Comparative Bioavailability Study of a New Orodispersible Formulation of Ibuprofen Versus Two Existing Oral Tablet Formulations in Healthy Male and Female Volunteers.
Clin Ther
; 41(8): 1486-1498, 2019 08.
Article
em En
| MEDLINE
| ID: mdl-31202508
ABSTRACT
PURPOSE:
This study aimed to assess the comparative bioavailability between ibuprofen acid orodispersible tablets (Test product) and ibuprofen acid oral tablets (Reference product).METHODS:
This was a randomized, single-dose, 3-way crossover, open-label, pharmacokinetic study in 36 healthy male and female volunteers. Blood samples were taken periodically over a 12-h period after dosing to derive total plasma ibuprofen and S(+)/R(-) ibuprofen enantiomer pharmacokinetic parameters; safety profile and tolerability were evaluated throughout the study.FINDINGS:
After a single-dose administration of ibuprofen acid oral tablets (2 × 200 mg), the total ibuprofen Cmax and AUC0-t (geometric least square [LS] mean) for the Test product was 29.4 µg/mL and 100.6 h/µg/mL, respectively, and for the Reference product it was 30.6 µg/mL and 98.7 h/µg/mL. The geometric LS mean Test/Reference ratio 90% CI for both total ibuprofen Cmax (90.71-101.77) and AUC0-t (98.72-105.23) was contained entirely within the predefined 80.00%-125.00% lower and upper limits; in addition, no statistically significant difference was found in Tmax (P = 0.1819) after fasted administration of the Test and Reference products. There were 4 mild treatment emergent adverse events, considered unrelated to the study drug, reported by 2 volunteers during the study; no serious adverse events, no suspected unexpected serious adverse events. and no clinically significant changes in laboratory safety, vital signs, or 12-lead ECG measurements were reported. The enantiomer-specific analysis mirrored that of total ibuprofen, with the Cmax and AUC0-t LS mean Test/Reference ratio 90% CI for both ibuprofen S(+) and R(-) enantiomers contained entirely within the predetermined 80%-125.00% limits. IMPLICATIONS This study found that ibuprofen acid 200 mg orodispersible tablets and ibuprofen acid 200 mg tablets met the regulatory criteria for bioequivalence for AUC0-t and Cmax. Post hoc analysis of ibuprofen both S(+) and R(-) enantiomers mirrored the findings for total ibuprofen. All investigational products were found to be well tolerated. Clinicaltrials.gov identifier NCT03180879.Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Anti-Inflamatórios não Esteroides
/
Ibuprofeno
Tipo de estudo:
Clinical_trials
/
Prognostic_studies
Limite:
Adult
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Female
/
Humans
/
Male
Idioma:
En
Revista:
Clin Ther
Ano de publicação:
2019
Tipo de documento:
Article