柚皮素-PVPK-30固体分散体的制备及体外特性研究  

Preparation of naringenin-PVPK-30 solid dispersion and its characteristics in vitro

作　　者：戴春兰[1] 王光发[1] 廖正根[1] 赵国巍[1] 梁新丽[1] 张南[1] 

机构地区：[1]江西中医学院现代中药制剂教育部重点实验室,江西南昌330004

出　　处：《中成药》2011年第1期45-49,共5页Chinese Traditional Patent Medicine

基　　金：江西省卫生厅中医药科研课题(2008A012);国家科技重大专项(重大新药创制2009ZX09310-005)

摘　　要：目的:采用固体分散技术提高柚皮素的体外溶出度。方法:以PVPK-30为载体采用喷雾干燥法制备柚皮素固体分散体,进行饱和溶解度和体外溶出度实验;采用差示扫描量热法(DSC)和X-射线衍射法分析药物的存在状态,红外光谱法(IR)分析药物与载体间的相互作用。结果:与原料药及物理混合物相比,固体分散体的溶解度、溶出速度和程度均有明显提高,DSC和X-射线衍射法分析表明药物在载体中以无定形或分子状态存在,红外光谱法测定结果显示柚皮素与PVPK-30可能以分子间氢键结合在一起。结论:采用喷雾干燥法制备的柚皮素-PVPK-30固体分散体可显著提高柚皮素的溶解度及溶出速度。AIM：To improve the dissolution of naringenin in water by solid dispersion.METHODS：Solid dispersion of naringenin was prepared by spray-drying technique with PVPK-30 as the carrier,and the saturation solubility and in vitro dissolution of naringenin was studied;The physical state was characterized by Differential Scanning Calorimetry（DSC）、X-ray diffractometry and the possible molecular interaction between naringenin and PVPK-30 was characterized by infrared spectroscopy（IR）.RESULTS：The results showed that naringenin content and in vitro dissolution rate was significantly improved by solid dispersion as compared with that of the pure naringe-nin and physical mixture.Solubility studies revealed a marked increase in the solubility of naringenin.The results of DSC and X-ray diffractometry showed that naringenin in solid dispersion took amorphous form,the results of in-frared spectroscopy showed there existed intermolecular hydrogen bond between naringenin and PVPK-30.CON-CLUSION：The solubility and dissolution of naringenin is improved by preparation of naringenin-PVPK-30 solid dispersion.

关 键 词：柚皮素 喷雾干燥 固体分散体 溶出度 

分 类 号：R944[医药卫生—药剂学]