Chem. Pharm. Bull. 55(5) 753—756 (2007)

derivative of tanshinone IIa, which is the main lipophilic component contained in Salvia miltiorrhiza known as ‘Danshen’ in traditional Chinese medicine. The pharmacological activity of STS is due to tanshinone IIA, which is a cardioprotective substance and may exert a beneficial effect on the clinically important vascular endothelium. The use of tanshinone IIA is limited by its poor water solubility. STS injection was thus developed and have been used successfully in China to treat patients with coronary artery disease and angina pectoris for more than 30 years. Clinical evidence and pharmacological researches showed that STS was effective in the therapy of various cardiovascular diseases. Subsequent extensive research suggested that STS also has wide pharmacological effects such as acts against adriamycin-induced lipid peroxidation, attenuates hypertrophy induced by angiotensin II in cultured neonatal rat cardiac cells, protects ischemia-reperfusion injury through an electron transfer reaction in rat heart mitochondria against forming reactive oxygen radicals and blocks calcium channel. The chemical structure of STS is illustrated in Fig. 1. As compared with the extensive research of pharmacological effects of STS, few studies have dealt with its pharmacokinetics and biodistribution, which is essential to understand physiological disposition of STS. Previous study has demonstrated that we developed the ion-pair reversed-phase HPLC method for determination of STS in mouse plasma. In this study, we validated the ion-pair RP-HPLC method for determination of sodium tanshinone IIA sulfonate in various biological samples, and applied the method for further pharmacokinetics and biodistribution of intravenously administrated STS in mice.