梓醇在大鼠体内的药代动力学和生物利用度研究  

Pharmacokinetics and bioavalibability of catalpol in rats

作　　者：武丽南[1,2] 陆榕[2] 谷元[2] 刘昌孝[2] 司端运[2] 

机构地区：[1]天津中医药大学 [2]天津药物研究院释药技术与药代动力学国家重点实验室,天津300193

出　　处：《中国临床药理学与治疗学》2012年第2期126-130,共5页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：国家重点基础研究发展计划项目(2010CB735602)

摘　　要：目的:研究梓醇在大鼠体内的药代动力学和生物利用度。方法:建立LC-MS/MS分析方法,应用Xcalibur 1.4数据处理工作站,以待测物(梓醇)与内标物(桃叶珊瑚苷)的色谱峰面积比计算大鼠灌胃50、100和200mg/kg和静脉注射50mg/kg梓醇后,各时间的血浆药物浓度。选用DAS 2.0软件计算药动学参数,t检验法统计实验数据,计算生物利用度。结果:梓醇在大鼠体内的药动学过程符合二室模型,大鼠灌胃50、100和200mg/kg梓醇后,AUC0→∞与剂量呈正比,t1/2与剂量无关;大鼠灌胃与静注50mg/kg梓醇后,AUC0→∞分别为(70±23)、(104±11)μg.h.mL-1,该剂量下梓醇的绝对生物利用度为66.7%。结论:梓醇的吸收和消除呈一级动力学特征,在大鼠体内的绝对生物利用度较高。AIM： To study the pharmacoki netics and bioavailability of catalpol in rats. METHODS. LC-MS/MS method was established for the quantitation of catalpol. The plasma con- centration of catalpol after i. g. administration of 50, 100 and 200 mg/kg dose of catalpol to six rats was calculated by peak area ratio of the determinated （catalpol） and the internal standard （aucubin） obtained by Xcalibur 1.4 program. The main pharmacokinetic parameters were obtained by DAS 2.0 program. The figures were checked by t text method, and calculated for bioavailability. RESULTS： The plasma concentratibn-time curve of catalpol conformed to two compartment model. After i. g. administration of 50, 100 and 200 mg/kg dose of catalpol, AUC0-∞ values increased in proportion to dose. tl/2 appeared to be independent of dose. Mean AUC0-∞ was （70 6 23） and （1046 11） μg·h. mL^-1 respectively after i. g. and i. v. administration of 50 mg/kg dose, the extent of bioavailability of catalpol was 66.7 %. CONCLUSION： The results of the pharmacokinetic study of catalpol showed that it exhibited first order kinetic characteristics and the bioavailability was satisfied.

关 键 词：梓醇 LC-MS/MS 药代动力学 生物利用度 

分 类 号：R969.1[医药卫生—药理学]