Comparison on pharmacokinetics and tissue distribution of tanshinone IIA lipid microsphere and sodium tanshinone IIA silate injection / 中草药

ABSTRACT

Objective: To compare the pharmacokinetics in rats and tissue distribution in mice of tanshinone IIA (TNS) lipid microsphere and sodium tanshinone IIA silate (STS) injection after iv injection. Methods: A sensitive and specific RP-HPLC method was established to determine the concentration of TSN and STS in rat plasma and mice tissue. The TSN and STS levels in plasma of rats and tissues of mice were compared after iv single dose administration of TSN lipid microsphere (5.40 mg/kg) and STS injection (7.27 mg/kg), and the results were fitted by pharmacokinetic and statistic analyses. Results: The bioavailability (AUC0-∞) and peak concentration (Cmax) values of TSN were 2.14 and 2.22 folds as those of STS, the clearance (CL), apparent volume of distribution (V), and mean repair time (MRT) values of TSN were lower (P < 0.01), and other pharmacokinetic parameters had no significant deviation. The results on the tissue distribution of TSN and STS in mice showed that the contents of TSN in heart, liver, spleen, lung, and kidney tissues were 1.94, 0.11, 0.98, 1.65, and 0.28 folds as those of STS with the same molar dose, and the content of TSN in brain tissue increased more significantly than that of STS which has not been detected. Conclusion: The pharmacokinetics and tissue distribution of TSN and STS at the same molar dose have significant differences, the AUC and Cmax values of TSN are higher, and the concentration of TSN could be increased in heart, brain, and lung tissues significantly, compared with those of STS.