Chromatographic/Mass Spectrometric Method for the Estimation of Itraconazole and its Metabolite in Human Plasma

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 °C for 95 days. The developed method was successfully used for a comparative 2x2 period, crossover bioequivalence study of two preparations of ITR (Itrakonazol Genexo 100 mg as the test drug) performed on 36 healthy volunteers.

Key words

Antifungal drugs - CAS 84625-61-6 - CAS 112559-91-8 - HPLC/mass spectrometry - Hydroxyitraconazole, bioavailability - Itraconazole, bioavailability - Itrakonazol Genexo

• References

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