Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing 210009, China.
Phytother Res. 2012 Jan;26(1):67-72. doi: 10.1002/ptr.3516. Epub 2011 May 5.
Zhi-Zi-Hou-Pu decoction (ZZHPD), a classic antidepressant formula, is composed of Gardenia jasminoides Ellis (ZZ), Fructus aurantii immaturus (ZS) and Cortex magnoliae officinalis (HP). ZZHPD has attracted a great deal of attention for its antidepressant effects. The aim of this study was to compare the pharmacokinetics of geniposide (one of the predominant active ingredients) after oral administration of different combinations of ZZHPD and to explore the influence of herb-herb interaction on the pharmacokinetics of geniposide. Twenty four rats were divided randomly into four groups and were administered one of the four extracts: ZZ, ZZ-HP, ZZ-ZS and ZZHPD (ZZ-HP-ZS) via intragastric gavage with approximately the same dose of 40.65 mg/kg geniposide (an effective human daily dose of ZZHPD). Plasma concentrations of geniposide were determined using an HPLC method. Pharmacokinetic parameters were calculated from the plasma concentration-time data. Compared with ZZ alone, the ZZ-ZS combination delayed T(max) and ZZ-HP, ZZ-ZS, ZZHPD remarkably shortened the T(1/2) of geniposide. In addition, ZZ-HP, ZZ-ZS, ZZHPD obviously increased the AUC of geniposide. The result illustrated that the oral bioavailability of geniposide was dramatically enhanced when ZZ was combined with HP or/and ZS. It can be deduced that herb-herb interaction may increase the absorption, and significantly improve the oral bioavailability of geniposide in rats.
栀子厚朴汤（ZZHPD），一种经典的抗抑郁方剂，由栀子（ZZ）、枳实（ZS）和厚朴（HP）组成。由于其抗抑郁作用，ZZHPD 引起了广泛关注。本研究旨在比较不同 ZZHPD 组合给药后京尼平苷（主要活性成分之一）的药代动力学，探讨草药-草药相互作用对京尼平苷药代动力学的影响。将 24 只大鼠随机分为 4 组，分别灌胃给予 ZZ、ZZ-HP、ZZ-ZS 和 ZZHPD（ZZ-HP-ZS），剂量约为 40.65mg/kg 京尼平苷（相当于 ZZHPD 的有效人体日剂量）。采用 HPLC 法测定血浆中京尼平苷的浓度。从血浆浓度-时间数据计算药代动力学参数。与 ZZ 单药相比，ZZ-ZS 合用使 T(max)延迟，ZZ-HP、ZZ-ZS、ZZHPD 显著缩短京尼平苷的 T(1/2)。此外，ZZ-HP、ZZ-ZS、ZZHPD 明显增加了京尼平苷的 AUC。结果表明，当 ZZ 与 HP 或/和 ZS 合用时，京尼平苷的口服生物利用度显著提高。可以推断，草药-草药相互作用可能会增加吸收，显著提高大鼠京尼平苷的口服生物利用度。
