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

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...

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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

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