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

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

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

Br J Dermatol. 2014 Jul;171(1):162-9. doi: 10.1111/bjd.12881. Epub 2014 Jul 16.

PubMed ID
24506775 [ View in PubMed
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Abstract

BACKGROUND: Persistent facial erythema is the most common primary pathological feature of rosacea, the only treatment for which is brimonidine tartrate (BT) gel. OBJECTIVES: To assess the relative bioavailability of topical BT gel in comparison with the ophthalmic BT solution. METHODS: A pharmacokinetic study was conducted to compare intraindividual systemic exposures after dermal application of BT gel (0.07%, 0.18% and 0.5%) under maximal use conditions in patients with moderate-to-severe facial erythema associated with rosacea, and administration of BT ophthalmic solution 0.2%. RESULTS: Patients who received BT ophthalmic solution 0.2% three times a day for 1 day had a mean Cmax of 54 +/- 28 pg mL(-1) and a mean 0-24-h area under the curve (AUC0-24 h ) of 568 +/- 277 pg h mL(-1) . Topical application of BT gel for 29 days resulted in quantifiable systemic exposure in 22%, 48%, 71% and 79% of patients who received BT gel 0.07% twice daily, 0.18% once daily, 0.18% twice daily and 0.5% once daily, respectively. The mean Cmax values for the BT gels ranged between 13 and 25 pg mL(-1) , and mean AUC0-24 h values ranged between 42 and 290 pg h mL(-1) . Systemic exposure increased with applied dose, with no drug accumulation for the duration of treatment. The systemic exposure observed with the highest dose of BT gel (0.5% once daily) was significantly lower than the systemic levels observed for the ophthalmic solution. 0.2% apply for all the concentrations. CONCLUSIONS: The systemic safety profile of BT gel may be considered better than that of the ophthalmic solution.

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