CAJ | 학술논문

目的：建立液相色谱-质谱／质谱联用法（ LC-MS／MS）测定人血浆中苯唑西林的浓度，研究苯唑西林钠胶囊与参比制剂苯唑西林钠胶囊（奇菲）的生物等效性。方法：采用随机、单剂量、双交叉对照试验设计，20名男性健康志愿者空腹口服受试及参比制剂1000 mg，采用蛋白沉淀法处理血浆样品，使用LC-MS／MS法测定血浆中苯唑西林的浓度，并以DAS 2.0软件进行方差分析及双单侧t检验，判断2种制剂是否具有生物等效性。结果：口服受试及参比制剂后，血浆中苯唑西林峰浓度（Cmax）分别为（17.0±2.77）、（15.5±3.46）μg／ml；达峰时间（tmax）分别为（0.63±0.14）、（0.72±0.26）h；药时曲线下面积（AUC0～6 h）分别为（22.52±4.38）、（22.54±5.79）μg／（ml· h）；受试制剂的相对生物利用度为（102.8±19.3）％。结论：受试制剂与市售参比制剂具有生物等效性。
목적：건립액상색보-질보／질보련용법（ LC-MS／MS）측정인혈장중분서서림적농도，연구분서서림납효낭여삼비제제분서서림납효낭（기비）적생물등효성。방법：채용수궤、단제량、쌍교차대조시험설계，20명남성건강지원자공복구복수시급삼비제제1000 mg，채용단백침정법처리혈장양품，사용LC-MS／MS법측정혈장중분서서림적농도，병이DAS 2.0연건진행방차분석급쌍단측t검험，판단2충제제시부구유생물등효성。결과：구복수시급삼비제제후，혈장중분서서림봉농도（Cmax）분별위（17.0±2.77）、（15.5±3.46）μg／ml；체봉시간（tmax）분별위（0.63±0.14）、（0.72±0.26）h；약시곡선하면적（AUC0～6 h）분별위（22.52±4.38）、（22.54±5.79）μg／（ml· h）；수시제제적상대생물이용도위（102.8±19.3）％。결론：수시제제여시수삼비제제구유생물등효성。
OBJECTIVE:To determine human plasma concentration of oxacillin by liquid chromatography -mass spectrometry ( LC-MS/MS ) and study the bioequivalence of the tested and the standard preparations of oxacillin sodium capsules.METHODS:In a randomized, single dose and double crossover design, 20 healthy male volunteers were administered orally with tested and reference oxcillin sodium capsules ( 1 000 mg ) .The plasma samples were treated by of protein precipitation method, and the plasma concentrations of oxacillin within 6 hours after administration were determined by LC-MS/MS;DAS 2.0 software was employed for analysis of variance and two one-sided t-test for evaluation of the bioequivalence of the two preparations.RESULTS: After oral administration of the tested vs. reference preparations, peak plasma concentration (Cmax) of oxacillin stood at (17.0 ±2.77) vs.(15.5 ±3.46) μg/ml, with tmax of (0.63 ±0.14) vs.(0.72 ±0.26) h, and area under the concentration-time curve (AUC0-6 h) of (22.52 ±4.38) vs.(22.54 ±5.79) μg/(ml· h).The relative bioavailability of the tested preparation was (102.8 ± 19.3)%.CONCLUSIONS:The tested oxacillin sodium capsules and the reference preparation are bioequivalent.