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M Yamaguchi, M Nakamura, J Inoue; Studies on Intraocular Penetration of Ophthalmic Solution by Use of Cyclodextrins for Anti-cataract Therapeutic Agent . Invest. Ophthalmol. Vis. Sci. 2002;43(13):1851.
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Purpose: For the cataract treatment by ophthalmic solution, enough amount of drug should be in aqueous humor and lens. Therefore, if the preparation which can penetrate sufficiently drug into intraocular by instillation were developed, it would bring big benefit for cataract treatment. SJA6017, which is potent calpain inhibitor and ameliorates cataract formation on various in vitro and in vivo models, was used for this study. Cyclodextrins were selected as optimum preparation that improve penetration of SJA6017 into intraocular, because cyclodextrins dissolve water-insoluble drug and have been reported to improve penetration of drug into several tissues. The studies were carried out to evaluate SJA6017 level in aqueous humor by comparing cyclodextrins solution to suspension. Experiment: Male albino rabbits weighing about 2 kg were used for the study. 1.0% ophthalmic solution of SJA6017 dissolved by cyclodextrin and 1.0% suspension were instilled into rabbit eyes. Aqueous humor was collected at 0.5, 1 and 3 hour after instillation. Drug concentration was measured by high performance liquid chromatography. Result and Conclusion: Drug concentration for the cyclodextrin ophthalmic solution was increased about 2.6 times in aqueous humor than the ophthalmic suspension. Thus, intraocular penetration of SJA6017 for the ophthalmic solution was superior to ophthalmic suspension. From this result, it had become apparent that the cyclodextrin ophthalmic solution was optimum preparation that improve penetration of SJA6017 in intraocular.
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