Docetaxel micelle production method and product

Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a docetaxel micelle production method and a product. A methoxypolyethylene glycol-polylactide-aspartic acid triblock copolymer is adopted as a micelle carrier. The obtained docetaxel micelle has the advantages of high drug loading capacity, good particle size uniformity, high stability and thelike; besides, there is no need to add other auxiliary components in the preparation, the solvent residual amount is lower, the safety is higher, and the preparation process is simple and easy to usein industry.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a production method and products of docetaxel micelles. Background technique [0002] Docetaxel (Docetaxel, Docetaxel, C 43 h 53 NO 14 ), is a new anti-tumor drug obtained after structural modification on the basis of the structure of the natural anti-tumor drug paclitaxel. Its anti-tumor spectrum is similar to that of paclitaxel. Thereby inhibiting the mitosis and proliferation of cancer cells, and the drug effect is stronger than paclitaxel. [0003] In vitro studies have shown that its IC50 is 9 times lower than paclitaxel in human breast, colon, bladder and epithelial cell lines. [0004] In vivo studies have shown that docetaxel has a high degree of anti-tumor activity, and the tumors in mice and transplanted tumors in mice can completely regress after administration. [0005] More importantly, docetaxel-resistant paclitaxel-resistant cel...

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.

[0008] The second disadvantage is that the method of administration is more complicated, which increases the difficulty of use

[0010] The use of polymers to make docetaxel micellar products can overcome the shortcomings of commercially available docetaxel medicaments, but the results of research on docetaxel micelles generally lack practical value, and the main disadvantages include that the particle size is too large and The EPR effect cannot be exerted, the drug loading is too low, the stability of the preparation is poor, etc.

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