Chromatographic/mass spectrometric method for the estimation of itraconazole and its metabolite in human plasma. Application to a bioequivalence study.
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.
Grabowski
Tomasz
T
Centre of Pharmacokinetics Research FILAB, Ravimed Sp. z o. o., Łajski, Poland. t.grabowski@filab.com.pl
Swierczewska
Anna
A
Borucka
Beata
B
Sawicka
Renata
R
Sasinowska-Motyl
Małgorzata
M
Gumułka
Stanisław Witold
SW
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
D000935:Antifungal Agents; C084794:hydroxyitraconazole; D017964:Itraconazole