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Abstract #11553 Published in IGR 6-3
Effects of the preservative puriteR on the bioavailability of brimonidine in the aqueous humor of rabbits
Dong JQ; Babusis DM; Welty DF; Acheampong AA; Tang Liu D; Whitcup SMJournal of Ocular Pharmacology and Therapeutics 2004; 20: 285-292
PURPOSE: To determine aqueous humor concentrations of brimonidine given the following ophthalmic formulations in female New Zealand White Rabbits: (1) BAK-preserved brimonidine tartrate 0.20% at a pH of 6.4; (2) BAK-preserved brimonidine tartrate 0.15% at a pH of 6.4, and (3) PuriteR-preserved brimonidine tartrate 0.15% at a pH of 7.3. METHODS: Eighteen (18) animals were given a 35-μL drop of formulation into each eye. Aqueous humor samples were collected at 9 time points over 8 hours. Brimonidine concentrations were quantified using LC-MS/MS. RESULTS: The Cmax was achieved between 0.33-0.67 hours postdosing for all 3 formulations. Mean Cmax after Purite-preserved brimonidine tartrate 0.15% was 88% higher than that after BAK-preserved brimonidine tartrate 0.15% (p = 0.040), and 44% higher than that after BAK-preserved brimonidine tartrate 0.20% (p = 0.0784). AUC0-3 hr values were comparable for all 3 formulations. CONCLUSIONS: Purite-preserved brimonidine tartrate 0.15% produced higher peak concentrations than BAK-preserved brimonidine tartrate 0.15%. It also had a concentration that was comparable to BAK-preserved brimonidine tartrate 0.20%. The differences in safety may result from the change in preservative.
Dr. J.Q. Dong, Dept. of Pharmacokin./Drug Metab., Allergan, Inc., 2525 Dupont Drive, Irvine, CA 92623-9534, USA
Classification:
11.3.3 Apraclonidine, brimonidine (Part of: 11 Medical treatment > 11.3 Adrenergic drugs)
11.6 Osmotic treatment (Part of: 11 Medical treatment)