AN EVALUATION OF MAPROTILINE INTRAVENOUS KINETICS AND COMPARISON OF 2 ORAL DOSES
AN EVALUATION OF MAPROTILINE INTRAVENOUS KINETICS AND COMPARISON OF 2 ORAL DOSES
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DOI：
10.1007/bf00563007
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发表时间：
1980-01-01
影响因子：
2.9
通讯作者：
SCOGGINS, BA
中科院分区：
文献类型：
--
作者：
MAGUIRE, KP;NORMAN, TR;SCOGGINS, BA
在快速静脉注射后，对 6 名正常志愿者进行了去甲肾上腺素摄取抑制剂马普替林的动力学评估。给药75毫克。血液水平可以使用双指数方程来解决。半衰期、分布容积和全身清除率的平均估计值为 40.+-。 15 小时，51.7 .+-。 18.0 升/千克和 0.92 .+-。分别为 0.241 升/千克每小时。受试者之间的血液/血浆浓度在 0.77-1.64 之间变化。在同一志愿者中对 2 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，2 个剂量获得的马普替林浓度之间没有观察到显着差异。 2 个剂量的浓度与时间曲线下面积没有发现显着差异。可以假定等效的生物利用度。基于静脉注射。注射研究显示，75 mg 片剂和三片 25 mg 片剂的全身生物利用度平均分别为 66% 和 70%。
The kinetics of the norepinephrine uptake inhibitor maprotiline were evaluated in 6 normal volunteers following rapid i.v. 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 .+-. 18.0 l/kg and 0.92 .+-. 0.241 l/kg per h, respectively. Blood/plasma concentrations varied between subjects from 0.77-1.64. A comparison of the bioavailability of 2 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 2 doses at sampling times up to 26 h. No significant difference was found in the area under the concentration vs. time curves for the 2 doses. Equivalent bioavailability can be assumed. Based on the i.v. injection study, systemic bioavailability averaged 66% and 70% for the 75 mg and three 25 mg tablets, respectively.