Plasma Levels of a Novel Antidysrhythmic Agent, Meobentine Sulfate, in Humans as Determined by Radioimmunoassay
作者:James T. Warren、Geoffrey G. Coker、Richard M. Welch、Arthur S.E. Fowle、John W.A. Findlay
DOI:10.1002/jps.2600710615
日期:1982.6
cross-reaction in radioimmunoassay procedures employing either tritiated or radioiodinated radioligands. The radioimmunoassay using[125I]meobentine was capable of detecting less than 0.4 ng/ml (40-pg mass) of meobentine. This assay was used to demonstrate the absorption of meobentine in humans after oral administration and also permitted studies of meobentinesulfate disposition in humanplasma following two
描述了一种用于定量硫酸美宾汀的放射免疫分析方法,硫酸美宾汀是一种生物流体中的新型抗心律失常和抗原纤化剂。响应于用牛血清白蛋白和甲氧基类似物与邻位甲氧基的丙酸侧链的结合物进行免疫,在兔中产生抗血清。这些抗血清对N-和O-去甲基美宾汀代谢物的亲和力很低,在使用tri化或放射性碘标记的放射性配体的放射免疫分析方法中,交叉反应的结合率不到5%。使用[125I]美宾汀的放射免疫分析能够检测到少于0.4 ng / ml(40 pg质量)的美宾汀。该试验用于证明口服后人体中美宾汀的吸收,并且还允许研究两次之后人血浆中硫酸美宾汀的处置(2。5和5 mg / kg)口服剂量。在两种情况下,血浆中美宾汀的平均峰值浓度均在给药后3小时出现,在2.5和5 mg / kg剂量后分别为230和451 ng / ml。所有治疗后的平均终末半衰期约为12小时。