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Titre du document / Document title

The effect of vehicle on corneal penetration of triturated ketoconazole and Itraconazole

Auteur(s) / Author(s)

GUZEK J. P. (1) ; ROOSENBERG J. M. (2) ; GANO D. L. (2) ; WESSELS I. F. (2 3) ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

(1) Departments of Ophthalmology, Jerry L. Pettis Memorial Veterans Administration Hospital, Loma Linda, CA, ETATS-UNIS
(2) Loma Linda University School of Medicine, Loma Linda, CA, ETATS-UNIS
(3) Department of Ophthalmology, University of Tennessee College of Medicine, Chattanooga, TN, ETATS-UNIS

Résumé / Abstract

■ BACKGROUND AND OBJECTIVES: Triturated (crushed and suspended) ketoconazole has been recommended for the treatment of fungal keratitis when commercial antifungal eyedrops are unobtainable. The authors evaluated the in vivo corneal stromal concentration with different vehicles in the eyes of adult rabbits. ■ MATERIALS AND METHODS: Ketoconazole and itraconazole tablets were triturated to 20 mg/ml in four vehicles: polyvinyl alcohol (PVA), boric acid, olive oil, and balanced salt solution (BSS). Six eyes (deepithelialized for better penetration) received one drop every 15 minutes for 2 hours. A yeast overlay bioassay of extracts 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 zones of 35.9, 39.4, 41.8, and 44.7 mm, respectively. From a standard curve, the concentrations of ketoconazole in tissue were 512, 773, 1221, and 1492 μg/g, respectively. ■ CONCLUSION: The vehicle that is used to triturate antifungals affects the tissue concentration. This may have an impact on fungal keratitis therapy.

Revue / Journal Title

Ophthalmic surgery and lasers   ISSN 1082-3069   CODEN OSLAF2 

Source / Source

1998, vol. 29, no11, pp. 926-929 (7 ref.)

Langue / Language

Anglais

Editeur / Publisher

Slack, Thorofare, NJ, ETATS-UNIS  (1995-2000) (Revue)

Mots-clés anglais / English Keywords

Keratitis ; Fungi ; Infection ; Cornea ; Mycosis ; Ketoconazole ; Itraconazole ; Antifungal agent ; Vehicle(excipient) ; Boric acid ; Olive oil ; Polyvinylalcohol ; Saline solution ; Comparative study ; Concentration ; Chemotherapy ; Treatment ; Animal ; Rabbit ; Imidazole derivatives ; Thallophyta ; Lagomorpha ; Mammalia ; Vertebrata ; Eye disease ; Keratopathy ;

Mots-clés français / French Keywords

Kératite ; Fungi ; Infection ; Cornée ; Mycose ; Kétoconazole ; Itraconazole ; Antifongique ; Excipient ; Borique acide ; Huile olive ; Vinylique alcool polymère ; Solution saline ; Etude comparative ; Concentration ; Chimiothérapie ; Traitement ; Animal ; Lapin ; Imidazole dérivé ; Thallophyta ; Lagomorpha ; Mammalia ; Vertebrata ; Oeil pathologie ; Kératopathie ;

Mots-clés espagnols / Spanish Keywords

Queratitis ; Fungi ; Infección ; Córnea ; Micosis ; Ketoconazol ; Itraconazol ; Antifúngico ; Excipiente(vehiculo) ; Bórico ácido ; Aceite oliva ; Vinílico alcohol polímero ; Solución salina ; Estudio comparativo ; Concentración ; Quimioterapia ; Tratamiento ; Animal ; Conejo ; Imidazol derivado ; Thallophyta ; Lagomorpha ; Mammalia ; Vertebrata ; Ojo patología ; Queratopatía ;

Localisation / Location

INIST-CNRS, Cote INIST : 14946, 35400007141956.0070

Nº notice refdoc (ud4) : 1673476

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