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Taxol freeze-dried powder preparation containing excipient and preparation method of taxol freeze-dried powder preparation

A technology of paclitaxel and freeze-dried powder, which is applied in the direction of freeze-dried transportation and powder transportation, which can solve the problems of large particle size and complicated process, and achieve the effect of simple formula, simple preparation process and low cytotoxicity

Inactive Publication Date: 2015-04-29
POLYMERCHEM
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  • Summary
  • 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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  • Taxol freeze-dried powder preparation containing excipient and preparation method of taxol freeze-dried powder preparation
  • Taxol freeze-dried powder preparation containing excipient and preparation method of taxol freeze-dried powder preparation
  • Taxol freeze-dried powder preparation containing excipient and preparation method of taxol freeze-dried powder preparation

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Embodiment (1-7

[0037] A paclitaxel freeze-dried powder preparation containing excipients is prepared by the following method.

[0038] 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-preparation;

[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 >12h to remove residual organic solvents to obtain a paclitaxel-containing polym...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a taxol freeze-dried powder preparation containing an excipient and a preparation method of the taxol freeze-dried powder preparation. The preparation takes taxol as a medicinal active ingredient and mPEG-PLA-lysine as a matrix and contains the excipient; and the excipient is selected from one or more of lactose, mannitol, dextran, glycine and glucose. The preparation method comprises the following steps: (1) mixing mPEG-PLA-lysine with taxol; (2) fully dissolving the mixture by using an organic solvent; (3) removing the organic solvent; (4) adding water for hydration to form a micellar liquid; and (5) adding the excipient of which the weight is not more than 5% of the total weight of the fed materials in the step (1) into the drug-loaded micellar liquid, dissolving the excipient fully, and then performing freeze-drying on the mixed micellar liquid according to a conventional freeze-drying process, thereby obtaining the taxol freeze-dried powder preparation. The preparation method provided by the invention is simple; the formula is simple, and the safety is high; and the freeze-dried powder preparation is good in solubility, can be re-dissolved quickly in water, has a relatively small average particle size after re-dissolution, and can give play to an ERP effect more easily.

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 containing 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, 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 tubu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K47/34A61K31/337A61K47/26A61K47/18A61K47/36
Inventor 顾晓军滕鑫
Owner POLYMERCHEM
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