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Medicinal composition of paclitaxel

A composition and technology of paclitaxel, which are applied in the directions of drug combination, anti-tumor drug, powder delivery, etc., can solve the problems of large particle size and complicated process of paclitaxel freeze-dried powder, and achieve the advantages of avoiding adverse reactions, simple preparation process and blood stability. high effect

Inactive Publication Date: 2015-04-15
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 preparation method thereof" (patent application number 200610016614), and its process is more complicated and needs to add a large amount of Stabilizer and co-solvent, and the obtained paclitaxel freeze-dried powder has a larger particle size after reconstitution, which is 100-150nm

Method used

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  • Medicinal composition of paclitaxel
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  • Medicinal composition of paclitaxel

Examples

Experimental program
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Effect test

Embodiment (1-7

[0032] A pharmaceutical composition of paclitaxel, which is a medicament composed of the following components by weight:

[0033] Paclitaxel 2.87~27.66 parts,

[0034] mPEG-PLA-Phenylalanine 100 parts.

[0035] The preparation method of composition among the present invention comprises the following steps:

[0036]① Weigh raw materials (paclitaxel, mPEG-PLA-phenylalanine) according to different feeding ratios. Among them, paclitaxel (CAS33069-62-4) is produced by Xi'an Ruilin Biotechnology Co., Ltd., with a purity greater than 95%. preparation;

[0037] 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.

[0038] 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 org...

Embodiment 8

[0057] Example 8 Tumor Inhibition Experiment

[0058] Using normal saline, taxol (commercially available paclitaxel injection) and the paclitaxel micelle solution obtained in Example 3, the inhibition test of human MCF-7 breast cancer xenograft tumor was carried out on nude mice. The route of administration is intravenous administration, administered once every three days, and the concentration of taxol and paclitaxel of the present invention is 20mg / kg equally. The tumor volume of nude mice was measured every day, and the results were as follows: figure 1 shown. The results show that: the tumor volume of the nude mice instilled with normal saline increases rapidly; the growth rate of the tumor volume of the nude mice instilled with Taxol is controlled to a certain extent, but the tumor volume still increases; the tumor volume of the nude mice instilled with the present invention is controlled and gradually decreases. Small. It is proved that the present invention has remar...

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Abstract

The invention belongs to the technical field of medicinal preparations, and concretely relates to a medicinal composition of paclitaxel. The medicinal composition comprises, by weight, 2.87-27.66 parts of paclitaxel and 100 parts of mPEG-PLA-phenylalanine. The medicinal composition has the following advantages: 1, the in vitro stability is high, and a re-dissolved paclitaxel solution keeps stable at room temperature for above 12h to meet medicinal treatment requirements; 2, the medicinal composition has high stability in blood and small particle size, and can easily perform the ERP effect; 3, a novel micelle carrier is adopted, so the toxicity is low, and the safety is high; and 4, a pharmacy common freeze-drying technology is directly adopted to prepare freeze-dried powder, so the medicinal composition is simple to prepare, and is convenient to transport and store, and untoward effects brought by the addition of an excipient are avoided The medicinal composition can be instantly re-dissolved by using common normal saline or glucose injection, so the administration process is greatly simplified.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a pharmaceutical composition and preparation containing paclitaxel. 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 a highly efficient, low toxicity, broad-spectrum natural anticancer drug isolated from Taxus genus. 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 dimer...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61K31/337A61K9/107A61K9/19A61P35/00
Inventor 顾晓军滕鑫
Owner POLYMERCHEM
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