The formulation of aqueous ophthalmic solutions containing indomethacin (IND) presents serious problems due to poor solubility and stability of the drug. The purpose of this study was to evaluate a novel 0.1% IND formulation containing a poly(oxyethylene)poly(oxypropylene) block copolymer (poloxamer 407) as solubilizer. This formulation was evaluated for stability, bioavailability and anti-inflammatory activity in comparison with an ophthalmic IND solution currently on the market. The experimental solution, tested for IND stability at different temperatures, compared favorably with the commercial solution. In rabbits, it produced significantly higher IND levels in the aqueous humor and, in an immunogenic uveitis model, it induced a comparatively faster resolution of the symptoms, as determined by inflammation scores and by IOP measurements. The data indicate poloxamer 407 as a potentially valuable nonirritating, solubilizing and stabilizing agent for indomethacin.

Pharmacokinetics and anti-inflammatory activity in rabbits of a novel indomethacin ophthalmic solution

CHETONI, PATRIZIA;BURGALASSI, SUSI;
2000

Abstract

The formulation of aqueous ophthalmic solutions containing indomethacin (IND) presents serious problems due to poor solubility and stability of the drug. The purpose of this study was to evaluate a novel 0.1% IND formulation containing a poly(oxyethylene)poly(oxypropylene) block copolymer (poloxamer 407) as solubilizer. This formulation was evaluated for stability, bioavailability and anti-inflammatory activity in comparison with an ophthalmic IND solution currently on the market. The experimental solution, tested for IND stability at different temperatures, compared favorably with the commercial solution. In rabbits, it produced significantly higher IND levels in the aqueous humor and, in an immunogenic uveitis model, it induced a comparatively faster resolution of the symptoms, as determined by inflammation scores and by IOP measurements. The data indicate poloxamer 407 as a potentially valuable nonirritating, solubilizing and stabilizing agent for indomethacin.
Chetoni, Patrizia; Panichi, L; Burgalassi, Susi; Benelli, U; Saettone, Mf
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/190465
Citazioni
  • ???jsp.display-item.citation.pmc??? 7
  • Scopus 28
  • ???jsp.display-item.citation.isi??? 27
social impact