摘要
目的建立大鼠血浆中丹参酮ⅡA和隐丹参酮的HPLC-UV检测法,并研究丹参脂溶性成分在大鼠体内的药动学。方法以吉非罗齐为内标,血浆样品经简单的甲醇沉淀蛋白后,上清液直接进样测定。大鼠尾iv丹参醇提取物(以丹参酮ⅡA计为5 m g/只),测定各时点丹参酮ⅡA和隐丹参酮的血药浓度,绘制药-时曲线,采用3p87计算药动学参数。结果大鼠尾iv丹参醇提取物后,丹参酮ⅡA的主要药动学参数分别为:t1/2α为(0.088±0.024)h,t1/2β为(2.1±0.7)h;VC为(0.8±0.6)L;CL为(2.0±1.1)L/h-1;AUC0-4和AUC0-∞分别为(2.2±0.9)m g.h/L和(3.4±1.7)m g.h/L。结论丹参醇提取物iv给药后,丹参酮ⅡA的药-时曲线符合二室模型,血浆中丹参酮ⅡA迅速下降,表观分布容积大;隐丹参酮在血浆中消除快,药动学参数不易获得。
Objective To establish a sensitive HPLC method with UV detection for the determination of tanshinone ⅡA（TS ⅡA） and cryptotanshinone （CT） in rat plasma and to study pharmacokinetics of Radix Salviae Miltiorrhizae （RSM） liposoluble components in rat in viva. Methods TS ⅡA and CT in plasma of rat at different sampling time were determined by pretreatment with Gemifibrozil as internal standard, the protein was precipitated in methanol solution after iv administration of alcohol extract of RSM 5 mg/per animal. The mean plasma concentration-time curve was protracted and pharmacokinetic parameters were calculated by 3p87. Results The main pharmacokinetic parameters of TS ⅡA were as follows： t1/2α was （0. 0884±0. 024） h; t1/2β was （2.1±0.7） h; Vc was （0.84±0.6） L; CL was （2.04±1.1） g/h^-1 AUC0-4 and AUC0. were （2.2 4±0. 9） mg · h/L and （3.4 ± 1.7） mg · h/L, respectively. Conclusion The concentration-time curve of TS ⅡA can be fitted to two-compartment model after ethanol extract of RSM iv administrated. Concentration of TS ⅡA in rat plasma declines rapidly with large apparent volume of distribution. CT decreases also rapidly and it is difficult to acquire its pharmacokinetic parameters in rat.
出处
《中草药》
CAS
CSCD
北大核心
2005年第10期1480-1482,共3页
Chinese Traditional and Herbal Drugs
基金
国家自然科学基金资助项目(3007093530271614)
关键词
丹参
丹参醇提取物
丹参酮ⅡA
隐丹参酮
药动学
高效液相色谱
Radix Salvia Miltiorrhiza （RSM）
alcohol extract of Salvia Miltiorrhiza Radix（AERSM） tashinone ⅡA （TS ⅡA）
cryptotanshinone （CT）
pharmacokinetics
HPLC
作者简介
李莉（1979-），四川内江人，药学硕士，主要从事新药开发研究工作。Tel： （028）80989144 E-mail： lily_309@163.com
通讯作者 蒋学华 （028）85501370 E-mail：jxh1013@163.com
