Bioequivalence Evaluation of Three Pediatric Oral Formulations of Bilastine in Healthy Subjects: Results from a Randomized, Open Label, Crossover Study

Sádaba, Belén; Azanza, J. R.; García-Bea, Aintzane; Labeaga, Luis; Campo, Cristina; Valiente, Román

doi:10.1007/s13318-019-00596-2

Cited by 6 publications

(2 citation statements)

References 19 publications

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“…The bioequivalence study confirmed that bilastine could be used interchangeably as an orodispersible tablet or an oral solution, and both formulations. These were well tolerated 13 . Pharmacokinetics (PK) of the intravenous route of administration of bilastine in man was predicted using a model developed with allometry and a semi-physiological method on the data of preclinical animal studies and oral administration of bilastine to man 16 .…”

Section: Properties Of Bilastinementioning

confidence: 94%

“…The maximum plasma drug concentration was measured at 1.31 hrs through the oral route of administration of bilastine 12 . However, no meaningful differences were reported in the bioequivalence trials of three pediatric oral formulations in children 13 . The ophthalmic administration of bilastine leads to low absorption into the bloodstream.…”

Section: Properties Of Bilastinementioning

confidence: 94%

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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: 94%

Section: Properties Of Bilastinementioning

confidence: 94%

An emerging antihistamine drug with multiple therapeutic benefits: Bilastine

Jacob,

Thangaraj Uthra,

Gupta

et al. 2024

Pharm Sci Asia

View full text Add to dashboard Cite

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Bioequivalence and Safety of Bilastine 20 mg Orodispersible Tablets and Conventional Tablets: A Randomized, Single-Dose, Two-Period Crossover Study in Healthy Volunteers Under Fasting Conditions

Román,

Ochoa,

Martin

et al. 2024

Drugs R D

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Background and Objective Orodispersible tablets (ODT) rapidly dissolve in the oral cavity and can improve patient’s convenience. This pharmacokinetic study assessed the bioequivalence of a novel 20 mg ODT formulation of bilastine compared with bilastine 20 mg tablets in healthy volunteers under fasting conditions. Methods A phase I, single-center, open-label, two-period, two-sequence crossover randomized clinical trial was conducted. The study comprised two periods, in which participants were administered a single oral dose of bilastine 20 mg in the form of ODT as the test product, or conventional tablets as the reference product, and a washout of 7 days between each period. Blood samples were collected for up to 72 h. Bioequivalence was established if the 90% confidence intervals of the C max and AUC 0–t were within the acceptance range (80−125%). Safety was evaluated at the follow-up visit (days 4−7 after the second dose) and throughout the study. Results A total of 42 healthy volunteers were randomized, and 41 completed the study. Pharmacokinetic parameters were comparable for both formulations after a single dose of 20 mg. Bilastine ODT and conventional tablets were bioequivalent as the 90% confidence intervals of the test over reference ratios were within the predefined range (80−125%). Both formulations were well tolerated and showed a similar safety profile. Conclusions Bilastine ODT was bioequivalent to the reference treatment formulated as conventional tablets when administered as a single oral dose of 20 mg under fasting conditions. Both formulations showed a similar tolerability and safety profile, with no serious adverse events or significant analytical alterations reported. Trial Registration: 2019-004071-39. Date of authorization: 10 December 2019.

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