Locniskar A, Greenblatt D J, Zinny M A, Harmatz J S, Shader R I
J Clin Pharmacol. 1984 May-Jun;24(5-6):255-63. doi: 10.1002/j.1552-4604.1984.tb02782.x.
A series of healthy volunteers received a single 7.5-mg intravenous dose of diazepam on one occasion and a single 15-mg oral dose of slow-release diazepam (DZ-SR) on another occasion. Diazepam concentrations were measured by gas chromatography in multiple plasma samples drawn during seven days after each dose. Absorption of diazepam from DZ-SR was slow, with mean +/- S.E. peak concentrations attained at 3.8 +/- 0.5 hours after dosage. Absolute bioavailability of DZ-SR averaged 0.98 +/- 0.06. In two other studies, diazepam absorption from DZ-SR was evaluated when coadministered with a standard breakfast or with an antacid preparation (Maalox). Neither food nor antacid altered the rate of diazepam absorption and did not impair the completeness of absorption. Higher peak total plasma diazepam concentrations occurred in the postprandial as opposed to the fasting state, but this was an artifact of reduced protein binding (increased free fraction) due to fasting. Thus, diazepam absorption from DZ-SR is slow and essentially complete.
一组健康志愿者一次接受了7.5毫克地西泮静脉注射单剂量，另一次接受了15毫克缓释地西泮（DZ-SR）口服单剂量。在每次给药后的七天内采集多个血浆样本，通过气相色谱法测量地西泮浓度。DZ-SR中地西泮的吸收缓慢，给药后3.8±0.5小时达到平均±标准误的峰值浓度。DZ-SR的绝对生物利用度平均为0.98±0.06。在另外两项研究中，当与标准早餐或抗酸制剂（氢氧化铝镁）合用时，评估了DZ-SR中地西泮的吸收情况。食物和抗酸剂均未改变地西泮的吸收速率，也未损害吸收的完整性。与禁食状态相比，餐后出现更高的地西泮总血浆峰值浓度，但这是由于禁食导致蛋白质结合减少（游离分数增加）的假象。因此，DZ-SR中地西泮的吸收缓慢且基本完全。
