| Online-Ressource |
Verfasst von: | Huppertz, Andrea [VerfasserIn]  |
| Bollmann, Johanna [VerfasserIn]  |
| Behnisch, Rouven [VerfasserIn]  |
| Bruckner, Thomas [VerfasserIn]  |
| Zorn, Markus [VerfasserIn]  |
| Burhenne, Jürgen [VerfasserIn]  |
| Haefeli, Walter E. [VerfasserIn]  |
| Czock, David [VerfasserIn]  |
Titel: | Differential effect of a continental breakfast on tacrolimus formulations with different release characteristics |
Verf.angabe: | Andrea Huppertz, Johanna Bollmann, Rouven Behnisch, Thomas Bruckner, Markus Zorn, Jürgen Burhenne, Walter E. Haefeli, and David Czock |
Jahr: | 2021 |
Umfang: | 9 S. |
Illustrationen: | Illustrationen |
Fussnoten: | Gesehen am 11.09.2023 |
Titel Quelle: | Enthalten in: Clinical pharmacology in drug development |
Ort Quelle: | Oxford [u.a.] : Wiley-Blackwell, 2012 |
Jahr Quelle: | 2021 |
Band/Heft Quelle: | 10(2021), 8, Seite 899-907 |
ISSN Quelle: | 2160-7648 |
Abstract: | Food 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. |
DOI: | doi:10.1002/cpdd.924 |
URL: | kostenfrei: Volltext: https://doi.org/10.1002/cpdd.924 |
| kostenfrei: Volltext: https://onlinelibrary.wiley.com/doi/abs/10.1002/cpdd.924 |
| DOI: https://doi.org/10.1002/cpdd.924 |
Datenträger: | Online-Ressource |
Sprache: | eng |
Sach-SW: | continental breakfast |
| food effects |
| immediate-release tacrolimus |
| pharmacokinetics |
| prolonged-release tacrolimus |
K10plus-PPN: | 1859251889 |
Verknüpfungen: | → Zeitschrift |
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Lokale URL UB: | Zum Volltext |
Differential effect of a continental breakfast on tacrolimus formulations with different release characteristics / Huppertz, Andrea [VerfasserIn]; 2021 (Online-Ressource)