CORNEAL CONCENTRATIONS AND PRELIMINARY TOXICOLOGICAL EVALUATION OF ANITRACONAZOLE DIMETHYL SULFOXIDE OPHTHALMIC OINTMENT/

The objectives of this study were to determine the concentration of it raconazole achieved in corneal tissue and aqueous humour after topical application of a 1% itraconazole ointment; to determine the effect of including dimethyl sulphoxide (DMSO) in the ointment on achievable oc ular tissue itraconazole concentrations; and to assess if any gross or histopathologic ocular toxicity results from the topical application of 1% itraconazole with or without the addition of DMSO. The experimen tal trial consisted of 6 horses considered to have normal eyes. Each h orse had one eye treated with 0.3 mL of 1% ultra-micronized itraconazo le ointment and the fellow eye with 0.3 mt of 1% itraconazole/30% DMSO ointment. The ointment was applied every 6 h for a total of 28 treatm ents. Both ointments were well tolerated and no gross or histopatholog ic abnormalities developed during the trial. Corneal tissue and aqueou s humour concentrations of itraconazole were determined using high per formance liquid chromatography, Corneal tissue concentration averaged 1.1 (+/- 0.4) mu g/g in horses treated with the 1% ultramicronized itr aconazole ointment and 7.9 (+/- 3.3) mu g/g for those treated with the 1% itraconazole/30% DMSO ointment; there was a statistically signific ant difference between ointments (P = 0.005) No itraconazole could be detected in the aqueous humour in either treatment group.