Maguire K P, Norman T R, Burrows G D, Scoggins B A
Eur J Clin Pharmacol. 1980 Oct;18(3):249-54. doi: 10.1007/BF00563007.
The kinetics of maprotiline have been evaluated in six normal volunteers following rapid intravenous administration of 75 mg. Blood levels could be resolved using a biexponential equation. Mean estimates of half-life, volume of distribution and systemic clearance were 40 +/- 15 h, 51.7 +/- 18.01/kg and 0.92 +/- 0.24/kg/h, respectively. Blood/plasma concentrations varied between subjects from 0.77 to 1.64. A comparison of the bioavailability of two oral doses (a 75 mg tablet and three 25 mg tablets) was carried out in the same volunteers. No significant difference was observed between the maprotiline concentrations obtained for the two doses at sampling times up to 26 h. No significant difference was found in the area under the concentration vs. time curves for the two doses. Equivalent bioavailability can be assumed. On the basis of the intravenous injection study, systemic bioavailability averaged 66% and 70% for the 75 mg and three 25 mg tablets respectively.
在6名正常志愿者快速静脉注射75毫克后，对马普替林的动力学进行了评估。血药浓度可用双指数方程解析。半衰期、分布容积和全身清除率的平均估计值分别为40±15小时、51.7±18.0升/千克和0.92±0.24升/千克/小时。受试者之间的血药/血浆浓度在0.77至1.64之间变化。在相同志愿者中对两种口服剂量（一片75毫克片剂和三片25毫克片剂）的生物利用度进行了比较。在长达26小时的采样时间内，两种剂量的马普替林浓度之间未观察到显著差异。两种剂量的浓度-时间曲线下面积未发现显著差异。可以假定生物利用度相当。根据静脉注射研究，75毫克片剂和三片25毫克片剂的全身生物利用度平均分别为66%和70%。
