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口服利尿药安体舒通是受“首过作用”影响较大的药物,Overdiek对空腹及进食后安体舒通及其代谢物的体内动态进行了研究。 9名健康受试者,分别在禁食过夜后空腹时及进晨餐后口服安体舒通200 mg,两试验间至少停药1周。在服药后24小时内于一定的时间间隔采集血标本,用HPLC法测定血中安体舒通及其代谢物浓度及药动学参数。试验结果,安体舒通的血药浓度-时间曲线下面积(AUC),空腹时为288±13 ng·h/ml,进食后为493±105 ng·h/ml。三种代谢物(7α-硫甲基安体舒通,6β-羟基-7α-硫甲
Oral diuretic spironolactone is a “first pass” effect of a larger drug, Overdiek fasting and after eating spironolactone and its metabolites in vivo dynamics were studied. Nine healthy subjects were given spironolactone 200 mg orally and fasting for at least one week after stopping fasting. Serum samples were collected within a certain time interval within 24 hours after taking the drug, and spironolactone and its metabolites concentrations and pharmacokinetic parameters were determined by HPLC. Test results, spironolactone plasma concentration-time area under the curve (AUC), fasting 288 ± 13 ng · h / ml, after eating 493 ± 105 ng · h / ml. Three metabolites (7α-thiomethyl spironolactone, 6β-hydroxy-7α-thiourea