Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10162415 | Journal of Pharmaceutical Sciences | 2014 | 10 Pages |
Abstract
A novel ophthalmic formulation based on the ionic complexation between Eudragit E 100 (EU) and flurbiprofen (FB) is proposed. The selected complex composition, named EU-FBH50Cl50, had the basic groups of EU completely neutralized with equal molar amounts of FB and HCl. This complex, obtained in the solid state, exhibited a high aqueous compatibility producing a colloidal dispersion with a high positive electrokinetic potential, in which more than 99% of FB was ionically condensed with EU. In bicompartimental Franz cells, FB diffusion from the complex was very slow. However, dispersion in 0.9% NaCl increased the FB release through an ionic exchange, providing an optimal constant rate of delivery. Corneal FB permeation from 0.1% EU-FBH50-Cl50 dispersed in 0.9% NaCl solution was substantially more effective compared with 0.1% FB solution, EU-FBH50-Cl50(Dex), or Tolerane® (a marketed formulation). This complex formulation was shown to be innocuous for rabbit ocular tissues because no irritant effects were evidenced. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association.
Keywords
Related Topics
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Pharmacology, Toxicology and Pharmaceutical Science
Drug Discovery
Authors
Daniela Alejandra Quinteros, Luis Ignacio Tártara, Santiago Daniel Palma, Ruben Hilario Manzo, Daniel Alberto Allemandi,