白藜芦醇β-环糊精包合物在大鼠体内生物利用度研究  

Pharmacokinetics of Resveratrol β-Cyclodextrin Inclusion Compound in Rats

作　　者：于琛琛 张纯刚[1] 程岚[1] Yu Chenchen;Zhang Chungang;Cheng Lan(College of Pharmacy,Liaoning University of Traditional Chinese Medicine,Dalian,116620,China)

机构地区：[1]辽宁中医药大学

出　　处：《亚太传统医药》2019年第11期19-21,共3页Asia-Pacific Traditional Medicine

基　　金：国家自然科学基金资助项目(81503257);国家重点研发计划(2018YFC1706903);辽宁省博士启动基金(201501098)

摘　　要：目的:研究口服白藜芦醇原料药和白藜芦醇β-环糊精包合物在大鼠体内的药动学过程。方法:建立大鼠血浆中白藜芦醇的HPLC-UV检测方法。考察大鼠经口服给予白藜芦醇原料药和包合物后血药浓度变化。用DAS3.0软件计算药动学参数。结果:白藜芦醇浓度在10~2500 ng/mL范围内线性关系良好(r=0.9995);定量下限为10 ng/mL;日内和日间精密度为3.26%~4.60%;准确度为97.26%~100.0%;提取回收率为96.6%~100.5%。大鼠经口服白藜芦醇原料药和β-环糊精包合物,白藜芦醇在大鼠体内消除半衰期分别为(2.56±2.00)和(4.42±0.52)h;Cmax分别为(473.3±200.8)和(1135.3±60.6)ng/mL;AUC0-t分别为(514.7±117.5)和(1191.4±147.9)ng/mL*h。白藜芦醇口服制剂与原料药对比,其相对生物利用度为225.6%。结论:白藜芦醇原料药的口服制备成β-环糊精包合物后相对生物利用度有较明显提高。Objective:The aim of this article was to study the bioavailability of Resveratrol crude drug andβ-cyclodextrin inclusion compound in rats.Methods:High performance liquid chromatography(HPLC)was established for detecting plasma concentrations of resveratrol and investigating its pharmacokinetics in rats with oral administration.The software of DAS3.0 was used to process the pharmacokinetic parameters.Results:The linear calibration curve was obtained in the range of 10~2500 ng/mL for resveratrol(r=0.9995),and the lower limit of quantitation was 10 ng/mL.Intra-and inter-day precision for all samples were in the range of 3.26%~4.60%,and the accuracy of three different concentrations was in the range of 97.26%~100.0%.The extraction recovery of resveratrol from rat plasma was between 96.6%~100.5%.The main pharmacokinetics parameters of resveratrol after oral administration of crude drug and preparations of resveratrol to rats were shown as follows:t1/2,(2.56±2.00)and(4.42±0.52)h;Cmax,(473.3200.8)and(1135.360.6)ng/mL;AUC0-t,(514.7±117.5)and(1191.4±147.9)ng/mL*h,respectively.The formulation produced a significant 2.26 fold improvement in the oral bioavailability of resveratrol as compared to crude drug.Conclusion:The preparation of resveratrol withβ-cyclodextrin as the carrier increases the bioavailability of resveratrol in rats.

关 键 词：白藜芦醇 包合物 相对生物利用度 高效液相色谱法 药代动力学 

分 类 号：R285.5[医药卫生—中药学]