香叶木苷对格列苯脲在大鼠体内药动学的影响

Effect of Diosmin on Pharmacokinetics of Glibenclamide in Rats

关键词:  香叶木苷  格列苯脲  药动学  药物相互作用

Key words:  diosmin  glibenclamide  pharmacokinetics  drug-drug interactions(DDI)

摘要:

目的 考察香叶木苷在大鼠体内对格列苯脲药动学的影响。方法 12只SD大鼠随机分为香叶木苷组和对照组，分别给予香叶木苷（325 mg·kg^-1，ig，qd）和同体积CMC-Na溶液7 d后，灌胃给予格列苯脲，于不同时间点采集血浆样品，测定血药浓度，DAS 2.0计算主要药动学参数，并进行统计学分析。结果 与对照组比，香叶木苷组C_max显著降低（P<0.05），t_max显著缩短（P<0.05），AUC_（0→t）和AUC_{（0→∞）}显著减少（P<0.05），CL显著增大（P<0.05），t_1/2差异不显著。结论 香叶木苷影响格列苯脲在大鼠体内的药动学过程，临床联合用药中应对格列苯脲的血药浓度进行监测，以避免潜在的药物相互作用风险。

Abstract:

OBJECTIVE To investigate the effect of diosmin on the pharmacokinetics of glibenclamide in rats. METHODS Twelve SD rats were randomly divided into the diosmin group and control group, which were administrated respectively with diosmin(325 mg·kg^-1, ig, qd) and CMC-Na solution for 7 d. Glibenclamide was given to the rats by intragastric administration. The plasma concentration of glibenclamide was determined. Main pharmacokinetic parameters were calculated by DAS 2.0 and analyzed statistically. RESULTS Compared with the control group, the C_max of the diosmin group was significantly lower(P<0.05), t_max was significantly shortened(P<0.05), the AUC_(0→t) and AUC_(0→∞) of glibenclamide were significantly lower(P<0.05), and the CL was significantly increased(P<0.05). There were no significant difference between the two groups of t_1/2. CONCLUSION Diosmin can affect the pharmacokinetics of glibenclamide in rats. To avoid the potential risk of drug interaction, the plasma concentration of glibenclamide shall be monitored when combination.