Pharmacokinetic Differences of Three Aconitum Alkaloids from Aconiti lateralis Radix Praeparata and Compatibility with Pinellia in Rats

Abstract:

Aim: This study aims to develop a highly sensitive and specific UPLC-MS/MS method to explore the pharmacokinetic properties of three representative active alkaloids (benzoylhypaconine, benzoylmesaconine, benzoylaconine) after administration of extracts of Aconiti lateralis Radix Praeparata and compatibility with Pinellia, compare the influence of Pinellia on pharmacokinetic characterization of three aconitum alkaloids. Methods: Chromatographic separation were performed on a C₁₈ column under the multiple reaction monitoring (MRM) in the positive electrospray ionization (ESI) mode. The pharmacokinetic parameters were evaluated by software DAS 3. 0. Results: The specificity, precision and accuracy,matrix effect and extraction recovery rate and stability all meet the requirements.The validation of the method was achieved in accordance to the FDA guidelines. After oral administration of the extract, similar tendency was found in the mean concentration of the three analytes in the curves, illustrating that three analytes exhibited a similar absorption and metabolic route. Compared the pharmacokinetic characteristics, the AUC0_-t, AUC_0-∞ and C_max values of BMA and BHA in Fuzi group were lower than those in Fuzi-Banxia group. Conclusion: This finding indicated the significant statistical decrease (p<0.05) in the absorption of these components. After Banxia in combination with Fuzi, the results showed that faster absorption and higher exposure of BMA and BHA in rat plasma.

Key words: Pharmacokinetic, Aconiti lateralis Radix, Pinellia, Aconitum alkaloids, UPLC–MS/MS.