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目的制备多西他赛自乳化半固体胶囊剂,并考察其在大鼠体内的药动学特性。方法通过测定溶解度和绘制三元相图的对自乳化处方进行筛选,应用单纯形网格法进行处方优化;采用熔融法制备半固体胶囊并对该半固体胶囊进行大鼠体内的药动学研究。结果作者制备高载药量的多西他赛自乳化半固体胶囊剂,受试制剂中多西他赛的相对生物利用度为参比制剂的1.61倍。结论多西他赛自乳化半固体胶囊剂能够显著提高多西他赛的生物利用度。
Objective To prepare docetaxel self-emulsifying semi-solid capsules and investigate its pharmacokinetics in rats. Methods The self-emulsifying prescriptions were determined by measuring the solubility and drawing the ternary phase diagram. The simplex grid method was used to optimize the formulation. Semi-solid capsules were prepared by melt method and the pharmacokinetics of the semi-solid capsules were studied in vivo . Results The authors prepared a high drug loading of docetaxel self-emulsifying semi-solid capsules. The relative bioavailability of docetaxel in the test formulation was 1.61 times that of the reference formulation. Conclusion Docetaxel self-emulsifying semi-solid capsules can significantly improve the bioavailability of docetaxel.