CAJ | 학술논문

试验研究了灌服单剂量喹赛多(40 mg/kg体重)后原药及其代谢物在健康猪体内的药代动力学特征.液相色谱—串联质谱法测定血浆中喹赛多及其代谢物的浓度,通过WinNonlin 5.2药代动力学软件分析,用非房室模型统计矩原理计算喹赛多及其代谢产物的药动学参数.主要药动学参数分别为喹赛多:t1/2(7.52±1.77)h,Cmax(0.02±0.01)μg/mL,AUC(0-36h)(0.26±0.24)(h·μg)/mL,MRT(11.37±3.21)h;N1(脱一氧喹赛多):t1/2(3.05±1.12)h,Cmmax(0.35±0.18)μg/mL,AUC(0-36 h)(2.13±2.31)(h·μg)/mL,MRT(11.83±3.34)h.N4(脱一氧喹赛多):t1/2(2.91±1.15)h,Cmax(0.60±0.32)μg/mL,AUC(0-36 h)(3.78±4.28)(h·μg)/mL,MRT(11.00±2.86)h.脱二氧喹赛多:t1/2(3.85±1.30)h,Cmax(0.46±0.19)μg/mL,AUC(0-36 h)(4.21±2.47)(h·μg)/mL,MRT(13.35±2.65)h.QCA(喹(噁)咻-2-羧酸):t1/2(5.08±0.57)h,Cmax(0.25±0.11)μg/mL,AUC(0-36 h)(3.05±1.46)(h· μg)/mL,MRT(15.15士1.83)h.结果表明,血浆中主要存在形式为代谢物,各代谢物的血药浓度及AUC(0-∞)均高于喹赛多,喹赛多消除半衰期最长,QCA平均滞留时间最长.
시험연구료관복단제량규새다(40 mg/kg체중)후원약급기대사물재건강저체내적약대동역학특정.액상색보—천련질보법측정혈장중규새다급기대사물적농도,통과WinNonlin 5.2약대동역학연건분석,용비방실모형통계구원리계산규새다급기대사산물적약동학삼수.주요약동학삼수분별위규새다:t1/2(7.52±1.77)h,Cmax(0.02±0.01)μg/mL,AUC(0-36h)(0.26±0.24)(h·μg)/mL,MRT(11.37±3.21)h;N1(탈일양규새다):t1/2(3.05±1.12)h,Cmmax(0.35±0.18)μg/mL,AUC(0-36 h)(2.13±2.31)(h·μg)/mL,MRT(11.83±3.34)h.N4(탈일양규새다):t1/2(2.91±1.15)h,Cmax(0.60±0.32)μg/mL,AUC(0-36 h)(3.78±4.28)(h·μg)/mL,MRT(11.00±2.86)h.탈이양규새다:t1/2(3.85±1.30)h,Cmax(0.46±0.19)μg/mL,AUC(0-36 h)(4.21±2.47)(h·μg)/mL,MRT(13.35±2.65)h.QCA(규(오)휴-2-최산):t1/2(5.08±0.57)h,Cmax(0.25±0.11)μg/mL,AUC(0-36 h)(3.05±1.46)(h· μg)/mL,MRT(15.15사1.83)h.결과표명,혈장중주요존재형식위대사물,각대사물적혈약농도급AUC(0-∞)균고우규새다,규새다소제반쇠기최장,QCA평균체류시간최장.