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Docetaxel pharmaceutical composition

A technology of docetaxel and composition, applied in the field of docetaxel pharmaceutical composition, can solve the problems of no breakthrough of docetaxel freeze-dried powder, increase the difficulty of use, increase the burden on patients, etc., and achieve easy industrialization. Application, high safety, simple prescription effect

Inactive Publication Date: 2016-02-03
POLYMERCHEM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, it is necessary to give patients oral glucocorticoids in advance for desensitization, and patients who have already experienced allergic reactions need to inject epinephrine, which undoubtedly increases the burden on patients.
[0006] The second disadvantage is that the method of administration is more complicated, which increases the difficulty of use
[0010] At present, no breakthrough has been made in the research results of docetaxel freeze-dried powder, especially in terms of components, particle size after reconstitution and drug loading, etc.

Method used

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  • Docetaxel pharmaceutical composition
  • Docetaxel pharmaceutical composition
  • Docetaxel pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment (1-7

[0033] Docetaxel is an anhydrous docetaxel raw material (CAS: 114977-28-5), produced by Xi'an Tianfeng Biotechnology Co., Ltd.;

[0034] Polyethylene glycol methyl ether-polylactide-phenylalanine was prepared by the inventor according to the process described in patent number PCT-CN-2013000453. The average molecular weight of different blocks is determined by mass spectrometry and combined with the molecular weight of the reaction raw materials.

[0035] The preparation process of the freeze-dried powder formulation of the pharmaceutical composition of docetaxel in the examples includes the following steps.

[0036] ① Weigh docetaxel and polyethylene glycol methyl ether-polylactide-phenylalanine according to different feeding ratios (see Table 2);

[0037] ② Put the above-mentioned raw materials into the container, and add organic solvents until they are completely dissolved. The types of organic solvents include ethanol, acetonitrile, etc. Rotary evaporation at 30-50°C for 2 hours u...

experiment example 8

[0046] Tumor suppression tests were performed using physiological saline, commercial docetaxel injection (Taxotere) and docetaxel micellar solution (obtained in the examples of the present invention). Balb / c mice transplanted with L7912 tumor strain were used as test subjects. The route of administration is intravenous administration, once every 3 days, for 30 consecutive days. The concentration of Taxotere and the docetaxel of the present invention is also 10 mg / kg. The tumor volume of the mice was measured twice a week, and the results are shown in Table 3. The results showed that the tumor volume of mice instilled with normal saline increased rapidly; the tumor volume growth rate of mice instilled with Taxotere was controlled to a certain extent, but the tumor volume still increased; the tumor volume of mice instilled with the present invention was controlled and rapidly Decrease (see Table 3). It is proved that the present invention has a significant inhibitory effect on...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations and particularly relates to a docetaxel pharmaceutical composition. The docetaxel pharmaceutical composition comprises, by weight, 3.57-25.76 parts of docetaxel and 100 parts of polyethylene glycol methyl ether-polylactide-phenylalanine. The docetaxel pharmaceutical composition has the advantages that the polyethylene glycol methyl ether-polylactide-phenylalanine lower in toxicity is used as a carrier, and besides active pharmaceutical ingredients and the carrier, the docetaxel pharmaceutical composition contains no additives, thereby being simpler in composition and higher in safety; the docetaxel pharmaceutical composition is above 20% in docetaxel content and is simple in technology and easy for industrial application.

Description

Technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and specifically relates to a docetaxel pharmaceutical composition. Background technique [0002] Docetaxel (Docetaxel, Docetaxel, C 43 H 53 NO 14 ) Is a new anti-tumor drug obtained after structural modification based on the structure of the natural anti-tumor drug paclitaxel. Its anti-spectrum is similar to paclitaxel. Its mechanism of action is to promote tubulin polymerization and prevent microtubule depolymerization. So as to inhibit the mitosis and proliferation of cancer cells, the drug effect is stronger than paclitaxel. [0003] In vitro studies have shown that in human breast, colon, bladder and epithelioid cell lines, its IC50 is 9 times lower than paclitaxel. In vivo studies have shown that docetaxel has a high degree of anti-tumor activity, and mouse tumors and mouse transplanted tumors can completely disappear after treatment. More importantly, cell lines resistant to...

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