Screening Of Effective Parts Of Qingre Mixture And Pharmacokinetics Of Heat - Clearing Granules

In this study, we studied the effective fractions of Qing-Re mixture (QR). We establish a method for simultaneous determining the assay of puerarin and baicalin by HPLC, which is simple, accurate and feasible, the linear rangers for puerarin and baicalin were 0.025～0.4μg and 0.25～4μg respectively. The contents of puerarin and baicalin in the fractions eluted by 40 % ethanol were the most, which were 0.541 and 12.403 mg·mL-1 respectively. Animal models of ear edema induced by xylene in mice, paw edema induced by egg white and fever induced by 2,4-dinitrophenol in rats and endotoxin in rabbits were made to investigate the fever-relieving and anti-inflammatory effects of the different fractions of QR for oral use. The 20%、40 %and 60% ethanol extraction fractions of Qing-Re mixture showed a marked suppressive effects, the 40% fraction of Qing-Re mixture was the most, and had same effect on the anti-inflammation and fever-relieving as Qing-Re mixture.In this study, we studied the pharmacokinetic characteristics of Qing-Re guanule. Following ig Qing-Re guanule in dose 1.13 g-kg-1, in which 203.6 mg baicalin was contained, plasma concentrations were determined. The result showed that the pharmacokinetic model of baicalin was two compartments open model. The main pharmacokinetic parameters were as follows respectively:tmax1 were (0.40±0.15) h, tmax2 were (6.75±2.09) h, Cmax1 were (7.40±3.38)μg·mL-1, Cmax2 were (4.57±1.99)μg·mL-1,t1/2 were (12.51±3.87) h, Ke were (0.061±0.04) h-1, CL/F were (3.05±0.97) L·(h·kg)-1, Vd/F were (53.47±20.66) L·kg-1, AUC0-t were (62.08±20.30)μg·h·mL-1, AUC0-∞were (72.36±24.04)μg·h·mL-1. Following ig Qing-Re guanule in dose 3.40 g·kg-1, in which 30.3 mg puerarin was contained, plasma concentrations were determined. The result showed that the pharmacokinetic model of puerarin was one compartment open model. The main pharmacokinetic parameters were as follows respectively: tmax were (0.90±0.24) h, Cmax were (0.77±0.34)μg-mL-1,t1/2 were (1.82±0.42) h, Ke were (0.432±0.075) h-1, CL/F were (17.29±9.34) L·(h·kg)-1, Vd/F were (43.35±20.64) L·kg-1, AUC0-t were (2.00±0.82)μg·h·mL-1, AUC0-∞were (2.14±0.90)μg·h·mL-1.