Russell W L, Lopez L M, Normann S A, Doering P L, Guild R T
Dig Dis Sci. 1984 May;29(5):385-9. doi: 10.1007/BF01296210.
The purpose of this study was to evaluate effects of antacids on predicted steady-state concentrations of cimetidine. Ten healthy volunteers received in random order one week apart, cimetidine and cimetidine and antacid suspension. Blood was obtained at specified times and analyzed for cimetidine. Bioavailability was assessed by comparison of peak concentration, time to peak concentration, area under the curve, and time spent over 0.5 micrograms/ml. Single-dose data were extrapolated to steady-state using computer simulation. Concurrent administration of antacid suspension reduced parameters of bioavailability approximately 30%. When steady-state conditions were simulated, concentrations of cimetidine greater than or equal to 0.5 micrograms/ml were maintained for the entire dosing interval in seven of 10 subjects. These data suggest that temporal separation of cimetidine and antacid suspension may be unnecessary.
本研究的目的是评估抗酸剂对西咪替丁预测稳态浓度的影响。10名健康志愿者按随机顺序,每隔一周分别接受西咪替丁以及西咪替丁与抗酸剂混悬液。在特定时间采集血液并分析其中的西咪替丁。通过比较峰浓度、达峰时间、曲线下面积以及血药浓度超过0.5微克/毫升的持续时间来评估生物利用度。使用计算机模拟将单剂量数据外推至稳态。同时服用抗酸剂混悬液使生物利用度参数降低了约30%。当模拟稳态条件时,10名受试者中有7名在整个给药间隔期内西咪替丁浓度维持在大于或等于0.5微克/毫升。这些数据表明西咪替丁与抗酸剂混悬液可能无需分开服用。