Registration Dossier
Registration Dossier
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EC number: 609-203-4 | CAS number: 36130-02-6
Endpoint summary
Administrative data
Link to relevant study record(s)
Description of key information
No toxicokinetic data of Fluocortolon-A-Acetat is available and results from Fluocortolon are consulted.
Key value for chemical safety assessment
Additional information
For fluocortolone-21-valerate (CAS No. 36130-02-6) no toxicokinetics data are available. Therefore, toxicokinetics data of fluocortolone (CAS No. 152-97-6) were used since these data are regarded as representative as most likely ester cleavage of fluocortolone-21-valerate occurs under physiological conditions.
Pharmacokinetic
After intravenous application of fluocortolone in human the half-life in the plasma was determined with 1.5 hours. The total clearance was 7.0 +/- 1.5 ml/min/kg and is equivalent to the metabolic clearance since fluocortolone is almost completely metabolised and only a small amount of this substance is found in the urin. After oral application of 10 mg and 20 mg fluocortolone to human the maximum plasma level was reached after 1.5 hours. The total bioavailability was 77.4% +/-17.8% and 89.0% +/- 29.4%, respectively. The plasma half-life is 1.7 hours. Fluocortolone is metabolised in the human liver and the metabolites are excreted with the urine. Reactions of biotransformation were oxidation of the hydroxy-group on C11, reduction of the keto-group on C20, hydroxylation on 6ß-position under defluoronation, carbonylic acid production under oxidation of the keto-group on C20 and conjugation with glucuronic acid and sulfuric acid. The plasma half-life of fluocortolone and metabolites is ca. 4 hours. [Täuber, U.; 1993]
Dermal absorption
Dermal absorption of fluocortolone creme as emulsion was tested on eleven healthy volunteers at different time points. It was shown that the resorption rate was increased with increasing exopsure time. After 8 hours exposure a dermal penetration rate of 44% in mean was found. After 12 and 20 times skin stripping the penetration rate could be increased to 10 and 20 %, respectively. Relevant differences between occlusiv and open application of test substance was not seen. When psoriasis patients were treated 24 hours with fluocortolone creme resorption rates of 65 % (5% SD) were found. Testing of water-based and fat-based cremes revealed that fatty cremes have approximately half of the penetration rate compared to water based cremes. [Täuber, U.; 1993]
Literature:
Täuber, U. Gutachten zur Pharmakokinetik und Bioverfügbarkeit beim Menschen, Wirkstoffe: Fluocortolon, Fluocortolon-21 -hexanoat und Fluocortolon-21-pivalat; Pharmakokinetik, Schering AG, 1993.
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