白藜芦醇乳脂体小鼠体内药动学及组织分布研究

Pharmacokinetics and Tissue Distribution of Resveratrol Emulsome in Mice

目的研究白藜芦醇乳脂体在小鼠体内的药动学与组织分布。方法采用薄膜分散法制备白藜芦醇乳脂体。以白藜芦醇乳剂为对照,考察乳脂体小鼠尾静脉注射后的药动学及组织分布。采用3P97程序计算药动学参数,并计算Re、Te。结果乳脂体在小鼠体内过程符合二室模型,主要药动学参数:T1/2β为50.17min;AUC为67.29μg.min.mL-1。乳脂体在心、肝、脾、肺、肾的Re分别为2.10、2.16、1.80、1.42、1.34。Te分别为0.92、1.60、0.94、0.79、0.25,Ce分别为1.31、1.18、0.70、0.29、0.43,乳脂体在各组织的分布特点:C肝>C心>C脾>C肺>C肾。结论乳脂体能相对延长白藜芦醇在体内滞留时间,且明显改变了小鼠体内的分布。

OBJECTIVE To study the pharmacokinetics and tissue distribution of Resveratrol emulsome in mice. METHODS Resvertrol emulsome was prepared by thin film dispersion （TFD）. Resvertrol emulsome injection pharmacokinetic parame ters and tissue distribution had been modeled with 3p97 program and statistic rules comparing with resvertrol emulsion. RE- SULTS The concentration-time curve of emulsome and emulsion after iv were in accordance with a two-compartment model and the main pharmaeokinetic parameters were as follows： T1/2β50.17 rain, AUC 67.29μg. min-mL 1 . Relative exposure （Re） of emulsome in heart, liver, spleen, lung, kidney was 2.10, 2.16, 1.80, 1.42, 1.34. Targeting efficiency was 0.92, 1.60, 0.94, 0.79, 0.25 and the ratio of maximum concentration was 1.31, 1.18, o. 70, o. 29, o. 43. The tissue distribution feature of emulsome was Cliver〉Cheart〉Cspleen〉Clung〉Ckldney. CONCLUSION The results indicate that emulsome injection could extend the retention time of resveratrol and improve drug concentration in mice with resveratrol emulsion.