Enhance of trascorneal permeation using novel eudragit-flurbiprofen complexes

QUINTEROS DANIELA; TARTARA IGNACIO; PALMA SANTIAGO; ALLEMANDI DANIEL

Cordoba

Congreso; I Reunión Internacional de Ciencias Farmacéuticas; 2010

RiCiFa

Enhance of trascorneal permeation using novel eudragit-flurbiprofen complexes Quinteros DA, Tartara LI, Palma SD, Allemandi DA  Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba. Ciudad Universitaria, X5000HUA-Córdoba, Argentina Introduction This work is a part of a project of modified ocular drug delivery system. The aim is the physico-chemical, pharmaceutical and biopharmaceutical characterization of Eudragit-drug complexes to evaluated the transcorneal permeation and ocular irritation in rabbit of novel Eu-Fl complexes using Flurbiprofeno (Fl) as a model drug. Materials Two Eu-Fl formulations, 0,1% of Fl in 5% dextrose and saline solutions, were assayed. A commercial product (Tolerane®) and 0,01% of Fl aqueous solution (control) were comparatively studied. (Table1) Methods Osmolality, Partition coeficient, pH, electrokinetic potential, solubility determination. Release and permeation transcorneal of rabbit of Fl test (bicompartmental diffusion cells). The potential ocular irritancy and/or damaging effects of the formulations under test were evaluated using a slightly modified version of the Draize test and histological sections of cornea. Results The complex solutions were transparent, stable, with high and positive electrokinetic potential (+35 - +55mV). A high proportion of Fl associated to the Eu by ionic condensation was determined. In agreement with this property, an increase of the solubility of Fl was observed in pHs where it exhibit low aqueous solubility. The kinetics of permeation of the 4 formulations show the same sequence obtained in the release assays. Comparison of the release and permeation rates show that dispersed systems Eu-Fl50 NaCl 0.9% in promoting sustained permeation of the active ingredient at a rate faster than expected. Moreover these systems have a slight irritation characterized in a congestion of the vessels of the conjunctiva in a discrete to moderate without corneal injury or intraocular Conclusions These characteristics also significantly increase the aqueous compatibility of the drug say they are favorable systems for use in ophthalmic formulations. Acknowledgements: CONICET, FONCYT and Universidad Nacional de Córdoba