PHARMACOLOGICAL EVALUATION OF ANTIINFLAMMATORY PYRROLE-ACETIC ACID-DERIVATIVE EYE DROPS

The effects of mucoadhesive eye drops containing a pyrrole-acetic acid derivative (tolmetin) at 0.5% concentration on ocular inflammation pr oduced by sodium arachidonate in the rabbit's eye were evaluated. Furt hermore, the bioavailability of the mucoadhesive formulation in the aq ueous humor against an aqueous-based solution was compared. Tolmetin e ye drops significantly reduced the signs of ocular inflammation elicit ed by sodium arachidonate on conjunctiva and iris. Tolmetin treatment significantly reduced the levels of prostaglandin E-2, polymorphonucle ar leukocytes and protein concentration in aqueous samples obtained fr om the eyes treated with arachidonate. The de novo production of prost aglandin E-2 by corneas obtained from rabbits sacrificed 2 hours after arachidonate instillation were significantly higher in samples taken from controls than in corneas obtained from the eyes treated with tolm etin eye drops. Furthermore, the drug treatment significantly reduced the rise in intraocular pressure arachidonate-induced. The mucoadhesiv e formulation showed a higher bioavailability in aqueous humor compare d to the aqueous-based solution both in the uninflamed and in the infl amed rabbit eyes.