虎杖苷在大鼠体内的药动学特点和组织分布研究

Pharmacokinetic characteristics and tissue distribution of polydatin in rats in vivo

目的建立RP-HPLC测定大鼠血浆及组织样本中虎杖苷的方法,研究虎杖苷在大鼠体内的药动学行为和组织分布特点。方法采用Diamonsil C18色谱柱(250mm×4.6mm,5μm),乙腈-水(26∶74)为流动相,体积流量为1.0mL/min,检测波长为303nm。结果虎杖苷在大鼠血浆及各组织中一定质量浓度范围内线性关系良好,其高、中、低3种不同质量浓度的回收率及日内、日间精密度均符合方法学要求。大鼠ig虎杖有效部位后,虎杖苷在大鼠体内的药动学行为符合二室开放模型,在体内分布广泛,以脾、心、肺、胃中分布较高。结论建立了大鼠血浆及组织匀浆中虎杖苷的RP-HPLC测定方法,此方法简便、快速,结果准确、可靠;并首次阐明了虎杖苷在大鼠体内的药动学特点和不同组织内的分布情况。

Objective To establish a RP-HPLC method to determine the polydatin in plasma and tissues of rats in vivo and to study its pharmacokinetic behaviour and tissue distribution characteristics. Methods Chromatographic separation was achieved by RP-HPLC using C18 column （250 mm× 4.6 mm, 5μm） as stationary phase and acetonitrile-water （26 ：74） as mobile phase with a flow rate of 1.0 mL/min.The UV detective wavelength was 303 nm. Results Good linearties were obtained in plasma and every kind of tissue over a certain range. The recovery, intra-day and inter-day precision of three different concentrations of polydatin in plasma and tissues met the requirements of methodology. The pharmacokinetic characteristics of polydatin after ig administration to rats complied with the open two-compartment model. The results of tissue distribution showed that polydatin was distributed widely in rats. The highest level was found in spleen, heart, lung, and stomach after ig administration （50 mg/kg） of polydatin. Conclusion The RP-HPLC method is established to determine the concentration of polydatin in plasma and tissues. The method is quick, precise, and reproducible. It is the first time to study the pharmacokinetic characters and tissue distribution of polydatin in rats in vivo after ig administration.