title: Influence of hydroxypropyl beta-cyclodextrin on the corneal permeation of pilocarpine.
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.
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Technology, Hacettepe University, Ankara, Turkey.
authors.forename: Yeşim
authors.initials: Y
authors.lastname: Aktaş
authors.forename: Nurşen
authors.initials: N
authors.lastname: Unlü
authors.forename: Mehmet
authors.initials: M
authors.lastname: Orhan
authors.forename: Murat
authors.initials: M
authors.lastname: Irkeç
authors.forename: A Atilla
authors.initials: AA
authors.lastname: Hincal
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000180:Acrylic Resins; D000818:Animals; D002626:Chemistry, Pharmaceutical; D003315:Cornea / Q000187:drug effects* / Q000378:metabolism; D003505:Cyclodextrins / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry / Q000494:pharmacology*; D005782:Gels; D006863:Hydrogen-Ion Concentration; D008297:Male; D009883:Ophthalmic Solutions; D009994:Osmolar Concentration; D010277:Parasympathomimetics / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D010539:Permeability; D014677:Pharmaceutical Vehicles; D010862:Pilocarpine / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D011817:Rabbits; D013997:Time Factors; D014783:Viscosity; D047392:beta-Cyclodextrins
chemical_list: D000180:Acrylic Resins; D003505:Cyclodextrins; D005079:Excipients; D005782:Gels; D009883:Ophthalmic Solutions; D010277:Parasympathomimetics; D014677:Pharmaceutical Vehicles; D047392:beta-Cyclodextrins; D010862:Pilocarpine; D000073738:2-Hydroxypropyl-beta-cyclodextrin; C006903:carbopol 940