In Vivo Ocular Pharmacokinetic Model for Designing Dosage Schedules and Formulations of Ophthalmic Drugs in Human

概要

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The purpose of this study was to develop an in vivo pharmacokinetic model and parameters for predicting the concentrations of ophthalmic drugs in the anterior chamber after instillation into human eyes. We have already reported the usefulness of mathematical model including a diffusion process in rabbits 1). Timolol was used as a model ophthalmic drug. The concentrations of timolol and fluorescein in the tear fluid were determined after instillation into the eyes of human volunteers. The in vivo pharmacokinetic parameters in the tear fluid were estimated by the elimination profile according to a one-compartment model. The concentrations of timolol in the aqueous humor were obtained from the data previously reported 2),3). Other parameters of timolol were estimated from the concentration profiles of timolol in the aqueous humor according to a pharmacokinetic model including a corneal diffusion process. The parameters for human were almost equal to those for rabbits reported previously 1). This mathematical model and in vivo parameters will be effective to estimate the adequate regimen for ophthalmic chemotherapy and develop the ocular drug delivery systems.
長崎大学の論文