A Novel Use of RIA and HPLC in the Identification of Plasma Metabolites of HR 158

作者: J. D. Robinson , I. D. Wilson , C. D. Bevan , J. Chamberlain

DOI: 10.1007/978-1-4684-4484-1_15

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摘要: The benzodiazepine HR 158 is active at dose levels of 1 mg, resulting in peak plasma 5–6 ng/ml. Although radio-labelled metabolism studies animals had indicated the nature main metabolites, these could not be confirmed man due to obligatory low doses. Moreover, conventional modes analysis such as HPLC or GC were too insensitive for metabolite detection and identification human plasma. high sensitivity radioimmunoassay (RIA) was used overcome this problem. Of two antisera available, one highly specific furnishing similar those found by a method, non-specific yielding much higher values thus indicating presence cross-reacting metabolites. latter on eluate fractions an system capable separating known putative metabolites RIA-chromatogram allowed ng/ml level.

参考文章(1)
JD Robinson, BA Morris, GW Aherne, V Marks, Pharmacokinetics of a single dose of phenytoin in man measured by radioimmunoassay. British Journal of Clinical Pharmacology. ,vol. 2, pp. 345- 349 ,(1975) , 10.1111/J.1365-2125.1975.TB02782.X