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Comparative pharmacokinetics and bioavailability of brimonidine following ocular administration and dermal application of brimonidine tartrate ophthalmic solution and gel in subjects with moderate to severe facial erythema of rosacea.

Br J Dermatol. 2014 Feb 7;

Authors: Benkali K, Leoni M, Rony F, Bouer R, Fernando A, Graeber M, Wagner N

Abstract
A pharmacokinetics (PK) study was conducted to perform an intra-individual comparison of the systemic exposure obtained with brimonidine tartrate (BT) gel (0.07%, 0.18%, and 0.5%) under maximal use conditions for 29 days and with BT ophthalmic solution 0.2% as reference treatment, in subjects with moderate to severe facial erythema of rosacea. Quantifiable exposure (≥10 pg/mL) was detected in 96 subjects who received BT ophthalmic 0.2% solution as a TID (Three times a day) regimen for one day (3 doses) with a mean Cmax of 54 ± 28 pg/mL and a mean AUC0-24h of 568 ± 277 pg.h/mL. Conversely, daily topical application of BT gel for 29 days resulted in quantifiable systemic exposure in 22%, 48%, 71%, and 79% of subjects who received BT gel 0.07% BID (Twice a day), 0.18% QD (Once a Day), 0.18% BID, and 0.5% QD, respectively. Systemic exposures obtained with BT gels increased with the applied dose with no drug accumulation throughout the treatment duration. At the end of the 29-day treatment, the mean Cmax values ranged between 13 and 25 pg/mL and the mean AUC0-24h values ranged between 42 and 290 pg.h/mL for the BT gels. The systemic exposure observed with the highest dose of BT gel (0.5% QD) was significantly lower than the systemic levels observed for the ophthalmic solution 0.2% after a one day TID regimen. Collectively, PK assessment showed that the systemic safety profile of the BT gel may be considered better than the marketed ophthalmic solution. This article is protected by copyright. All rights reserved.

PMID: 24506775 [PubMed - as supplied by publisher]

http://www.ncbi.nlm.nih.gov/pubmed/24506775?dopt=Abstract = URL to article