Dolores Ochoa, Manuel Roman, Carmen Belmonte, Samuel Martin-Vilchez, Gina Mejia-Abril, Francisco Abad-Santos, Gonzalo Hernandez, Paula Arranz, Lorena Elgezabal, Nieves Fernandez
Adv Ther . 2021 Jun 12. doi: 10.1007/s12325-021-01801-y. Online ahead of print.
Bilastine is a second-generation H1 antihistamine for allergic conditions. A new ophthalmic formulation was developed based on the efficacy and safety profiles of the oral formulation. The aim of this study was to assess the safety and pharmacokinetics of ophthalmic bilastine (6 mg/ml) in adults after one and various doses.
This was an open-label, single-centre, phase 1, bioavailability study that included 12 healthy participants (aged 18-55 years old). Participants were administered one drop of the bilastine eye formulation in each eye for five days. Serum levels of bilastine were assessed by HPLC-MS/MS and adverse drug reactions registered during administration and follow-up.
After various admininistrations, bilastine blood levels were 2682,26 ± 1615,88 pg/mL at 2,5 hours. The half-life of bilastine was 7,88 ± 6,72 h. Area under the curve was 19512,51 ± 9248,76 h/pg/mL. Dysgeusia was the main adverse event, which was mild and transient.
The ophthalmic formulation has proved to be absorbed in low amounts to the bloodstream, showing a good safety profile after administration of various doses.