Abstract Schisandra chinensis fructus (SCF) is widely used traditional Chinese medicine, which possesses hepato-protective potential. Schisandrin (SD), schisantherin (ST), and γ-schizandrin (SZ) are the major bioactive lignans. The main problem associated with the major bioactive lignans oral administration is low oral bioavailability due to the lignans’ poor aqueous solubility and taste. The aim of the present research work was to develop liposome (SCL) encapsulated β-cyclodextrin (β-CD) inclusion complex loaded with SCF extract (SCF-E). The SD, ST, and SZ were selected as effective candidates to perform comparisons of liver targeting among the solution (SES), β-cyclodextrin inclusion compound (SCF-E-β-CD), liposome (SEL), and SCL of SCF-E to characterize the pharmacokinetic behaviors and liver targeting in rats. The β-CD inclusion complex (SCF-E-β-CD) was used to improve the solubility. The concentrations were determined using high-performance liquid chromatography (HPLC) and analyzed by DAS3.0. The pharmacokinetic results indicate that the plasma concentration-time courses were fitted well to the one-compartment model with the first weighing factor. The half-life period (t1/2) and area under the concentration-time curve (AUC) of the three components in SCL were the largest. The SCL exhibit a relatively high liver targeting effect. The results would be helpful for guiding the clinical application of this herbal medicine.

中文翻译：

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五味子提取物β-环糊精包合物脂质体口服给药后三种五味子木脂素在大鼠体内的药代动力学及肝摄取

摘要 五味子(SCF)是一种应用广泛的中药，具有保肝作用。五味子素（SD）、五味子素（ST）和γ-五味子素（SZ）是主要的生物活性木酚素。与主要生物活性木脂素口服给药相关的主要问题是由于木脂素的水溶性和味道差，口服生物利用度低。本研究工作的目的是开发装载有 SCF 提取物 (SCF-E) 的脂质体 (SCL) 封装的 β-环糊精 (β-CD) 包合物。选择 SD、ST 和 SZ 作为有效候选物，以在溶液 (SES)、β-环糊精包合物 (SCF-E-β-CD)、脂质体 (SEL) 和 SCF-的 SCL 之间进行肝脏靶向的比较。 E 表征大鼠的药代动力学行为和肝脏靶向。β-CD 包合物（SCF-E-β-CD）用于提高溶解度。使用高效液相色谱法 (HPLC) 确定浓度并通过 DAS3.0 进行分析。药代动力学结果表明，血浆浓度-时间过程与具有第一个权重因子的单室模型非常吻合。SCL中三种成分的半衰期(t1/2)和浓度-时间曲线下面积(AUC)最大。SCL 表现出相对较高的肝脏靶向作用。研究结果将有助于指导该草药的临床应用。药代动力学结果表明，血浆浓度-时间过程与具有第一个权重因子的单室模型非常吻合。SCL中三种成分的半衰期(t1/2)和浓度-时间曲线下面积(AUC)最大。SCL 表现出相对较高的肝脏靶向作用。研究结果将有助于指导该草药的临床应用。药代动力学结果表明，血浆浓度-时间过程与具有第一个权重因子的单室模型非常吻合。SCL中三种成分的半衰期(t1/2)和浓度-时间曲线下面积(AUC)最大。SCL 表现出相对较高的肝脏靶向作用。研究结果将有助于指导该草药的临床应用。