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Investigative Ophthalmology & Visual Science, Vol 27, 519-524, Copyright © 1986 by Association for Research in Vision and Ophthalmology

ARTICLES AND REPORTS

Pharmacokinetic of topical cyclosporin A in the rabbit eye

M Wiederholt, D Kossendrup, W Schulz and F Hoffmann

3H labelled cyclosporin A (CS-A) eye drops (2% in castor oil) were applied in rabbits. When a single drop of 10 microliters was given CS-A reached a maximal concentration of 900-1400 ng/ml in the cornea 6 hr after application and then slowly decreased. A substantial level of 600- 900 ng/ml was still present after 48 hr. When corneas were analysed for their cellular compartments, 67% of CS-A was found in the epithelium, 25% in the stroma (probably in keratocytes), and 8% in the endothelium. In corneas denervated by circular keratotomy, slightly reduced concentrations were found after surgery, the reduction was not therapeutically significant. Using the HPLC method a significant corneal metabolism of CS-A could be excluded. Scleral concentrations of CS-A as high as 180 ng/ml were found. Concentrations of CS-A in aqueous humor, lens, vitreous body and uvea/retina were below the therapeutic range.


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