Effect of food on the pharmacokinetics of YH4808, a potassium-competitive acid blocker, after single- and multiple-oral dosing in healthy subjects.

Purpose: YH4808 is a potassium-competitive acid blocker, developed for the treatment of acid-related disorders. Two clinical studies in healthy male subjects were conducted to evaluate the effect of food on the pharmacokinetics of YH4808.Methods: The first study, a randomized, three-treatment, three...

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Published in:European Journal of Clinical Pharmacology Vol. 74; no. 10; pp. 1261 - 1273
Main Authors: Kim, Eunwoo, Kim, Anhye, Yi, Sojeong, Kim, Yu Kyong, Jang, Seong Bok, Byun, Hae Mi, Yoon, Seo Hyun, Cho, Joo-Youn, Jang, In-Jin, Yu, Kyung-Sang, Lee, SeungHwan
Format: research tables/charts randomized controlled trial Journal Article
Published: Springer Nature Oct2018
Online Access:View this record in EBSCOhost
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      dt: Oct2018
      vid: 74
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      pub: Springer Nature
      place: New York, New York
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        10.1007/s00228-018-2502-9
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        atl: Effect of food on the pharmacokinetics of YH4808, a potassium-competitive acid blocker, after single- and multiple-oral dosing in healthy subjects.
      aug:
        au:
          Kim, Eunwoo
          Kim, Anhye
          Yi, Sojeong
          Kim, Yu Kyong
          Jang, Seong Bok
          Byun, Hae Mi
          Yoon, Seo Hyun
          Cho, Joo-Youn
          Jang, In-Jin
          Yu, Kyung-Sang
          Lee, SeungHwan
        affil: Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul, Republic of Korea
      sug:
        subj:
          Antacids Pharmacokinetics
          Antacids Administration and Dosage
          Food
          Human
          Randomized Controlled Trials
          Crossover Design
          Dietary Fats
          Meals
          Fasting
          Antacids Blood
      ab: Purpose: YH4808 is a potassium-competitive acid blocker, developed for the treatment of acid-related disorders. Two clinical studies in healthy male subjects were conducted to evaluate the effect of food on the pharmacokinetics of YH4808.Methods: The first study, a randomized, three-treatment, three-period, crossover study, compared pharmacokinetics of YH4808 (300 mg) after a single dose at fed state with a standard or a high-fat meal to those at fasted state. The second study, a randomized, two-treatment, two-period, crossover study, investigated pharmacokinetics at fasted or fed state with a standard meal after twice daily dose of YH4808 (100 mg) for 7 days. Bloods for pharmacokinetic evaluation were sampled up to 48 h post-dose and 24 h post-dose at steady state, respectively. The pharmacokinetic parameters were estimated by non-compartmental method.Results: After single dosing, the geometric means of maximum plasma concentration increased by 1.2 and 2.1 times in the fed states with a standard meal and a high-fat meal, respectively, of that in fasted state. Corresponding values of area under the plasma concentration-time curve (AUC) from time 0 to the last measurable time point increased by 1.8 and 2.8 times, respectively. After multiple dosing, the geometric mean for 24-h AUC at steady state slightly increased in fed state by 1.1 times of that in fasted state.Conclusions: As fat content of the food increased, the systemic exposure of YH4808 after single dosing increased. However, systemic exposures at steady state after multiple dosing between fasted and fed states were similar.Trial registration: <ext-link>ClinicalTrials.gov</ext-link> registry no.: NCT01520012
      pubtype: Academic Journal
      doctype:
        research
        tables/charts
        randomized controlled trial
        Journal Article
      ougenre: Article
    language: English
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