Pierce D M, Franklin R A, Harry T V, Nicholson A N
Br J Clin Pharmacol. 1984 Jul;18(1):31-5. doi: 10.1111/j.1365-2125.1984.tb05018.x.
The bioavailability, pharmacokinetics, and effects on performance of lormetazepam (1 mg) have been compared using soft gelatin capsule and tablet formulations. Lormetazepam was more rapidly absorbed from the soft gelatin capsule (tmax = 1.0 +/- 0.2 h) than from the tablet (tmax = 2.4 +/- 0.4 h), and the plasma concentration-time curve for the capsule was shifted to the left. Bioavailability and elimination kinetics did not differ between the formulations. The number of substitutions in the digit symbol test was reduced between 0.5 and 1.5 h for both formulations (P less than 0.001), but the degree of impairment at 0.5 h was greater after the capsule than after the tablet (P less than 0.01). Visuo-motor co-ordination was impaired from 0.5 to 1.5 h after the tablet and the capsule (P less than 0.01), and extended to 5.5 h after the tablet (P less than 0.05). These observations reflect the differences in the plasma concentration-time curves.
已使用软胶囊和片剂剂型比较了氯硝西泮（1毫克）的生物利用度、药代动力学及其对行为表现的影响。氯硝西泮从软胶囊中的吸收速度（达峰时间tmax = 1.0±0.2小时）比从片剂中的吸收速度（tmax = 2.4±0.4小时）更快，且软胶囊的血浆浓度-时间曲线向左偏移。两种剂型的生物利用度和消除动力学无差异。两种剂型在0.5至1.5小时之间数字符号测试中的替代次数均减少（P<0.001），但在0.5小时时，软胶囊后的损害程度大于片剂后（P<0.01）。片剂和软胶囊后0.5至1.5小时视觉运动协调能力受损（P<0.01），片剂后该损害持续至5.5小时（P<0.05）。这些观察结果反映了血浆浓度-时间曲线的差异。
