Comparative Fasting Bioavailability of 2 Bepotastine Formulations in Healthy Male Chinese Volunteers: An Open-Label, Randomized, Single-Dose, 2-Way Crossover Study

Shentu, Jianzhong; Zhou, Haiyan; Hu, Xiurong; Wu, Guolan; Wu, Lihua; Zhu, Meixiang; Zhai, You; Zheng, Yang; Liu, Jian

doi:10.1016/j.clinthera.2014.02.020

Cited by 1 publication

(1 citation statement)

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“…A 90% interval of the predicted concentrations obtained from the simulated population generated by PK-Sim was compared with that of the observed concentrations. In addition, we verified whether PK parameters such as C max , time to reach maximum concentration (T max ), and half-life predicted from the developed model were similar to those from previous studies [ 5 , 22 ] and were consistent with the known properties of drugs, including the urinary drug excretion ratio for 24 h. The PK data of Japanese children aged 7 to 15 who received the same tablet dose (10 mg) as adults were also compared with the simulation results of the developed PBPK model for external validation [ 6 ]. In clinical trials for children, the drug was administered after a meal, so a delayed gastric emptying time was applied to children based on the literature [ 6 , 23 ].…”

Section: Methodssupporting

confidence: 65%

Pharmacokinetic Modeling of Bepotastine for Determination of Optimal Dosage Regimen in Pediatric Patients with Allergic Rhinitis or Urticaria

Yoon,

Jin,

Kim

et al. 2024

Pharmaceutics

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Bepotastine, a second-generation antihistamine for allergic rhinitis and urticaria, is widely used in all age groups but lacks appropriate dosing guidelines for pediatric patients, leading to off-label prescriptions. We conducted this study to propose an optimal dosing regimen for pediatric patients based on population pharmacokinetic (popPK) and physiologically based pharmacokinetic (PBPK) models using data from two previous trials. A popPK model was built using NONMEM software. A one-compartment model with first-order absorption and absorption lag time described our data well, with body weight incorporated as the only covariate. A PBPK model was developed using PK-Sim software version 10, and the model well predicted the drug concentrations obtained from pediatric patients. Furthermore, the final PBPK model showed good concordance with the known properties of bepotastine. Appropriate pediatric doses for different weight and age groups were proposed based on the simulations. Discrepancies in recommended doses from the two models were likely due to the incorporation of age-dependent physiological factors in the PBPK model. In conclusion, our study is the first to suggest an optimal oral dosing regimen of bepotastine in pediatric patients using both approaches. This is expected to foster safer and more productive use of the drug.

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Section: Methodssupporting

confidence: 65%