CAJ | 학술논문

目的：以Beagle犬为模型考察自制左乙拉西坦缓释片与参比缓释片（Keppra XR）在动物体内的生物等效性。方法 Beagle犬分别单剂量口服自制缓释片与参比制剂1000 mg ，采用LC‐MS／MS方法测定犬血浆中左乙拉西坦的浓度，通过药代动力学计算软件WinNonlin 5．2以非房室模型分别计算左乙拉西坦的药代动力学参数。结果自制缓释片与市售参比缓释片单剂量口服后，左乙拉西坦的达峰时间 tmax分为1．67 h和3．0 h ；峰浓度Cmax分别为89．50μg／ml和71．18μg／ml；消除半衰期 t1／2分别为3．68 h和3．50 h；药时曲线下面积AUC（0‐48）分别为826．57μg?h／ml和757．84μg?h／ml；药时曲线下面积AUC（0‐∞）分别为826．68μg?h／ml和757．93μg?h／ml。与参比缓释片相比，自制左乙拉西坦缓释片的相对生物利用度为109．07％。结论初步判定两种制剂在犬体内具有类似的药代动力学特征和生物等效性。
목적：이Beagle견위모형고찰자제좌을랍서탄완석편여삼비완석편（Keppra XR）재동물체내적생물등효성。방법 Beagle견분별단제량구복자제완석편여삼비제제1000 mg ，채용LC‐MS／MS방법측정견혈장중좌을랍서탄적농도，통과약대동역학계산연건WinNonlin 5．2이비방실모형분별계산좌을랍서탄적약대동역학삼수。결과자제완석편여시수삼비완석편단제량구복후，좌을랍서탄적체봉시간 tmax분위1．67 h화3．0 h ；봉농도Cmax분별위89．50μg／ml화71．18μg／ml；소제반쇠기 t1／2분별위3．68 h화3．50 h；약시곡선하면적AUC（0‐48）분별위826．57μg?h／ml화757．84μg?h／ml；약시곡선하면적AUC（0‐∞）분별위826．68μg?h／ml화757．93μg?h／ml。여삼비완석편상비，자제좌을랍서탄완석편적상대생물이용도위109．07％。결론초보판정량충제제재견체내구유유사적약대동역학특정화생물등효성。
Objective To study the bioequivalence of two kinds of levetiracetam extended‐release tables including the ref‐erence product of Keppra XR in Beagle dogs .Methods Dogs were administrated orally with single dose of levetiracetam tablets (1 000 mg) .The concentration of levetiracetam in dog plasma was detected by LC‐MS/MS .All parameters of pharmacokinetics were performed by WinNonlin 5 .2 software .Results Main pharmacokinetic parameters of test and reference tablets were as follow :tmax were 1.67 h and 3 .0 h ,Cmax were 89 .50 μg/ml and 71 .18 μg/ml ,t1/2 were 3 .68 h and 3 .50 h ,AUC(0‐48) were 826 .57 μg?h/ml and 757 .84 μg?h/ml ,AUC(0‐∞ )were 826 .68 μg?h/ml and 757 .93 μg?h/ml .The relative bioavailability of test tablets was 109 .07% to reference products of Keppra XR .Conclusion Therefore ,the two kinds of levetiracetam extended‐release tablets were bioequivalent in Beagle dogs .