黄芩苷对大鼠口服非索非那定的药动学影响

为了研究黄芩苷在大鼠体内对非索非那定药动学及P-gp表达的影响，将SD大鼠36只随机分为A、B、C三组，连续灌胃7天，A组给予黄芩苷200mg/kg，B组蒸馏水空白对照，C组维拉帕米药物对照(10mg/kg)，第8天灌胃后2小时，各组随机取6只大鼠处死，解剖并迅速取出肝脏、空肠，荧光定量PCR测定各组织P-gp的mRNA表达水平。各组另外6只大鼠灌胃后同时给予非索非那定（30mg/kg），按时间点连续采集血样，采用高效液相色谱法测定非索非那定血药浓度。结果表明，黄芩苷对非索非那定的吸收有明显促进作用，主要表现在黄芩苷组非索非那定峰浓度(Cmax)比空白对照组增加17.04%（P<0.05），曲线下面积AUC(0-12)增加19.23%（P<0.05），黄芩苷减少了大鼠空肠和肝脏P-gp蛋白的表达（P<0.05）。结论：黄芩苷能下调大鼠P-gp表达，增加P-gp底物非索非那定在大鼠体内的生物利用度，是一种P-gp抑制剂。

Effects of baicalin on pharmacokinetics of fexofenadine in rats in vivo

To investigate effects of baicalin on the pharmacokinetics of fexofenadine in rats in vivo, and evaluate the effect of baicalin on expression of P-gp mRNA.36 SD rats were randomly divided into A,B and C groups, rats in A group were administered with baicalin(200mg/kg), B with distilled water and C were verapamil (10mg/kg) for 7 days. On the 8 day, After 2 hours of administering with baicalin,distilled water and verapamil, 6 rats in every group were killed to collected the liver and jejunum. The rest of rats were administered with fexofenadine(30mg/kg) o. The concentrations of fexofenadine in plasma after administration were determined by HPLC and P-gp mRNA expression level of liver and jejunum were evaluated by real time PCR. After administered with baicalin, AUC(0-12) and Cmax of nifedipine were significantly increased which suggested that the bioavailability of nifedipine were obviously increased. The RT-PCR detection indicated that rats administered with baicalin can decrease the P-gp mRNA expression level in liver and jejunum.It is concluded that baicalin is an inhibitor of P-gp, and it can enhance the bioavailability of nifedipine and decrease the P-gp mRNA expression level significantly