Ma. Ball et al., CORNEAL CONCENTRATIONS AND PRELIMINARY TOXICOLOGICAL EVALUATION OF ANITRACONAZOLE DIMETHYL SULFOXIDE OPHTHALMIC OINTMENT/, Journal of veterinary pharmacology and therapeutics, 20(2), 1997, pp. 100-104
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.