Pharmacokinetics of alcohol extract of Radix Salviae Miltiorrhiaze in rat in vivo / 中草药

ABSTRACT

Objective To establish a sensitive HPLC method with UV detection for the determination of tanshinone Ⅱ_A(TSⅡ_A) and cryptotanshinone(CT) in rat plasma and to study pharmacokinetics of Radix Salviae Miltiorrhizae(RSM) liposoluble components in rat in vivo. Methods TS Ⅱ_A 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 Ⅱ_A were as follows t_(1/2?) was(0.088?0.024) h;t_(1/2?) was(2.1?0.7) h;V_C was(0.8?0.6) L;CL was(2.0?1.1) L/h~(-1);AUC_(0-4) and AUC_(0-∞) were(2.2?0.9) mg?h/L and(3.4?1.7) mg?h/L,respectively.Conclusion The concentration-time curve of TS Ⅱ_A can be fitted to two-compartment model after ethanol extract of RSM iv administrated.Concentration of TS Ⅱ_A 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.