title: Pharmacokinetic of sulfisoxazole in aqueous humor after topical and subconjunctival application in dogs.
abstract: This study was undertaken to evaluate the ocular pharmacokinetic of sulfisoxazole. Male, 2-3 years old 10 mix breed dogs weighing 12-15 kg were used. A 2 mg dose/eye of sulfisoxazole was administrated to the animals by either subconjunctivally or by topically. Samples of aqueous humor were collected after 0.083, 0.25, 0.5, 1, 2, 4, 6, 24 and 72 h and level of sulfisoxazole was determined. Pharmacokinetic parameters including absorption rate constant (k(a)), slope factor (beta), absorption half-life (t1/2a), half-life of elimination in aqueous humor (t1/2beta), maximal concentration in aqueous humor (C(max)), time to reach C(max) (t(max)), mean residence time in aqueous humor (MRT) and area under the concentration time curve from zero up to infinity (AUC(0-infinity)) were calculated. Compared to topical application, value of k(a) in subconjunctival application increased while values of t1/2a and t(max) decreased and the value of t1/2beta prolonged (p < 0.05). There was no significant difference between groups regarding other parameters (p > 0.05). These results indicate that sulfisoxazole may not be potent enough to treat intraocular infections caused by bacteria when applied either subconjunctivally or topically at a dose of 2 mg/eye. Furthermore, subconjunctival application of sulfisoxazole could be more efficient for treatment of intraocular infections due to higher absorption of drug and longer remaining time in the eye compared to topical application.
authors.affiliation: Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Erciyes, Kayseri, Turkey.
authors.forename: Gokhan
authors.initials: G
authors.lastname: Eraslan
authors.forename: Murat
authors.initials: M
authors.lastname: Kibar
authors.forename: Dinc
authors.initials: D
authors.lastname: Essiz
authors.forename: Fatma
authors.initials: F
authors.lastname: Sahindokuyucu
authors.forename: Bilal Cem
authors.initials: BC
authors.lastname: Liman
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000493:pharmacokinetics* / Q000494:pharmacology; D001082:Aqueous Humor / Q000187:drug effects* / Q000378:metabolism; D019540:Area Under Curve; D003228:Conjunctiva / Q000187:drug effects* / Q000378:metabolism; D004285:Dogs; D007700:Kinetics; D008297:Male; D015233:Models, Statistical; D013444:Sulfisoxazole / Q000493:pharmacokinetics* / Q000494:pharmacology; D013997:Time Factors; D016896:Treatment Outcome
chemical_list: D000890:Anti-Infective Agents; D013444:Sulfisoxazole