利用固体分散体技术改善吴茱萸次碱体外溶出度研究

Improvement of in Vitro Dissolution Rate of Rutaecarpine Using Solid Dispersion Technology

目的:制备吴茱萸次碱(Rut)固体分散体(SD),提高Rut体外溶出度。方法:分别以聚乙烯吡咯烷酮(PVP)为载体,采用溶剂-共沉淀法,制备含不同辅助载体(微粉硅胶、乳糖、微晶纤维素、去氧胆酸、卵磷脂、滑石粉等)及比例的Rut-SD,评价其体外溶出度并进行处方优选;采用X-射线衍射分析和差示热分析法对SD进行物相鉴别。结果:处方组成以Rut-PVP-微粉硅胶(1∶2∶1)和Rut-PVP-乳糖(1∶2∶2)较好,其累积溶出度(60 min)较同成分组成的物理混合物提高了约6倍;物相鉴别结果表明Rut以微晶状态存在于SD中。结论:以PVP为载体、适当比例的微粉硅胶和乳糖为辅助载体制备的Rut-SD可显著提高Rut的体外溶出度。

OBJECTIVE： To prepare rutaecarpine （Rut） solid dispersion （SD）, and to improve the dissolution rate of rutaecarpine in vitro. METHODS： Rut-SD containing different supplementary carriers （gum arabic, lactose, avicel, chenic acid, lecithin, talcum, etc.） with different ratios was prepared by solvent-melting method using PVP as carrier. The dissolution rate in vitro was evaluted and the formula was optimized. Differential thermal analysis and X-ray diffraction were used for phase identification of SD. RESULTS ： The optimal formula included Rut-PVP-gum arabic （ 1 ： 2 ： 1 ） and Rut-PVP-lactose （ 1 ： 2 ： 2）. The accumulative dissolution rate of them （60 min） was improved about 6 times as physical mixture with same component. Phase identification indicated that Rut existed in the form of microcrystal in SD. CONCLUSION： Rut-SD can improve in vitro dissolution rate of Rut which has been prepared with PVP as carrier and using suitable ratio of gum arabic and lactose as supplementary carrier.