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Huppertz, Andrea; Bollmann, Johanna; Behnisch, Rouven; Bruckner, Thomas; Zorn, Markus; Burhenne, Jürgen; Haefeli, Walter E.; Czock, David

Differential Effect of a Continental Breakfast on Tacrolimus Formulations With Different Release Characteristics

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  • Media type: E-Article
  • Title: Differential Effect of a Continental Breakfast on Tacrolimus Formulations With Different Release Characteristics
  • Contributor: Huppertz, Andrea; Bollmann, Johanna; Behnisch, Rouven; Bruckner, Thomas; Zorn, Markus; Burhenne, Jürgen; Haefeli, Walter E.; Czock, David
  • Published: Wiley, 2021
  • Published in: Clinical Pharmacology in Drug Development, 10 (2021) 8, Seite 899-907
  • Language: English
  • DOI: 10.1002/cpdd.924
  • ISSN: 2160-763X; 2160-7648
  • Origination:
  • Footnote:
  • Description: AbstractFood reduces tacrolimus bioavailability after immediate‐release tacrolimus (IR‐Tac) and after a new prolonged‐release tacrolimus formulation (PR‐Tac), when using a high‐fat breakfast, but the effects of a continental breakfast on PR‐Tac are unknown. In an open‐label, 4‐phase, randomized, 2‐sequence, crossover pharmacokinetic trial, 36 healthy volunteers (18 females) received single 5‐mg tacrolimus doses as PR‐Tac and as IR‐Tac fasted or with a standardized continental breakfast. Tacrolimus pharmacokinetics were analyzed using noncompartmental methods and mixed‐model analysis of variance. The continental breakfast significantly decreased average tacrolimus exposure (area under the plasma concentration–time curve) with both preparations (IR‐Tac, 67%; 90% confidence interval [CI], 59%‐75%; P < .01; and PR‐Tac, 79%; 90%CI, 70%‐89%; P < .01) with a nonsignificant difference between both preparations (P = .10). The maximum concentration (Cmax) and the time to maximum concentration (tmax) were significantly affected only after IR‐Tac (Cmax IR‐Tac, 39%; 90%CI, 34%‐45%; P < .01; and PR‐Tac, 87%; 90%CI, 76%‐101%; P = .11; tmax IR‐Tac, 212%, 90%CI, 179%‐252%; P < .01; and PR‐Tac, 101%; 90%CI, 86%‐120%; P = .89), which was significantly different between both preparations (P < .01). Considering switching from IR‐Tac to PR‐Tac, predicted dose requirements differed according to the timing of drug intake in relation to food. In conclusion, a continental breakfast decreased average tacrolimus exposure of both preparations to a similar extent. Cmax and tmax were affected only after IR‐Tac. The effect of a standardized continental breakfast on PR‐Tac was considerably smaller than previously reported effects of a high‐fat breakfast on PR‐Tac.