Characterization of Ocular Pharmacokinetics of Tilisolol after Instillation into Anesthetized Rabbits

Hitoshi SASAKI; Kenzo YAMAMURA; Takahiro MUKAI; Koyo NISHIDA; Junzo NAKAMURA; Mikiro NAKASHIMA; Masataka ICHIKAWA

doi:10.1248/bpb.22.1253

Hitoshi SASAKI, Kenzo YAMAMURA, Takahiro MUKAI, Koyo NISHIDA, Junzo NAKAMURA, Mikiro NAKASHIMA, Masataka ICHIKAWA

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Keywords: ocular pharmacokinetics, tilisolol, diffusion model, ocular penetration, drug delivery system, tear deficiency

JOURNAL FREE ACCESS

1999 Volume 22 Issue 11 Pages 1253-1255

DOI https://doi.org/10.1248/bpb.22.1253

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Abstract

The purpose of this study was to characterize the ocular pharmacokinetics of a beta-blocker, tilisolol, after instillation into anesthetized rabbits using a mathematical model including a diffusion process. The samples were analyzed by HPLC. Anesthetized rabbit was used as a model of tear secretion deficiency. Anesthetized rabbits showed higher drug concentration in the tear fluid and aqueous humor after instillation than unanesthetized rabbits. A mathematical model including a diffusion process and in vivo penetration parameters well described the concentrations of tilisolol in the aqueous humor after instillation in anesthetized rabbits.

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