目的:考察以聚乙烯吡咯烷酮为载体制备固体分散体对大豆苷元溶解度、溶出度和生物利用度的改善。方法:溶剂法制备大豆苷元固体分散体,差示量热法、傅立叶红外、平衡溶解度法、溶出度法考察固体分散体的性质;小鼠血浆动力学比较大豆苷元固体分散体和大豆苷元的生物利用度。结果:以聚乙烯吡咯烷酮为载体的固体分散技术将大豆苷元的溶解度提高了8倍,且明显增加了其溶出度;提高了大豆苷元在小鼠血浆中的达峰浓度和曲线下面积。结论:以聚乙烯吡咯烷酮为载体的固体分散技术可提高大豆苷元在小鼠体内的生物利用度。
Objective:To study on the dispersion of daidzein with polyvinylpyrrolidone(PVP)and its effects on the aqueous solubility,dissolution rate and bioavailability of daidzein.Methods:The solid dispersion of daidzein at various daidzein to PVP ratios were obtained via the solvent evaporation method and characterized by differential scanning calorimetry and fourier transform infrared spectroscopy.In addition,the bioavailability of free daidzein as well as its solid dispersion were studied in mice.Results:It was found that the daidzein solubility in the solid dispersion form was 8 times greater than that of the free drug in water at(37±0.1)℃.Meanwhile,the daidzein dissolution rate was significantly increased after dispersing with PVP.The results of the bioavailability showed that both Cmax and AUC value of daidzein solid dispersion were about 5 times larger than unprocessed daidzein,implying that the rate-limiting step in daidzein absorption may be the dissolution process.Conclusions:The results in this work reveal the substantial advantages of adopting polyvinylpyrrolidone dispersion as an oral preparation to improve daidzein bioavailability.