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血浆和尿液中奥芬溴铵灵敏放射受体测定法的开发。

Development of a sensitive radioreceptor assay for oxyphenonium in plasma and urine.

作者信息

Ensing K, Kluivingh F, Gerding T K, De Zeeuw R A

出版信息

J Pharm Pharmacol. 1984 Apr;36(4):235-9. doi: 10.1111/j.2042-7158.1984.tb04356.x.

Abstract

A radioreceptor assay (RRA) for oxyphenonium has been developed. It is based on competition between [3H]dexetimide and oxyphenonium for binding to muscarinic receptors from calf striata. The RRA is optimized towards incubation medium and to extraction by ion pair formation with sodium picrate. At least 4 X 10(-10) M of oxyphenonium is necessary to permit a reliable assay. This corresponds to a detection limit of drug of 2 ng ml-1 urine. After extraction, drug at 100 pg ml-1 of plasma can be estimated using 4 ml samples. The method is applicable to monitoring the drug and to the determination of its pharmacokinetics after therapeutic dosing. Urine levels can also be monitored.

摘要

已开发出一种用于奥芬溴铵的放射受体分析法(RRA)。它基于[3H]右甲吗南与奥芬溴铵竞争结合小牛纹状体中的毒蕈碱受体。该RRA针对孵育介质以及通过与苦味酸钠形成离子对进行萃取进行了优化。至少4×10⁻¹⁰ M的奥芬溴铵对于进行可靠的分析是必要的。这相当于尿液中药物的检测限为2 ng/ml。萃取后,使用4 ml血浆样本可以估算出血浆中100 pg/ml的药物。该方法适用于监测药物以及治疗给药后其药代动力学的测定。尿液水平也可以进行监测。

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