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目的探讨大鼠中白杨黄素和柚皮素与P-糖蛋白底物沙奎那韦同服时,对后者口服生物利用度及药动学的影响。方法将SD大鼠分为3组分别灌胃沙奎那韦(30 mg·kg~(-1))、沙奎那韦(30 mg·kg~(-1))+柚皮素(40 mg·kg~(-1))、沙奎那韦(30mg·kg~(-1))+白杨黄素(40 mg·kg~(-1)),采用LC-MS/MS测定给药后的血药浓度,计算药动学参数。结果沙奎那韦在沙奎那韦对照组,沙奎那韦+柚皮素组和沙奎那韦+白杨黄素组大鼠体内主要药动学参数分别为:AUC0-t,882.91,861.32,934.84ng·h·m L~(-1);AUC0-∞,903.97,865.90,947.92 ng·h·m L~(-1);ρmax,177.72,89.8,130.72 ng·m L~(-1);tmax,1,2,0.5 h;t1/2,11.73,12.61,13.33 h;MRT0-∞,27.09,31.63,26.60 h;CL/F,21.65,21.45,20.62 m L·kg~(-1)·h~(-1)。结论沙奎那韦的药时曲线存在双峰现象;柚皮素和白杨黄素对沙奎那韦的口服生物利用度和药动学参数没有显著性影响。
OBJECTIVE To investigate the effects of paclitaxel and naringin on the oral bioavailability and pharmacokinetics of the latter in the same dose of saqugamycin as the P-glycoprotein substrate. Methods SD rats were randomly divided into three groups: salquinavir (30 mg · kg -1), saquinavir (30 mg · kg -1) + naringenin (40 mg · Kg -1 -1), saquinavir (30 mg · kg -1) + chrysin (40 mg · kg -1) Blood concentration, calculate pharmacokinetic parameters. Results The major pharmacokinetic parameters of saquinavir in the saquinavir control group, saquinavir + naringenin group and the saquinavir + chlortixan group were AUC0-t, 882.91, 861.32, 934.84ng · h · m L -1; AUC0-∞, 903.97,865.90,947.92 ng · h · m L -1; ρmax, 177.72,89.8,130.72 ng · m L -1 ; tmax, 1,2,0.5 h; t1 / 2,11.73,12.61,13.33 h; MRT0-∞, 27.09,31.63,26.60 h; CL / F, 21.65,21.45,20.62 m L · kg -1 · H ~ (-1). Conclusions Saquinavir has a bimodal pharmacokinetic profile. Naringenin and chrysin has no significant effect on oral bioavailability and pharmacokinetic parameters of saquinavir.