Five ophthalmic formulations containing 5% 4-biphenylacetic acid (BPAA), a potent non-steroidal anti-inflammatory agent, were prepared and their tolerability and activity were evaluated after topical administration to the rabbit eye. Among the assayed formulations, a gel containing Carbopol 940®, a water-in-oil emulsion and an absorption ointment did not cause any significant conjunctival congestion and elicited significant anti-inflammatory activity in an ocular NaOH-induced inflammation model. The Carbopol 940® ointment was the most effective in reducing eye inflammation after a 3-days treatment. To correlate the pharmacological activity with drug availability from ointments, an absorption simulator was used to investigate the in vitro release of BPAA. The results agreed with the in vivo studies, showing a sharp higher diffusion rate of BPAA from water-soluble base formulations.
Effect of different ointment bases on ocular anti-inflammatory activity of 4-biphenylacetic acid in the rabbit
Pignatello R.;
1990-01-01
Abstract
Five ophthalmic formulations containing 5% 4-biphenylacetic acid (BPAA), a potent non-steroidal anti-inflammatory agent, were prepared and their tolerability and activity were evaluated after topical administration to the rabbit eye. Among the assayed formulations, a gel containing Carbopol 940®, a water-in-oil emulsion and an absorption ointment did not cause any significant conjunctival congestion and elicited significant anti-inflammatory activity in an ocular NaOH-induced inflammation model. The Carbopol 940® ointment was the most effective in reducing eye inflammation after a 3-days treatment. To correlate the pharmacological activity with drug availability from ointments, an absorption simulator was used to investigate the in vitro release of BPAA. The results agreed with the in vivo studies, showing a sharp higher diffusion rate of BPAA from water-soluble base formulations.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
