Τίτλος:
Usefulness of the BioGIT system in screening for differences in early exposure in the fasted state on an a priori basis
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
The objective of the present study was to confirm the usefulness of BioGIT data in the evaluation of the impact of dose and/or formulation on early exposure after oral administration of immediate release or enabling products of low solubility active pharmaceutical ingredients (APIs) with a glass of water in the fasted state. BioGIT experiments were performed with four APIs: Compound Α (tablet, three dose levels), Compound E (capsule PiC1, capsule PiC2 and tablet), fenofibrate (Lipidil® capsule and Lipidil 145 ONE® tablet) and Compound F (HP-β-CD aqueous solution and tablet). Based on mean plasma AUC0-60min values which became available after completion of the BioGIT experiments, mean BioGIT AUC0-50min values were useful for the evaluation of the impact of dose and/or formulation on early exposure. The log-transformed ratios of mean BioGIT AUC0-50min values for two doses and/or two formulations estimated in this study and in a recent study for two diclofenac potassium products (Cataflam® tablet and Voltfast® sachet, same dose) vs. the corresponding log-transformed ratios of mean plasma AUC0-60min values (n = 7 pairs of ratios), were included in a previously established correlation between log-transformed ratios of mean BioGIT AUC0–50min values and log-transformed ratios of plasma AUC0–60min values (n = 9 pairs of ratios). The correlation between log-transformed plasma AUC0–60min ratios vs. log-transformed BioGIT AUC0–50min ratios was confirmed (n = 16 pairs of ratios, R = 0.90). Compared with the previously established correlation the statistical characteristics were improved. Based on this study, the BioGIT system could be useful as a screening tool for assessing the impact of dose and/or formulation differences on early exposure, after administration of immediate release or enabling drug products of low solubility APIs with a glass of water in the fasted state, on an a priori basis. © 2023 Elsevier B.V.
Συγγραφείς:
Kostantini, C.
Spilioti, E.
Bevernage, J.
Ceulemans, J.
Hansmann, S.
Hellemans, K.
Jede, C.
Kourentas, A.
Reggane, M.
Shah, L.
Wagner, C.
Reppas, C.
Vertzoni, M.
Περιοδικό:
International Journal of Pharmaceutics
Λέξεις-κλειδιά:
2 hydroxypropyl beta cyclodextrin; diclofenac potassium; fenofibrate; lipidil 145one; water; diclofenac; fenofibrate, aqueous solution; area under the curve; Article; controlled study; drug capsule; drug dose; drug exposure; drug formulation; drug release; drug screening; drug solubility; fasting; high performance liquid chromatography; tablet formulation; crossover procedure; diet restriction; oral drug administration; tablet manufacture; therapeutic equivalence, Administration, Oral; Area Under Curve; Cross-Over Studies; Diclofenac; Fasting; Fenofibrate; Tablets; Therapeutic Equivalency
DOI:
10.1016/j.ijpharm.2023.122670
