托伐普坦片的制备及体外溶出评价

Preparation and in Vitro Evaluation of Tolvaptan Tablets

目的探讨流化床干燥法制备固体分散体,以改善托伐普坦的溶出度。方法以乳糖为底物,水溶性材料羟丙纤维素为载体,采用流化床干燥法制备托伐普坦固体分散体,利用粉末X射线衍射对固体分散体进行表征,并研究其体外溶出度。结果X射线衍射结果显示,托伐普坦在流化床干燥过程中转变成了无定形;体外溶出结果显示,固体分散体样品的溶出度优于物理混合物样品。结论采用流化床干燥法制成固体分散体,可显著提高托伐普坦的体外溶出度。

Objective To explore the preparation of solid dispersion by fluidized bed drying method to improve the dissolution of tolvaptan.Methods Tolactopan solid dispersion was prepared by fluidized bed drying method using lactose as substrate and water-soluble material hydroxypropyl cellulose as carrier.The solid dispersion was characterized by powder X-ray diffraction and the dissolution rate in vitro was studied.Results X-ray diffraction results showed that tolvaptan turned into amorphous during the fluidized bed drying process;in vitro dissolution results showed that the dissolution rate of the solid dispersion sample was better than that of the physical mixture sample.Conclusion The application of fluidized bed drying method for preparing solid dispersion can significantly improve the in vitro dissolution of tolvaptan.