Pharmacokinetic of sulfisoxazole in aqueous humor after topical and subconjunctival application in dogs. 2007

Gokhan Eraslan, and Murat Kibar, and Dinc Essiz, and Fatma Sahindokuyucu, and Bilal Cem Liman
Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Erciyes, Kayseri, Turkey.

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.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008297 Male Males
D003228 Conjunctiva The mucous membrane that covers the posterior surface of the eyelids and the anterior pericorneal surface of the eyeball. Bulbar Conjunctiva,Palpebral Conjunctiva,Plica Semilunaris of Conjunctiva,Plicae Semilunares of Conjunctiva,Tunica Conjunctiva,Conjunctiva, Bulbar,Conjunctiva, Palpebral,Conjunctivas
D004285 Dogs The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065) Canis familiaris,Dog
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000890 Anti-Infective Agents Substances that prevent infectious agents or organisms from spreading or kill infectious agents in order to prevent the spread of infection. Anti-Infective Agent,Anti-Microbial Agent,Antimicrobial Agent,Microbicide,Microbicides,Anti-Microbial Agents,Antiinfective Agents,Antimicrobial Agents,Agent, Anti-Infective,Agent, Anti-Microbial,Agent, Antimicrobial,Agents, Anti-Infective,Agents, Anti-Microbial,Agents, Antiinfective,Agents, Antimicrobial,Anti Infective Agent,Anti Infective Agents,Anti Microbial Agent,Anti Microbial Agents
D001082 Aqueous Humor The clear, watery fluid which fills the anterior and posterior chambers of the eye. It has a refractive index lower than the crystalline lens, which it surrounds, and is involved in the metabolism of the cornea and the crystalline lens. (Cline et al., Dictionary of Visual Science, 4th ed, p319) Aqueous Flare,Intraocular Fluid,Aqueous Flares,Aqueous Humors,Flare, Aqueous,Fluid, Intraocular,Fluids, Intraocular,Humor, Aqueous,Humors, Aqueous,Intraocular Fluids
D013444 Sulfisoxazole A short-acting sulfonamide antibacterial with activity against a wide range of gram- negative and gram-positive organisms. Sulfafurazole,Gantrisin,Gantrisin Pediatric,Neoxazoi,Sulfadimethyloxazole,Sulfafurazol FNA,Sulfasoxizole,Sulfisoxazole Diolamine,Sulfisoxazole, Ammonium Salt,Sulfisoxazole, Monolithium Salt,Sulfisoxazole, Monosodium Salt,Sulfisoxazole, Monosodium, Monomesylate Salt,Sulfisoxazole, Triammonium Salt,TL-azole,V-Sul,Ammonium Salt Sulfisoxazole,Diolamine, Sulfisoxazole,Monolithium Salt Sulfisoxazole,Monosodium Salt Sulfisoxazole,Pediatric, Gantrisin,TL azole,Triammonium Salt Sulfisoxazole,V Sul
D013997 Time Factors Elements of limited time intervals, contributing to particular results or situations. Time Series,Factor, Time,Time Factor
D015233 Models, Statistical Statistical formulations or analyses which, when applied to data and found to fit the data, are then used to verify the assumptions and parameters used in the analysis. Examples of statistical models are the linear model, binomial model, polynomial model, two-parameter model, etc. Probabilistic Models,Statistical Models,Two-Parameter Models,Model, Statistical,Models, Binomial,Models, Polynomial,Statistical Model,Binomial Model,Binomial Models,Model, Binomial,Model, Polynomial,Model, Probabilistic,Model, Two-Parameter,Models, Probabilistic,Models, Two-Parameter,Polynomial Model,Polynomial Models,Probabilistic Model,Two Parameter Models,Two-Parameter Model

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