Self-emulsifying preparation of taxane compound and preparation method thereof

Abstract

The invention provides a self-emulsifying pharmaceutical composition for delivering taxane drugs and a preparation method thereof. The self-emulsifying pharmaceutical composition is a clear liquid, comprising effective doses of taxane compounds, oil components, surfactants and ethanol, and preferably contains lactic acid, wherein the surfactants are phospholipids and polyoxyethylene castor sesame oil. When the above self-emulsifying composition is added to glucose injection, it can be self-emulsified to form a microemulsion with an average particle diameter of 50-300 nm, and the microemulsion can be stable at room temperature for more than 12 hours. The preferred taxane compound in the present invention is paclitaxel.

Description

technical field [0001] The invention relates to a taxane self-emulsifying pharmaceutical composition, in particular to a taxane self-emulsifying pharmaceutical composition which can be administered intravenously. Background technique [0002] Taxane compound is a general term for a class of taxanes and taxanes with molecular results similar to taxines, analogs and derivatives, which are currently used in the treatment of metastatic ovarian cancer, lung cancer, esophagus First-line treatment drugs for cancer, including paclitaxel, docetaxel, gibberellin, gibberelin diacetate, paclitaxel B, etc. Among them, the most commonly used taxane compounds in clinical practice are paclitaxel and docetaxel Paclitaxel. [0003] Paclitaxel has the structure of formula I, is a white crystalline powder, odorless, tasteless, its English name is Paclitaxel or Taxol, and its molecular formula is C 47 h 51 NO 14 , the molecular weight is 853.92. [0004] [0005] Docetaxel is a semi-synt...

AI Technical Summary

Problems solved by technology

③Compatibility changes: Compatibility of 60 commonly used clinical drugs with paclitaxel injection will cause infusion turbidity, and some drugs will compete with paclitaxel for binding to plasma proteins, which will increase toxicity

The preparation method of the emulsion is also relatively complicated, and industrial production is relatively difficult

[0013] Chinese patent application CN100341485C discloses a self-emulsifying pre-concentrate of paclitaxel, which is composed of paclitaxel, surfactants such as polyoxyethylene castor oil, oil phases such as medium-chain triglycerides, ethanol or propylene glycol, however, from its implemented technology It can be seen from the scheme that the product prepared by it is unstable after forming an emulsion, so it can only be administered orally and cannot be given to patients in the form of intravenous injection

However, after the emulsion is formed, the stability time is not long, paclitaxel is easy to separate out from the solution, which affects clinical use, and due to the large amount of surfactant, the irritation is still very large when used

[0016] Therefore, it can be seen that the current technical solution is far from meeting the clinical demand for paclitaxel, and the prior art still needs a stable taxane injection preparation that is simple to prepare, easy to use, less irritating, low in cost, and capable of industrial production.

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