Abstract:

AIM: To study the pharmacokinetics and bioequivalence of cryptotanshinone and its metabolites tanshinone IIA between traditional decoction piece and ultrafine granular powder of salvia miltiorrhiza.  METHODS: Twenty-four healthy volunteers, half male and half female were orally administrated with a single dose of subject drug (ultrafine granular powder of salvia miltiorrhiza) and reference drug (traditional decoction piece of salvia miltiorrhiza). Plasma concentrations of cryptotanshinone and tanshinone IIA were determined by a validated LC-MS method. Collected data were calculated and analyzed by DAS Ver3.2.2 and SPSS software. After logarithmic transformation of AUC _0-60 and C _max, one-sided t-test was performed and 90% confidence interval was calculated. RESULTS: The main pharmacokinetics parameters of cryptotanshinone and tanshinone IIA in subject drug and reference drug including T _max, C _max, AUC _0-60 and t _1/2 exhibited no significant difference (P>0.05) between different periods and different genders, while significant difference was observed between different preparations (P<0.05). The relative bioavailability of subject drug and reference drug were as follow:（4 456.8±3 706.8）%，(4 690.3±3 416.7) %. CONCLUSION: The bioavailability of cryptotanshinone and tanshinone IIA in ultrafine granular powder is significantly higher than traditional decoction piece, which is referential for reducing dosage in clinical application.

Key words: cryptotanshinone, tanshinone IIA, traditional decoction piece of salvia miltiorrhiza, ultrafine granular powder of salvia miltiorrhiza, pharmacokinetics, bioequivalence