Stevens L A, Bevan C D, Salmon J, Krieger J, Perianu M, LeGo A
Eur J Clin Pharmacol. 1983;25(5):651-5. doi: 10.1007/BF00542354.
The pharmacokinetics of loprazolam have been studied in eight healthy male volunteers after single and repeated 2 mg oral doses taken at night, for eight nights. The absorption and disposition of unchanged drug (HPLC-GC assay) and receptor active benzodiazepine-type materials (radioreceptor assay) were examined after the first and eighth dose. Maximum levels of approximately 10 ng ml-1 (range 3.6 to 15.5 ng ml-1) were reached within about 2.5 h after dosing. The post-peak levels declined in a single exponential fashion with an overall mean +/- SD half-life of 7.06 +/- 1.98 h and total areas under the curve ranging from 35.9 to 189.0 ng ml-1 h. There were no statistical differences between the values for the first and eighth doses. There was no evidence to suggest that significant accumulation of parent drug or receptor active benzodiazepine-type materials had occurred, and it is concluded that the kinetics of loprazolam would allow repeated daily doses of 2 mg.
在8名健康男性志愿者中研究了氯普唑仑的药代动力学，他们在夜间单次及重复口服2mg剂量，共服用8晚。在首次和第八次给药后，检测了未变化药物（采用高效液相色谱-气相色谱法测定）和具有受体活性的苯二氮䓬类物质（采用放射受体分析法测定）的吸收和处置情况。给药后约2.5小时内达到约10ng/ml的最高血药浓度（范围为3.6至15.5ng/ml）。峰后血药浓度以单指数方式下降，总体平均±标准差半衰期为7.06±1.98小时，曲线下总面积范围为35.9至189.0ng/ml·h。首次和第八次给药的值之间无统计学差异。没有证据表明母体药物或具有受体活性的苯二氮䓬类物质发生了显著蓄积，得出的结论是氯普唑仑的药代动力学允许每日重复给予2mg剂量。
