Influence of hydroxypropyl beta-cyclodextrin on the corneal permeation of pilocarpine.
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.
Aktaş
Yeşim
Y
Faculty of Pharmacy, Department of Pharmaceutical Technology, Hacettepe University, Ankara, Turkey.
Unlü
Nurşen
N
Orhan
Mehmet
M
Irkeç
Murat
M
Hincal
A Atilla
AA
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
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