[Effect of constituents combination on pharmacokinetics of Shuxiong tablet]

To study the effect of combination components on pharmacokinetics of Shuxiong tablet to provide evidence for the new recipe.

Six groups of rats (6 for each group) were orally administered with co-extractum of chuanxiong and honghua (CHE), mixed solution of hydroxysafflor yellow A (HSYA) and ferulic acid (FA) (HFM). Panax notoginseng saponins solution (PNS), mixed solution of PNS and CHE (PCHE), mixed solution of PNS and HFM (PHFM) and mixed emulsion of Chuanxiong volatile oil (CVO) and PHFM (CVO-PHFM), respectively. The concentrations of HSYA, FA, ginsnenoside Rg1 and Rb1 in rat plasma were determined by HPLC. Pharmacokinetic parameters (Ka, Kel, Cmax, Tmax and AUC) were calculated by model simulation. The differences of HSYA, FA, Rg1 and Rb1 in pharmacokinetics parameters after administration of six preparations were demonstrated by statistical analysis.

After oral administration of six preparations to rats, the concentration-time curve of HSYA and Rg1 fitted to one-compartment model, and that of FA fitted to double-compartment model. After oral administration of CHE, Kel of FA reduced; Cmax decreased; but K12 increased, significantly, compared with oral administration of HFM. Other parameters were not significant differences. After co-administration of PNS and CHE (PCHE) or PNS and HFM (PHFM), Ka of HSYA increased; Tmax reduced, significantly. After oral administration of PNS and HFM (PHFM), Ka of Rg1 improved, Tmax decreased, significantly. However, the parameters of FA and Rb1 were not significantly changed. After co-administration of CVO and PHFM (CVO-PHFM), Cmax of Rb1 decreased, K12 improved, significantly. Meanwhile, the oral bioavailability of HSYA, FA and Rg1 was improved by 6.056, 2.854 and 2.055 folds, respectively.

After oral administration of different combinations of Shuxiong tablet constituents, some pharmacokinetics parameters of active ingredients are significantly changed, but the bioavailability is improved only when CVO is co-administered.