CAJ | 학술논문

目的研究马来酸左旋氨氯地平分散片与马来酸左旋氨氯地平片在健康志愿者中的相对生物利用度和生物等效性.方法采用双周期、随机、交叉试验设计,20例男性健康受试者随机分成两组,单剂量、交叉口服受试制剂马来酸左旋氨氯地平分散片和参比制剂马来酸左旋氨氯地平片5mg,采集不同时间点的静脉血样,用LC-MS/MS法(液相色谱-串联质谱法)测定给药后不同时间左旋氨氯地平的血药浓度.结果马来酸左旋氨氯地平分散片与马来酸左旋氨氯地平片(对照药)的Tmax分别为(5.8±2.4)h和(6.6±2.6)h;Cmax分别为(3.7±0.9)ng/mL和(3.8±1.0)ng/mL;AUC0→120分别为(173.7±37.9)ng/(h·mL)和(176.6±40.2)ng/(h·mL);AUC0→∞分别为(214.8±56.8)ng/(h·mL)和(219.3±58.8)ng/(h·mL).受试制剂对参比制剂的相对生物利用度F为99%±6%(85%~110%).统计分析结果表明二者在不同制剂间和不同周期间差异无显著性意义(P>0.05).结论马来酸左旋氨氯地平分散片与马来酸左旋氨氯地平片参比制剂具有生物等效性.
목적연구마래산좌선안록지평분산편여마래산좌선안록지평편재건강지원자중적상대생물이용도화생물등효성.방법채용쌍주기、수궤、교차시험설계,20례남성건강수시자수궤분성량조,단제량、교차구복수시제제마래산좌선안록지평분산편화삼비제제마래산좌선안록지평편5mg,채집불동시간점적정맥혈양,용LC-MS/MS법(액상색보-천련질보법)측정급약후불동시간좌선안록지평적혈약농도.결과마래산좌선안록지평분산편여마래산좌선안록지평편(대조약)적Tmax분별위(5.8±2.4)h화(6.6±2.6)h;Cmax분별위(3.7±0.9)ng/mL화(3.8±1.0)ng/mL;AUC0→120분별위(173.7±37.9)ng/(h·mL)화(176.6±40.2)ng/(h·mL);AUC0→∞분별위(214.8±56.8)ng/(h·mL)화(219.3±58.8)ng/(h·mL).수시제제대삼비제제적상대생물이용도F위99%±6%(85%~110%).통계분석결과표명이자재불동제제간화불동주기간차이무현저성의의(P>0.05).결론마래산좌선안록지평분산편여마래산좌선안록지평편삼비제제구유생물등효성.
Objective To study the pharmacokinetics and bioavailability of levamlodipine maleate dispersible tablets in health in healthy volunteers. Methods Healthy volunteers were orally given a single dose of 5 mg of two different formulations of levamlodipine maleate in an open randomized cross-over test. The levamlodipine concentration in plasma was determined by LC-MS/MS method. Results The peak time (tmax) of levamlodipine maleate dispersible tablets and levamlodipine maleate tablets were (5.8±2.4)h and(6.6±2.6)h, the pesk plassmal levels (Cmax) were(3.7±0.9)ng/mL and (3.8±1.0)ng/mL, and AUC0→120 were(173.7±37.9)ng/(h·mL) and(176.6±40.2)ng/(h·mL), AUC0→∞were(214.8±56.8)ng/(h·mL) and (219.3±58.8)ng/(h·mL). The relative bioavailability was (99%±6)%(85%~110%). Conclusion Levamlodipine maleate dispersible tablets and levamlodipine maleate tablets were bioequivalent.