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Related Experiment Videos

A corneal perfusion device for estimating ocular bioavailability in vitro.

J B Richman1, D D Tang-Liu

  • 1Department of Pharmacokinetics, Allergan, Inc., Irvine, CA 92715.

Journal of Pharmaceutical Sciences
|February 1, 1990
PubMed
Summary

A new in vitro model simulates tear turnover to study drug penetration across the cornea. Ocular bioavailability was 5-16% for solutions and <0.3% for suspensions, highlighting rapid precorneal washout effects.

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Area of Science:

  • Ophthalmology
  • Pharmacokinetics
  • Drug Delivery

Background:

  • Investigating ocular drug penetration is crucial for developing effective ophthalmic formulations.
  • Existing methods may not accurately reflect in vivo conditions, particularly precorneal drug elimination.

Purpose of the Study:

  • To develop and validate a novel in vitro corneal penetration model that simulates physiological tear turnover.
  • To assess the in vitro ocular bioavailability of various marketed ophthalmic drug formulations.

Main Methods:

  • A modified corneal chamber with reduced donor volume and simulated tear turnover was utilized.
  • Oxygenation and circulation were maintained in the receiver chamber.
  • Drug penetration and bioavailability of solutions (flurbiprofen, levobunolol, fluorometholone) and suspensions (prednisolone acetate) were quantified.

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Main Results:

  • The model demonstrated rapid drug elution from the donor chamber (12%/min).
  • Corneal absorption ranged from 5-16% for solutions and <0.3% for suspensions.
  • High recovery from the donor effluent confirmed significant precorneal drug loss, consistent with in vivo findings.

Conclusions:

  • The developed in vitro model effectively simulates precorneal washout and ocular drug absorption.
  • Results indicate low ocular bioavailability for many ophthalmic preparations due to rapid elimination.
  • The model offers a valuable tool for researching ocular drug absorption and metabolism.