口服葛根总黄酮纳米混悬液冻干粉的制备及其4种有效成分溶出度考察  

Preparation of lyophilized powder of oral Pueraria flavonoids nanosuspension and determination of dissolution rates of its four effective components

作　　者：王治平[1] 周群[2] 樊化[3] 王一飞[3] 

机构地区：[1]广东药学院药科学院,广东广州510006 [2]华中科技大学同济药学院,湖北武汉430030 [3]暨南大学生物医药研究院,广东广州510632

出　　处：《中草药》2014年第5期635-641,共7页Chinese Traditional and Herbal Drugs

基　　金：国家重大新药创制项目(2011ZX09401-307)

摘　　要：目的制备葛根总黄酮纳米混悬液冻干粉,并考察其主要有效成分(3′-羟基葛根素、葛根素、大豆苷和大豆苷元)的溶出度。方法采用高压均质法制备葛根总黄酮纳米混悬液,以甘露醇为冻干保护剂制备冻干粉,以人工胃液(pH 1.2)为溶出介质,考察葛根总黄酮纳米混悬液冻干粉及其物理混合物中葛根素、3′-羟基葛根素、大豆苷和大豆苷元的溶出度。结果单因素试验并验证制备葛根总黄酮纳米混悬液冻干粉,其粒径、多分散指数及Zeta电位分别为(479.7±14.7)nm、0.524±0.220及(29.68±3.97)mV。葛根总黄酮纳米混悬液冻干粉4种有效成分的溶出速率显著高于其物理混合物。结论葛根总黄酮纳米混悬液冻干粉制备方法简便,能显著提高主要有效成分的溶出速率,有望成为葛根总黄酮的新型纳米给药系统。Objective To prepare the lyophilized powder of Pueraria flavonoids nanosuspension （PF-NS） and to determine the dissolution rates of its four effective components （3′-hydroxypuerarin, puerarin, daidzin, and daidzein）. Methods PF-NS was prepared by the high pressure homogenization （HPH） technology. The lyophilized formula contained mannitol as lyoprotectant. The dissolution rates of the four effective components from lyophilized powder of PF-NS as well as the physical mixture were determined, with artificial gastric juice （pH 1.2） as dissolvent. Results The optimal lyophilized powder of PF-NS was loosed with the particle size of （479.7 ±14.7） nm, polydisperse index of 0.524± 0,220, and Zeta potential of （29.68 ±3.97） mV, respectively. The in vitro accumulated dissolution rate of lyophilized powder of PF-NS was higher than that of the physical mixture. Conclusion The method employed to prepare the lyophilized powder in PF-NS is simple and feasible. The lyophilized powder of PF-NS could improve the in vitro dissolution rate notablely. It might be a novel vehicle potentially for nano-drug delivery system of PF.

关 键 词：葛根总黄酮 纳米混悬液 有效成分 溶出度 冻干粉 3′-羟基葛根素 葛根素 大豆苷 大豆苷元 

分 类 号：R283.6[医药卫生—中药学]