Taxol microemulsion drug composition and preparation method thereof

Abstract

The invention discloses a taxol microemulsion drug composition and a preparation method thereof. The drug composition comprises the following active ingredients: taxol, an oil phase, a solubilizing agent, a stabilizing agent, an excipient, an acidity regulator and water for injection and is characterized in that the main grain size of taxol microemulsion ranges from 10nm to 40nm; and the parts by weight of taxol, an emulsifying agent, the oil phase and the water phase are respectively 30, 1500-3000, 100-350 and 5000-50000. The drug composition has the beneficial effects that taxol is taken as the main drug and different auxiliary materials are added to prepare microemulsion; the taxol microemulsion freeze-dried preparation prepared through freeze drying has good water solubility and stability; the clinical defect of severe allergic reaction of the taxol injection in the market is overcome; meanwhile, the preparation process is simple and is suitable for industrial mass production; and a new administration dosage form is provided for clinical application of taxol.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a novel paclitaxel microemulsion pharmaceutical composition and a preparation method thereof. [0002] Background technique [0003] Paclitaxel has good anticancer activity and is mainly used clinically for the first-line and second-line treatment of ovarian cancer, breast cancer and non-small cell lung cancer. However, paclitaxel injections currently in clinical use are all solubilized preparations of polyoxyethylene castor oil (CremPHor EL)-absolute ethanol (V:V=50:50), which has severe allergic reactions, which greatly limits the wide clinical use of paclitaxel. application. Therefore, safe, stable and efficient new formulations of paclitaxel have been receiving people's attention. Existing new technologies, such as emulsion technology, nanotechnology, polymeric micelle technology, cyclodextrin inclusion technology, liposome technology, microsphere tec...

AI Technical Summary

Problems solved by technology

Existing new technologies, such as emulsion technology, nanotechnology, polymeric micelle technology, cyclodextrin inclusion technology, liposome technology, microsphere technology and other new technologies have been applied to the study of paclitaxel solubilization, however, these new preparations Although the deficiencies of the existing paclitaxel preparations have been improved to a certain extent, they all have their own defects, such as: emulsions and microemulsions are easy to separate; cyclodextrin itself has extremely high nephrotoxicity; liposome preparations have low encapsulation efficiency , easy to leak, poor stability; low drug loading of polymer nanoparticles, obvious burst release phenomenon, difficult to remove organic solvents, etc.; microsphere preparations have many problems such as limited drug loading, poor stability, and difficulty in withstand autoclave sterilization

These insurmountable defects have seriously hindered the industrialization development and practical clinical application of new paclitaxel preparations.

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