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Systemic morphine pharmacokinetics after ocular administration.

F Chast1, C Bardin, H Sauvageon-Martre

  • 1Service de Pharmacie, Hôtel-Dieu de Paris, France.

Journal of Pharmaceutical Sciences
|October 1, 1991
PubMed
Summary
This summary is machine-generated.

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Ocular morphine application in rabbits shows rapid absorption and high bioavailability. Lacrimal canaliculi ligature alters pharmacokinetics but not overall drug bioavailability, highlighting conjunctival resorption capacity.

Area of Science:

  • Ophthalmology
  • Pharmacology
  • Drug Delivery

Background:

  • Ocular drug delivery presents challenges due to rapid clearance and limited absorption.
  • Morphine's pharmacokinetic profile after ocular administration requires detailed investigation.

Purpose of the Study:

  • To determine the pharmacokinetics of a single ocular dose of morphine in rabbits.
  • To investigate the impact of lacrimal canaliculi ligature on morphine ocular absorption.
  • To identify the primary sites of morphine resorption following conjunctival administration.

Main Methods:

  • Pharmacokinetic analysis of morphine in rabbits after single ocular application.
  • Utilized sensitive reversed-phase ion-pair chromatography for morphine determination.
  • Compared drug absorption before and after lacrimal canaliculi ligature.

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Main Results:

  • Morphine administered ocularly rapidly achieved high blood levels, indicating significant pharmacological activity.
  • Ocular bioavailability of morphine was found to be higher compared to non-parenteral routes.
  • Lacrimal canaliculi ligature modified the pharmacokinetic profile but did not significantly alter overall drug bioavailability.

Conclusions:

  • The conjunctiva demonstrates a substantial capacity for drug resorption.
  • The nasal mucosa plays a major role in morphine absorption under physiological conditions.
  • Ocular administration is a viable route for achieving systemic drug levels with high bioavailability.