title: Gemifloxacin mesylate (GFM): dissolution test based on in vivo data.
abstract: Gemifloxacin mesylate (GFM) is a synthetic, broad-spectrum, fluoroquinolone antibacterial agent. It is different from other class members because it achieves adequate plasma concentrations to inhibit both topoisomerase IV and gyrase. The aim of this study was to develop and validate a dissolution test for GFM in coated tablets, using a simulated absorption profile based on in vivo data obtained from the literature. The fraction and percentage of the dose absorbed were calculated using model-dependent Loo-Riegelman approach for two compartments. The best in vitro dissolution profile was obtained using 900 mL of pH 6.0 phosphate buffer as a dissolution medium at 37 °C ± 0.5 °C and paddles at 50 rpm. The in vitro dissolution samples were analyzed using a liquid chromatography method, and the validation was performed according to USP 34 (2011). The method showed specificity, precision, accuracy, robustness and linearity. Under these conditions, a level-A in vitro-in vivo correlation was suggested (r = 0.9926). The prediction errors were calculated to determine the validity and accuracy of the suggested correlation. The dissolution test can be used to evaluate the dissolution profile of GFM-coated tablets and minimize the number of bioavailability studies as part of new formulation development.
authors: Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Pampa (UNIPAMPA), Campus Uruguaiana , Uruguaiana - RS , Brasil and.
authors: Clésio Soldateli
authors: CS
authors: Paim
authors: Bibiana
authors: B
authors: Verlindo de Araújo
authors: Nádia Maria
authors: NM
authors: Volpato
authors: Martin
authors: M
authors: Steppe
authors: Elfrides Eva Sherman
authors: EE
authors: Schapoval
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000032:analysis / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D001682:Biological Availability; D001938:Brazil; D002851:Chromatography, High Pressure Liquid; D003198:Computer Simulation; D004345:Drug Industry / Q000295:instrumentation / Q000379:methods*; D065546:Drug Liberation; D024841:Fluoroquinolones / Q000032:analysis / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D000077735:Gemifloxacin; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007408:Intestinal Absorption; D016014:Linear Models; D008954:Models, Biological; D009287:Naphthyridines / Q000032:analysis / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D015203:Reproducibility of Results; D013056:Spectrophotometry, Ultraviolet; D013608:Tablets, Enteric-Coated; D059003:Topoisomerase Inhibitors / Q000032:analysis / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics
chemical_list: D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D009287:Naphthyridines; D013608:Tablets, Enteric-Coated; D059003:Topoisomerase Inhibitors; D000077735:Gemifloxacin
keywords: Dissolution test validation; HPLC; fluoroquinolones; gemifloxacin mesylate; in vitro–in vivo correlation