title: Chromatographic/mass spectrometric method for the estimation of itraconazole and its metabolite in human plasma. Application to a bioequivalence study.
abstract: A HPLC/mass spectrometry method for the estimation of itraconazole (CAS 84625-61-6, ITR) and its active metabolite hydroxyitraconazole (CAS 112559-91-8, HOX) in human plasma was developed. Terconazole (CAS 67915-31-5) was used as an internal standard. The analytical method was fully validated according to FDA and EMEA requirements. The accuracy and precision of the developed method was satisfactory and stability studies showed an acceptable variation (below 15%) of ITR and HOX concentrations when the samples were stored frozen at -75 degrees C for 95 days. The developed method was successfully used for a comparative 2 x 2 period, crossover bioequivalence study of two preparations of ITR (Itrakonazol Genexo 100 mg as the test drug) performed on 36 healthy volunteers.
authors.affiliation: Centre of Pharmacokinetics Research FILAB, Ravimed Sp. z o. o., Łajski, Poland. t.grabowski@filab.com.pl
authors.forename: Tomasz
authors.initials: T
authors.lastname: Grabowski
authors.forename: Anna
authors.initials: A
authors.lastname: Swierczewska
authors.forename: Beata
authors.initials: B
authors.lastname: Borucka
authors.forename: Renata
authors.initials: R
authors.lastname: Sawicka
authors.forename: Małgorzata
authors.initials: M
authors.lastname: Sasinowska-Motyl
authors.forename: Stanisław Witold
authors.initials: SW
authors.lastname: Gumułka
mesh_terms: D000328:Adult; D000935:Antifungal Agents / Q000097:blood*; D019540:Area Under Curve; D001711:Biotransformation; D002138:Calibration; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D006801:Humans; D017964:Itraconazole / Q000031:analogs & derivatives / Q000097:blood*; D008297:Male; D011786:Quality Control; D012015:Reference Standards; D015203:Reproducibility of Results; D021241:Spectrometry, Mass, Electrospray Ionization; D013810:Therapeutic Equivalency; D055815:Young Adult
chemical_list: D000935:Antifungal Agents; C084794:hydroxyitraconazole; D017964:Itraconazole