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AN INVESTIGATION OF THE DOSE PROPORTIONALITY OF DEFLAZACORT PHARMACOKINETICS
Author(s) -
Rao Niranjan,
Bhargava Vijay O.,
Reynolds Donald L.,
Eller Mark G.,
Weir Scott J.
Publication year - 1996
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/(sici)1099-081x(199612)17:9<753::aid-bdd988>3.0.co;2-d
Subject(s) - deflazacort , pharmacokinetics , cmax , oral dose , metabolite , oral administration , active metabolite , chemistry , pharmacology , medicine , corticosteroid
The dose proportionality of deflazacort was assessed following single‐dose oral administration at doses of 3, 6, and 36 mg to 24 healthy young adult volunteers. The active metabolite of deflazacort (21‐desacetyl deflazacort) was monitored in plasma using a sensitive, semi‐microbore liquid chromatographic method. C max averaged 10·4±5·0, 19·8±7·5, and 132·6±52·5 ng mL −1 for the 3, 6, and 36 mg doses, respectively. AUC(0–∞) averaged 38·5±37·1, 64·9±20·8, and 411·7±148·5 ng h mL −1 for the same three doses, respectively. Elimination half‐life ranged from 1·9±0·5 h at the 6 mg dose to 2·4±1·5 h at the 36 mg dose. Regression analyses of dose versus C max and AUC(0–∞) yielded intercepts which were not significantly different from zero ( p >0·05) and slopes which were significant ( p <0·05). Regression analysis of dose versus apparent oral clearance yielded a slope which was not significantly different from zero ( p >0·05). These data indicate that deflazacort exhibits dose‐proportional pharmacokinetics.