AN INVESTIGATION OF THE DOSE PROPORTIONALITY OF DEFLAZACORT PHARMACOKINETICS

✍ Scribed by Niranjan Rao; Vijay O. Bhargava; Donald L. Reynolds; Mark G. Eller; Scott J. Weir

• Book ID: 101277405
• Publisher: John Wiley and Sons
• Year: 1996
• Tongue: English
• Weight: 369 KB
• Volume: 17
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/(sici)1099-081x(199612)17:9<753::aid-bdd988>3.0.co;2-d

✦ Synopsis

The dose proportionality of deflazacort was assessed following single-dose oral administration at doses of 3, 6, and 36mg 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 , , averaged 10.4+5.0, 19457.5, and 132.6+52.5ngmL-l for the 3, 6, and 36 mg doses, respectively. AUC(O-m) averaged 38.5 & 37.1, 64.9 &-20-8, and 41 1.7 148.5 ng hmL-' for the same three doses, respectively. Elimination half-life ranged from 1.9+0.5 h at the 6mg dose to 2.4+ 1.5 h at the 36mg dose. Regression analyses of dose versus C , , and AUC(&co) 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.