Pharmacokinetics of main components in Salvia Miltiorrhizae Radix et Rhizoma diterpene quinones composition and its solid dispersion micro-pellets in rats in vivo / 中草药

ABSTRACT

Objective: To establish a UPLC-MS/MS method for determining the plasma concentration of dihydrotanshinone I, tanshinone I, cryptotanshinone, and tanshinone IIA in rats, and to study the pharmacokinetics of Salvia miltiorrhiza diterpene quinones composition (SMDQC) and its solid dispersion micro-pellets (SDMP). Methods: Sprague-Dawley rats were ig administered with SMDQC and its SDMP, respectively. Then the blood samples were obtained at different time points. Electrospray ionization (ESI) source was applied and operated in the positive ion mode. The plasma concentration of dihydrotanshinone I, tanshinone I, cryptotanshinone, and tanshinone IIA was then detected by UPLC-MS/MS, and the pharmcoknetic parameters were calculated by DAS 2.1.1 program. Results: The RSDs of intra- and inter-day precisions of all analytes were less than 14.6%, and the average recoveries of the four active constituents were more than 74.49%. The pharmacokinetic results showed that after ig administration of SDMP, Cmax and AUC0-∞ of the four active constituents increased significantly compared with those of SMDQC. Conclusion: The method has the high sensitivity and selectivity, and proves to be suitable for the pharmacokinetic study of SMDQC and its SDMP. The results show that the SDMP could enhance the solubility of SMDQC to improve its absorption. The relative bioavailability of the four representative constituents is 138%-204% of the crude drug.