ISSN Print 2713-0894    ISSN Online 2713-0908
BIOMEDICAL JOURNAL OF ERMC EASTERN EUROPEAN

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4-(5-methyl-1,3,4-oxadiazole-2-yl)-benzenesulfonamide (ODASA), which is a novel selective type II carbonic anhydrase inhibitor for treating open-angle glaucoma, is undergoing preclinical testing. Pharmacokinetics of the substance have only been studied in rats. Prior to clinical studies, it is necessary to assess the systemic exposure of ODASA in non-rodents. ODASA was administered to Soviet Chinchilla rabbits at a dose of 0.28 mg/kg. About 40 µl of ocular suspension of ODASA was instilled into each eye of animals from the first group, whereas the second group received intraperitoneal injections of the investigational drug. Each group consisted of 6 male rabbits. Samples were obtained prior to administration of ODASA and during 288 hours following the administration at 16 time points. A 10% ascorbic acid solution was added to plasma before freezing. The samples were analyzed using HPLC-MS/MS. Following eyedrop instillation, relative bioavailability for ODASA was 31% as compared to IP administration. Thus, as ODASA was well absorbed into the systemic circulation of rabbits following topical eyedrop instillation, testing its pharmacokinetics in healthy volunteers will be obligatory if the preparation proceeds to phase 1 of clinical studies.
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