Influence of hydroxypropyl beta-cyclodextrin on the corneal permeation of pilocarpine

Drug Dev Ind Pharm. 2003 Feb;29(2):223-30. doi: 10.1081/ddc-120016730.

Abstract

The influence of hydroxypropyl beta-cyclodextrin (HPbetaCD) on the corneal permeation of pilocarpine nitrate was investigated by an in vitro permeability study using isolated rabbit cornea. Pupillary-response pattern to pilocarpine nitrate with and without HPbetaCD was examined in rabbit eye. Corneal permeation of pilocarpine nitrate was found to be four times higher after adding HPbetaCD into the formulation. The reduction of pupil diameter (miosis) by pilocarpine nitrate was significantly increased as a result of HPbetaCD addition into the simple aqueous solution of the active substance. The highest miotic response was obtained with the formulation prepared in a vehicle of Carbopol 940. It is suggested that ocular bioavailability of pilocarpine nitrate could be improved by the addition of HPbetaCD.

Publication types

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

MeSH terms

  • 2-Hydroxypropyl-beta-cyclodextrin
  • Acrylic Resins
  • Animals
  • Chemistry, Pharmaceutical
  • Cornea / drug effects*
  • Cornea / metabolism
  • Cyclodextrins / chemistry
  • Cyclodextrins / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Compounding
  • Excipients / chemistry
  • Excipients / pharmacology*
  • Gels
  • Hydrogen-Ion Concentration
  • Male
  • Ophthalmic Solutions
  • Osmolar Concentration
  • Parasympathomimetics / administration & dosage
  • Parasympathomimetics / pharmacokinetics*
  • Parasympathomimetics / pharmacology
  • Permeability
  • Pharmaceutical Vehicles
  • Pilocarpine / administration & dosage
  • Pilocarpine / pharmacokinetics*
  • Pilocarpine / pharmacology
  • Rabbits
  • Time Factors
  • Viscosity
  • beta-Cyclodextrins*

Substances

  • Acrylic Resins
  • Cyclodextrins
  • Excipients
  • Gels
  • Ophthalmic Solutions
  • Parasympathomimetics
  • Pharmaceutical Vehicles
  • beta-Cyclodextrins
  • Pilocarpine
  • 2-Hydroxypropyl-beta-cyclodextrin
  • carbopol 940