Abstract
Purpose :
Allergic conjunctivitis (AC) is a common ocular disease with a growing incidence rate. Topical second generation antihistamines are the first-line treatment. The aim of this work was to evaluate the bioavailability of Bilastine Eye Drops, a preservative free, once daily formulation in healthy volunteers.
Methods :
A single-center phase I, multiple ophthalmic dose, open-label and one period clinical trial was conducted to evaluate the bioavailability of bilastine ophthalmic solution after multiple dose administration. Safety and tolerability were also assessed. Twelve healthy volunteers were included in this study. They were administered 1 drop of Bilastine in each eye once daily for 5 days. Blood samples were obtained at predefined times from baseline to 72h after administration. Bilastine plasma concentrations were measured in plasma by LC-MS/MS. A complete ophthalmological examination was performed at baseline and after last drug administration in order to assess the safety of this new formulation. Vital signs, electrocardiogram, safety laboratory test were also performed.
Results :
After single ophthalmic dose administration, median plasma Tmax was 2.13 h. AUC0-24 of bilastine was 19537.81 h*pg/mL and Cmax was 2793.79 pg/mL. The steady state was reached on day 2. In steady state conditions AUC(0-τ)ss of bilastine was 19512.51 h*pg/mL and Cmax,ss was 2682.26 pg/mL. Cmin,ss was 54.45 pg/mL. As secondary parameters, median Tmax,ss was 2.50 h. Fluctuation was 306.16 and Cτ,ss was 234.10 pg/mL. Neither serious adverse events nor significant analytical alterations attributable to Bilastine preservative free eye drops were detected
Conclusions :
This bioavailability study shows that Bilastine 0.6% preservative free eye drops, is rapidly absorbed after multiple dose administration. Bilastine reached maximum blood levels within 2.52 hours after administration at steady state. Moreover, Bilastine showed a good safety profile. These results support the conjunctival pathway as preferential absorption route of Bilastine.
This is a 2020 ARVO Annual Meeting abstract.