目的 制备口服葛根总黄酮固体脂质纳米粒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释放度。方法 采用高压均质法制备葛根总黄酮固体脂质纳米粒混悬液，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，考察葛根总黄酮固体脂质纳米粒冻干粉中4种有效成分的释放度。结果 正交试验优选制备工艺：脂质-表面活性剂比例及用量为2：1及2.0%、葛根总黄酮用量2.5%、150 MPa均质15次，并制备葛根总黄酮固体脂质纳米粒冻干粉，其粒径、多分散指数及Zeta电位分别为(517.1±10.3)nm、0.484±0.210及(-21.91±2.03)mV。葛根总黄酮固体脂质纳米粒冻干粉中4种有效成分的释放速率显著低于其物理混合物，具有明显的缓释特征。结论 葛根总黄酮固体脂质纳米粒冻干粉制备方法简便，能显著延缓主要有效成分的释放速率，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 loaded solid lipid nanoparticles (PF-SLN) and determine the dissolution rate of its four effective components: 3'-hydroxypuerarin, puerarin, daidzin, and daidzein. Methods PF-SLN was prepared by the high pressure homogenization (HPH) technology. The lyophilized formula contained mannitol as cryoprotectant. The release rates of the four effective components from the PF-SLN lyophilized powder as well as the physical mixture were determined, with artificial gastric juice (pH 1.2) as dissolvent. Results The technical parameters of PF-SLN preparation optimized by orthogonal test were as follows: The ratio and the dosage of lipid-surfactant were 2:1 and 2.0%, PF dosage was 2.5%, and 150 MPa homogeneity was 15 cycles. The optimal PF-SLN lyophilized powder was loosen with the particle size of (517.1 ± 10.3) nm, polydisperse index of 0.484 ± 0.210, and Zeta potential of (-21.91 ± 2.03) mV, respectively. The in vitro accumulated dissolution rates of PF-SLN lyophilized powder were slower than those of the physical mixture. Conclusion The method employed to prepare PF-SLN lyophilized powder is feasible. PF-SLN lyophilized powder could delay the in vitro dissolution rate notablely. It might be a novel vehicle potentially for nano-drug delivery system of Pueraria flavonoids.

国家重大新药创制项目（2011ZX09401-307）