparation method comprises the following steps: 1, mixing mPEG-PLA-aspartic acid with paclitaxel; 2, fully dissolving the above obtained mixture in an organic solvent; 3, removing the organic solvent; 4, adding water, and hydrating to form a micelle solution; and 5, adding the excipient accounting for 5% or less of the total weight of materials added in step 1 to the medicine-loaded micelle solution, fully dissolving the excipient, lyophilizing the above obtained mixed micelle solution through a routine lyophilizing technology to prepare the excipient-containing lyophilized paclitaxel powder preparation. The excipient-containing lyophilized paclitaxel powder preparation has the advantages of simple preparation method, simple formula, high safety, good dissolution, rapid re-dissolving in water, and realization of small average particle size and easy performance of the ERP effect after the re-dissolving.

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 and a preparation method. 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 tubulin polymerization and...

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 顾晓军滕鑫
Owner POLYMERCHEM
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