[关键词]
[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。
[Key word]
[Abstract]
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.
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[基金项目]
国家重大新药创制项目(2011ZX09401-307)