Studies on pharmacokinetics of 9 -fluorohydrocortisone in the rat, guinea pig and dog
Wenzl, H.; Garbe, A.; Nowak, H.
Arzneimittel-Forschung 21(8 Suppl): 1115-1122
1971
ISSN/ISBN: 0004-4172 PMID: 5109326 Document Number: 5799
The pharmacokinetics of 9a-fluoro-11ß,17a,21-trihydroxy4-pregnene-3,20-dione (9a-F) were investigated in rats, guinea pigs and dogs. a) After a single i.v. injection of 3H labelled 9a-F the plasma radioactivity decreased in 2 (rats) and 3 phases resp. (guinea pigs, dogs) of different half lives. It is suggested that these phases correspond to the different elimination rates of the original drug (plasma half life 80 min) and its metabolites (plasma half lives of 3.5 and 10 11.). b) After oral application of 9a-F rats showed a maximum concentration in plasma after 5-10 min, guinea pigs after 2 h, and dogs 5 h. c) Evaluation according to the principle of corresponding areas indicated nearly total absorption of the drug. d) In rats the drug is almost exclusively excreted with feces, in dogs and guinea pigs predominantly with urine. e) In rats with canulated bile duct 70% of radioactivity appeared in the bile within 7 h, in guinea pigs in the same time about 50-60%.
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