摘要
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。
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＆amp;nbsp;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.
出处
《中国医院用药评价与分析》
2015年第5期597-600,共4页
Evaluation and Analysis of Drug-use in Hospitals of China
