Preparation, Characterization Evaluation of Tanshinone IIA Lipid Microspere and Comparative Study of Pharmacokinetics with Sodium Tanshinone IIA Sulfonate Injection

In this study, Tanshinone IIA lipid microspere (Tan-IIA-LM) was successfully prepared by an ultrasonic and high-pressure homogenization method. The particle size, zeta potential, drug entrapment efficiency and morphological properties of Tan-IIA-LM were characterized in detail. A pharmacokinetic comparative study of Tan-IIA-LM with Sodium Tanshinone IIA Silate (STS) injection was developed. A sensitive and specific HPLC method was established to determine the mass concentration of Tan-IIA and STS in rats plasma samples which were compared between Tan-IIA-LM and STS injection after single dose intravenous administration of 18.35μmol/kg and the results were fitted and analyzed by dedicated software. After intravenous administration, the AUC0- and Cmax values of Tan-IIA were 2.14, 2.22 fold higher than STS. The clearance, apparent volume of distribution and mean residence time (MRT) of Tan-IIA were lower (P 0.05). The pharmacokinetic of Tan-IIA, STS have significant differences at the same molar doses and the AUC and Cmax values of Tan-IIA were higher compared with STS.