Pharmacokinetics and Safety of a Bilastine Once-Daily, Preservative-Free, Ophthalmic Formulation

Ochoa, Dolores; Román, Manuel; Belmonte, Carmen; Martı́n-Vı́lchez, Samuel; Mejía‐Abril, Gina; Abad‐Santos, Francisco; Hernández, Gonzalo; Arranz, Paula; Elgezabal, Lorena; Fernández, Nieves

doi:10.1007/s12325-021-01801-y

Cited by 7 publications

(6 citation statements)

References 37 publications

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“…The ophthalmic administration of bilastine leads to low absorption into the bloodstream. The median time for maximum plasma concentration attained within 2.5 hrs and half-life in plasma has been reported as 7.88 ± 6.72 hrs 14 . However, a recent experiment on a rabbit model for biodistribution of 0.6% bilastine eye drops showed quantifiable concentrations of bilastine up to 24 hrs in the conjunctiva tissues after installation into the eyes 15 .…”

Section: Properties Of Bilastinementioning

confidence: 99%

An emerging antihistamine drug with multiple therapeutic benefits: Bilastine

Jacob,

Thangaraj Uthra,

Gupta

et al. 2024

Pharm Sci Asia

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Histamine mediates numerous physiological processes. It is crucial in controlling allergic reactions, immune system responses, and also plays a significant role in allergic inflammation. Histamine mainly exhibits its effects in the human body by mediating through receptors such as H1, H2, H3, and H4. H1 receptor is widely distributed in major cells types such as immune and inflammatory cells. The binding of histamine to this receptor the chronotropic and vasoconstriction effects, rendering H1 receptor as an essential therapeutic target for medications that treat various allergic illnesses, including allergic rhinoconjunctivitis, urticarial, or atopic dermatitis 1 . H1 AHs, structurally distinct from histamine, stabilize the receptor's inactive conformation by acting as an inverse agonist. The first and second-generation H1 antihistamines (AHs) are inverse agonists that stabilize the inactive conformation of the receptor in its active state. First-generation agents such as bromopheniramine, dimenhydrinate, diphenhydramine, and doxylamine can frequently interact with other receptors due to poor receptor selectivity, leading to anti-cholinergic,

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Section: Properties Of Bilastinementioning

confidence: 99%

An emerging antihistamine drug with multiple therapeutic benefits: Bilastine

Jacob,

Thangaraj Uthra,

Gupta

et al. 2024

Pharm Sci Asia

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“…To prepare ten grams of SNEDDS components mixture, the oil concentration was ranged from 15 % to 30 % for each selected Smix. While the concentration of tween 60 and transcutol was calculated according to their ratio (Smix) as shown in table (1). The effects of oil concentration and Smix on the particle size distribution and emulsification time were studied.…”

Section: Formulation Of Bilastine-loaded Sneddsmentioning

confidence: 99%

“…Bilastine (BL) is a new, well tolerated second generation H1-antihistamine. It is indicated for the treatment of chronic spontaneous urticaria and seasonal rhino conjunctivitis (1) . BL is also effective in all nasal symptoms including obstruction and in allergic conjunctivitis (2) .…”

Section: Introductionmentioning

confidence: 99%

Design, Optimization and Characterization of Self-Nanoemulsifying Drug Delivery Systems of Bilastine

Abbas,

Shaimaa Nazar Abd-AlHammid

2023

IJPS

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Self-nanoemulsifying drug delivery systems are innovative methods that have the potential to resolve a variety of drug formulation issues, including solubility, stability and bioavailability. Bilastine is a potent and highly selective H1-antihistamine. The aim of this study is to develop bilastine as an oral self-nanoemulsion to enhance its permeability from prepared formulas and possibility of lymphatic transport. Based on the solubility investigations of bilastine in some oils, surfactants and cosurfactants, fifteen formulae of liquid SNEDDS were created utilizing oleic acid, tween 60 and transcutol as oil, surfactant and co-surfactant respectively. Pseudoternary phase diagrams were used to evaluate the component phase behavior and the area of the nanoemulsion. The prepared formulas were evaluated for particle size, polydispersity index, zetapotential, self-emulsification time, drug content, and robustness to dilution. When compared to the pure drug powder, the produced SMEDDS formulations showed enhanced drug release. This study's findings showed that a formula 8 with a 20% oleic acid, 40% tween 60, and 40% transcutol composition exhibited lower particle size and higher zetapotential with acceptable drug content compared to other formulas and better in-vitro drug release characteristics than pure bilastine powder. All of these criteria favor the development of self-nano emulsifying drug delivery systems as a potential approach to enhance the bioavailability of drugs like bilastine that are poorly soluble. Keywords: Bilastine, SNEDDS

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“…Therefore, a once-daily, preservative-free, bilastine ophthalmic formulation has been developed for the specific treatment of allergic conjunctivitis. Pre-clinical in vivo biodistribution and pharmacokinetic studies in humans with this formulation showed that bilastine is predominantly distributed in the conjunctiva, the intended target tissue, while it is poorly absorbed in the blood stream [31,32].…”

Section: Introductionmentioning

confidence: 99%

Efficacy of Once-Daily Ophthalmic Bilastine for the Treatment of Allergic Conjunctivitis: A Dose-Finding Study

Gomes¹,

Ciolino²,

Arranz³

et al. 2023

J Investig Allergol Clin

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Background and objectives: Bilastine is a non-sedating second-generation antihistamine for the symptomatic treatment of allergic rhinoconjunctivitis and urticaria. This trial aimed to evaluate the optimal dose, efficacy, and safety of a newly developed once-daily preservative-free ophthalmic formulation of bilastine for allergic conjunctivitis. Methods: This phase 2, single-center, double-masked, randomized study evaluated the efficacy of 3 doses of a bilastine ophthalmic formulation (0.2%, 0.4%, and 0.6%) compared to vehicle for the treatment of allergic conjunctivitis. The primary efficacy endpoint was ocular itching reduction. The Ora-CAC® Conjunctival Allergen Challenge model was used to assess ocular and nasal symptoms at the onset of action (15 minutes), 8- and 16-hours post-treatment. Tolerance and safety were also evaluated. Results: A total of 121 adults with seasonal and/or perennial ocular allergy were randomized. Bilastine ophthalmic formulation 0.2%, 0.4% and 0.6% were significantly superior (p>0.001) to vehicle for the treatment of ocular itching at 3, 5 and 7 minutes post-challenge at onset of action (15 minutes) and 8 hours post-treatment. Bilastine 0.6% was also effective at 16 hours post-treatment. Treatment differences for bilastine 0.6% were statistically significant (p<0.001) compared to vehicle at all timepoints for tearing, eyelid swelling, and nasal symptoms. No relevant adverse events were observed. Conclusions: All the tested ophthalmic bilastine doses were efficacious in rapidly reducing ocular itching. The 0.6% formulation was effective up to 16 hours post-treatment, making it suitable for once-daily administration. The new formulation was safe and well tolerated.

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Pharmacokinetics and Safety of a Bilastine Once-Daily, Preservative-Free, Ophthalmic Formulation

Cited by 7 publications

References 37 publications

An emerging antihistamine drug with multiple therapeutic benefits: Bilastine

An emerging antihistamine drug with multiple therapeutic benefits: Bilastine

Design, Optimization and Characterization of Self-Nanoemulsifying Drug Delivery Systems of Bilastine

Efficacy of Once-Daily Ophthalmic Bilastine for the Treatment of Allergic Conjunctivitis: A Dose-Finding Study

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