Drug Metabolism and Pharmacokinetics
Print ISSN : 0916-1139
Studies on the Metabolic Fate of Mometasone furoate (MF)(I):Percutaneous Absorption, Distribution, Excretion after Topical Application to Rats and Rabbits
Koichi SUGENOKenji MIZOJIRIYoshio ESUMIMatsuo TAKAICHITakayuki MIYAKEHideaki SEKI
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1990 Volume 5 Issue 6 Pages 785-794

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Abstract

The absorption and excretion of 14C-MF in rats and rabbits were studied following topical application of 0.1% dermal formulations mostly as a form of ointment.
1. When the ointment was applied to the intact skin, radioactivity was not detected in plasma of both rats and rabbits. Less than lOng equiv./ml of radioactivity was detected after application to the stripped skin in both animal species, and it disappeared 24 or 48hr after application.
2. The absorption of radioactivity from the ointment in rats, estimated as the sum of urinary and fecal excretion, was 5 ?? 10% of the applied dose in intact skin and 30 ?? 50% in stripped skin. In rabbits, it was lower than those of rats.
3. Radioactivity was predominantly excreted in feces than in urine in both animal species, and this difference was more prominent in rats than in rabbits.
4. Female rats showed slightly higher absorption ratio as compared to male rats. It probably was due to the difference of skin thickness, less thinner skin was observed in females than in males.
5. When 14C-MF was applied as a cream or lotion to intact skin of rats, almost same results as those of ointment were obtained.

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© The Japanese Society for the Study of Xenobiotics
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