THE EFFECT OF VEHICLE ON CORNEAL PENETRATION OF TRITURATED KETOCONAZOLE AND ITRACONAZOLE

BACKGROUND AND OBJECTIVES: Triturated (crushed and suspended) ketocona zole has been recommended for the treatment of fungal keratitis when c ommercial antifungal eyedrops are unobtainable. The authors evaluated the in vivo corneal stromal concentration with different vehicles in t he eyes of adult rabbits. MATERIALS AND METHODS: Ketoconazole and itra conazole tablets were triturated to 20 mg/ml in four vehicles: polyvin yl alcohol (PVA), boric acid, olive oil, and balanced salt solution (B SS). Six eyes (de-epithelialized for better penetration) received one drop every 15 minutes for 2 hours. A yeast overlay bioassay of extract s determined the stromal concentration. RESULTS: Itraconazole in BSS, olive oil, PVA, and boric acid produced inhibition zones of 17.3, 15.6 , 15.4, and 13.2 mm, respectively. Ketoconazole produced inhibition zo nes of 35.9, 39.4, 41.8, and 44.7 mm, respectively. From a standard cu rve, the concentrations of ketoconazole in tissue were 512, 773, 1221, and 1492 mu g/g, respectively. CONCLUSION: The vehicle that: is used to triturate antifungals affects the tissue concentration. This may ha ve an impact on fungal keratitis therapy.