摘要
目的:建立一种快速、灵敏的HPLC-MS/MS法测定大鼠血浆中芍药苷,考察桂枝-白芍药对不同比例配伍水煎液灌胃给予大鼠后芍药苷在大鼠体内的药代动力学行为。方法:大鼠分别灌胃给予桂枝-白芍药对不同比例配伍水煎液(给药剂量:以芍药苷50 mg/kg计算),给药前后不同时间点采血。采用甲醇沉淀蛋白的方法处理血浆样品,以华法林为内标,应用HPLC-MS/MS测定芍药苷血药浓度,分析计算芍药苷大鼠体内主要药物动力学参数。结果:血浆样品HPLC-MS/MS方法学验证结果均符合生物样品测定要求。桂枝-白芍药对不同比例配伍水煎液大鼠灌胃给药后,配伍比例为1∶1时芍药苷的药时曲线中呈现较快的药物吸收趋势。单芍组的Cmax、AUC(0-t)、AUC(0-∞)与其他三组之间差异有统计学意义(P<0.05或P<0.01)。不同比例配伍的桂枝-白芍药对(1∶1、1∶2、5∶3)的芍药苷相对生物利用度分别为302.61%、155.56%、245.45%。各组的达峰时间虽未见明显变化,但各组生物半衰期之间的差异有统计学意义(P<0.05)。结论:桂枝-白芍药对不同比例配伍对芍药苷体内药动学有明显的影响。本实验从药动学角度在一定程度上解释古方用药针对不同病症药物不同用量的科学性与合理性。
AIM：To develop and validate a simple and sensitive high performance liquid chromatography-tandem mass spectrometry （HPLC-MS/MS） method for the quantification of paeoniflorin and to investigate the effect of different proportions of Ramulus Cinnamomi and Radix Paeoniae Alba on the pharmacokinetics of paeoniflorin in rats.METHODS：After the different proportion of Ramulus Cinnamomi and Radix Paeoniae Alba were orally administrated to each group at a paeoniflorin dose of 50 mg/kg in rats,the plasma samples were collected at the designated time points.The plasma concentration of paeoniflorin was determined by HPLC-MS/MS,warfarin as the internal standard.The main pharmacokinetic parameters were calculated and analyzed.RESULTS：The results of HPLCMS/MS assay in plasma samples were in accordance with the requirements of biological samples.This method was successfully applied to the pharmacokinetics study of paeoniflorin in rats.The ratio of Ramulus Cinnamomi and Radix Paeoniae Albaat 1：1 showed the rapid drug absorption trends.The C AUC（0-1） and AUC（0-∞） of single peony group was statistically significant compared with other groups （P 〈 0.05 or P 〈 0.01）.The relative bioavailability of paeoniflorin in different proportions of Persicae Ramulus and Paeoniae Radix Alba were 302.61%,155.56%,245.45%,respectively.There was no significant change in tmax,but there was significant difference in biological half-life （P 〈 0.05）between each group.CONCLUSION：The pharmacokinetics of paeoniflorin was affected by the proportion of Ramulus Cinnamomi and RadixPaeoniae Alba.In the view of pharmacokinetics,this experiment explains the scientific nature and rationality of ancient traditional Chinese to a certain extent.
作者
陈永财
钱江辉
王彬辉
沙先谊
翁金月
CHEN Yongcai;QIAN Jianghui;WANG Binhui;SHA Xianyi;WENG Jinyue(Department of Pharmaceuties, Wenzhou Hospital of Traditional Chinese Medicine, Wenzhou 325000, Zhejiang, China;Department of Pharmaceutics, School of Pharmacy, Fudan University, Shanghai 201232, China;Academy of Integrative Medicine, Fudan University, Shanghai 201232, China;Department of Pharmaeeu- tics, Affiliated Hospital of Taizhou Medical College, Taizhou 318002, Zhejiang, China;Department of Pharmaeeutics, Wenzhou Central Hospital, Wenzhou 325000, Zhejiang, China)
出处
《中国临床药理学与治疗学》
CAS
CSCD
2017年第11期1237-1243,共7页
Chinese Journal of Clinical Pharmacology and Therapeutics
基金
浙江省中医药资助项目(2015ZA195)
温州市公益性科技计划项目(Y20140746)
关键词
桂枝
白芍
配伍
药动学
芍药苷
Ramulus Cinnamomi
Radix Paeoniae Alba
compatibility
pharmacokinetics
paeoniflorin
