PMID: 6109770Dec 1, 1980Paper

Radioimmunoassay for terfenadine in human plasma

Journal of Pharmaceutical Sciences
C E CookG J Wright

Abstract

A radioimmunoassay procedure was developed for the antihistamine terfenadine (alpha[4-(1,2-dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol). The keto analog of terfenadine was converted to its O-carboxymethyloxime derivative, which was conjugated to bovine thyroglobulin by a mixed anhydride technique. Rabbits were immunized with the resulting conjugate, and antiserums capable of binding radiolabeled terfenadine were obtained. Tritium-labeled terfenadine was prepared by a combination of exchange and reduction with platinum oxide in the presence of tritium gas, and the procedure yielded a specific activity of 48 Ci/mmole. Plasma containing terfenadine was diluted with sodium carbonate solution and extracted with hexane, and the hexane extracts were evaporated and analyzed. The between-assay coefficient of variation on control samples ranged from 8% at 10 ng/ml to 14% at 1 ng/ml. The lower practical sensitivity limit was at least as low as 0.25 ng/ml (25 pg measured). Two metabolites of terfenadine cross-reacted 16-30% with the antiserum used. However, extraction eliminated essentially all of these compounds. Analysis of plasma samples from human subjects given terfenadine showed marked intersubject variability...Continue Reading

References

Jan 1, 1978·Clinical Pharmacokinetics·T B Cooper
Nov 15, 1976·Clinica Chimica Acta; International Journal of Clinical Chemistry·B J Morris
Jan 1, 1975·Perspectives in Biology and Medicine·S Rodbard
Dec 1, 1971·The Journal of Clinical Endocrinology and Metabolism·J VaitukaitisG T Ross
Aug 1, 1964·Journal of Pharmaceutical Sciences·M FREIFELDERV PAPENDICK

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Citations

Jan 11, 1991·Chirality·K ZamaniL R Cantilena
Mar 1, 1988·Journal of Pharmacological Methods·K K MidhaM D Moore
Jan 1, 1987·Journal of Pharmaceutical and Biomedical Analysis·H N AlkaysiA A Badwan
Sep 1, 1996·Journal of Pharmaceutical and Biomedical Analysis·A XuJ Hulse
Apr 1, 1997·Clinical Biochemistry·J U EskolaT Korpela
Jan 1, 1987·Drug Metabolism Reviews·J W Findlay
Apr 1, 1981·Biopharmaceutics & Drug Disposition·R A OkerholmC E Cook
May 1, 1991·The British Journal of Psychiatry : the Journal of Mental Science·S R MarderJ Mintz
Jan 1, 1981·British Journal of Clinical Pharmacology·K K MidhaP K Yeung
Nov 1, 1985·Drug Intelligence & Clinical Pharmacy·C A CarterL A Rickman

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