应用固体分散技术提高黄豆苷元溶出速率∗

摘要

Objective Daidzein solid dispersions were prepared by solid dispersion technology to improve in vitro dissolution rate. Methods Daidzein solid dispersions were prepared by solvent method using polyvinyl pyrrolidone K30 ( PVP K30) as carrier.The in vitro dissolution characteristics of solid dispersions were evaluated,and the properties were detected by IR and XRD. Results The dissolution rates of different mass ratio of daidzein-PVP solid dispersion were significantly improved compared with that of daidzein API.The cumulative dissolution of solid dispersion with mass ratio of 1∶6 within 30 minutes was up to 87.8%,equivalent to six times of API. The in vitro drug release kinetics were fitted mathematically to Korsemeyer-Peppas model. Conclusion Solid dispersion with PVP K30 as carrier could significantly improve dissolution rate of daidzein.%目的：应用固体分散技术制备黄豆苷元固体分散体，提高难溶性药物溶出速率。方法以聚乙烯吡咯烷酮为载体，采用溶剂法制备黄豆苷元固体分散体，考察药物体外溶出特性；应用红外光谱、X-射线衍射分析法进行物相鉴别，评价固体分散体的性质。结果不同药物/载体质量比例的黄豆苷元固体分散体在水中的溶出速率均远高于黄豆苷元原料药。质量比为1∶6的固体分散体30 min内药物累积溶出率可达87.8％，相当于原料药的6倍。固体分散体的体外释药动力学符合Korsemeyer -Peppas模型。结论应用固体分散技术，以聚乙烯吡咯烷酮为载体制备黄豆苷元固体分散体，可有效提高药物溶出速率。