The effect of some macromolecular ionic complexes on the pharmacokinetics and -dynamics of ocular cyclopentolate in rabbits

J Ocul Pharmacol. 1992 Spring;8(1):59-67. doi: 10.1089/jop.1992.8.59.

Abstract

The effect of mucoadhesive polymeric vehicles on the mydriatic efficacy, and on the systemic and ocular absorption of cyclopentolate from eyedrops was studied in albino rabbits. Combining cyclopentolate base to polygalacturonic (CY-PGA) or hyaluronic (CY-HA) acid resulted in an increased mydriatic effect when compared with cyclopentolate hydrochloride (CY-HCl). During the first half an hour, the systemic absorption of cyclopentolate was lower after CY-PGA than after CY-HCl. The ocular penetration of cyclopentolate, based on drug concentrations in aqueous humor 30 minutes after the eyedrop instillation, was increased 3 fold when the polygalacturonate complex was used. CY-PGA, as well as other polymeric salts, might offer a possibility to increase the therapeutic index of cyclopentolate.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Absorption
  • Animals
  • Cyclopentolate / pharmacokinetics*
  • Cyclopentolate / pharmacology
  • Drug Carriers
  • Eye / metabolism*
  • Female
  • Hyaluronic Acid / pharmacokinetics*
  • Hyaluronic Acid / pharmacology
  • Male
  • Pectins / pharmacokinetics*
  • Pectins / pharmacology
  • Rabbits
  • Random Allocation

Substances

  • Drug Carriers
  • Pectins
  • Hyaluronic Acid
  • Cyclopentolate
  • polygalacturonic acid