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溴法罗明(CGP 11 305 A):与液相色谱法相比,采用生物学技术测定血浆浓度

Brofaromine (CGP 11 305 A): estimation of plasma concentrations by a biologic technique as compared to liquid chromatography.

作者信息

Fritze J, Becker T, Ziegler V, Laux G, Bieck P, Sofic E, Riederer P

机构信息

Department of Psychiatry and Clinical Neurochemistry, School of Medicine, University of Würzburg, Federal Republic of Germany.

出版信息

J Neural Transm Suppl. 1990;32:197-201. doi: 10.1007/978-3-7091-9113-2_29.

Abstract

In an open clinical trial 13 depressives significantly improved under the reversible and selective type-A monoamine oxidase (MAO) inhibitor brofaromine. The inhibitory potency of deproteinated plasma on a crude MAO preparation from human placenta was measured as a parameter for plasma brofaromine. There were no significant differences in plasma MAO inhibitory potency between responders (improvement greater than 50%; n = 5) and non-responders. MAO inhibitory potency significantly (p less than 0.05) increased parallel to the increase of the dosage from 50 mg b.i.d. to t.i.d. confirming the validity of this technique. The biologic assay, however, overestimated brofaromine by a factor of two in acute kinetic experiments with healthy volunteers as compared to a chromatographic technique, although both methods significantly correlated (r = 0.928).

摘要

在一项开放性临床试验中,13名抑郁症患者在可逆性和选择性A型单胺氧化酶(MAO)抑制剂溴法罗明的作用下病情显著改善。将脱蛋白血浆对人胎盘粗制MAO制剂的抑制效力作为血浆溴法罗明的一个参数进行测定。在有反应者(改善超过50%;n = 5)和无反应者之间,血浆MAO抑制效力没有显著差异。MAO抑制效力随着剂量从每日两次50毫克增加到每日三次而显著(p小于0.05)平行增加,证实了该技术的有效性。然而,与色谱技术相比,在对健康志愿者进行的急性动力学实验中,生物测定法将溴法罗明高估了两倍,尽管两种方法显著相关(r = 0.928)。

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