Distribution of clobetasone in rabbit eye tissues after topical application.
This study describes the bioavailability of Clobetasone, which is topically applied as an anti-inflammatory drug. Right eyes of Chinchilla rabbits received Clobetasone eye drops 3 times daily over a period of consecutive 14 days. 30 min up to 96 h after the last application animals were killed at different times and the eyes removed immediately. Nine different eye tissue samples were prepared for Clobetasone estimation by radioimmunoassay (RIA) using 3H-labeled Clobetasone and an antibody directed against Clobetasone. Results indicate that Clobetasone penetrates relatively fast into the different eye tissues. The concentrations are different in the various tissues and show a relationship to the distance from cornea to vitreous. Concentrations decline in the following order: cornea greater than conjunctiva, sclera, iris (200 ng/g) greater than lens, vitreous, aqueous humour (5-15 ng/g). In all samples investigated Clobetasone levels decrease with time. No accumulation of the drug has been measured at any time. Clobetasone levels in the left, untreated eye, indicate that the compound has a small systemic resorption.
Rink
H
H
Institut für Strahlenbiologie, Universität Bonn.
Connors
B
B
Wegener
A
A
Umlauf
A
A
Hockwin
O
O
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001682:Biological Availability; D002990:Clobetasol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D005123:Eye / Q000378:metabolism*; D011817:Rabbits; D011863:Radioimmunoassay; D014018:Tissue Distribution
D000893:Anti-Inflammatory Agents; C010893:clobetasone butyrate; D002990:Clobetasol