Greenblatt D J, Joyce T H, Comer W H, Knowles J A, Shader R I, Kyriakopoulos A A, MacLaughlin D S, Ruelius H W
Clin Pharmacol Ther. 1977 Feb;21(2):222-30. doi: 10.1002/cpt1977212222.
A single dose of 4 mg of lorazepam was injected into the deltoid muscles of six healthy male volunteers. Multiple venous blood samples were drawn during 48 hr after the dose and all urine was collected for 24 hr after the dose. Concentrations of lorazepam and its major metabolite, lorazepam glucuronide, were determined by electron-capture gas-liquid chromatography. Lorazepam was rapidly absorbed from the injection site, reaching peak concentrations within 3 hr. Mean pharmacokinetic pamrameters for unchanged lorazepam were: apparent absorption half-life: 21.2 min; elimination half-life: 13.6 hr; volume of distribution: 0.9 L/kg; total clearance: 58.2 ml/min. Lorazepam glucuronide rapidly appeared in plasma, reached peak concentrations within 12 hr of the dose, then was eliminated approximately in parallel with the parent drug. Within 24 hr a mean of 47.6% of the dose was recovered in the urine as lorazepam glucuronide and less than 0.5% was recovered as unchanged lorazepam.
向6名健康男性志愿者的三角肌注射4毫克单剂量劳拉西泮。给药后48小时内采集多份静脉血样，并在给药后24小时收集所有尿液。采用电子捕获气液色谱法测定劳拉西泮及其主要代谢产物劳拉西泮葡糖醛酸苷的浓度。劳拉西泮从注射部位迅速吸收，3小时内达到峰值浓度。未变化的劳拉西泮的平均药代动力学参数为：表观吸收半衰期：21.2分钟；消除半衰期：13.6小时；分布容积：0.9升/千克；总清除率：58.2毫升/分钟。劳拉西泮葡糖醛酸苷迅速出现在血浆中，给药后12小时内达到峰值浓度，然后与母体药物大致平行消除。24小时内，平均47.6%的剂量以劳拉西泮葡糖醛酸苷形式在尿液中回收，以未变化的劳拉西泮形式回收的不到0.5%。
