Other Antibiotics Azole Antifungals

Itraconazole and its active metabolite (hydroxyitra-conazole) in serum are analysed with a Lichrospher RP8 column using a mobile phase of acetonit-rile-water (62 : 38) containing 0.05% diethylamine. The pH of the mobile phase is adjusted to 6.0 with 30% acetic acid. Itraconazole and hydroxyitra-conazole are detected at 258 nm with detection limits of 10 and 7 ng mL"1, respectively. Serum is extracted with heptane-isoamyl-alcohol (9 : 1).

Itraconazole and hydroxyitraconazole in plasma and tissue are also analysed with an ODS column using a mobile phase of water-acetonitrile-diethylamine (42 : 58 : 0.05). The pH of the mobile phase is adjusted to 2.45 with 85% phosphoric acid. Itraconazole and hydroxyitraconazole are detected fluorometrically at 260 nm excitation and 365 nm emission. Detection limits of itraconazole are 5ngmg"1 and 5ngmL"1 for tissue biopsy and plasma, respectively. Itraconazole in tissue or plasma is extracted with methanol.

Fluconazole in plasma is analysed with an octyl column using a mobile phase of water-acetonitrile (72:28). Fluconazole is detected at 260 nm with a detection limit of 0.4 igmL"1. Plasma is de-proteinized with acetonitrile.

Miconazole in plasma is analysed with an ODS column using a mobile phase of methanol-aceto-nitrile-0.01 mol L"1 phosphate buffer (pH 7.0, 36 : 36 : 28). Miconazole is detected at 230 nm with a detection limit of 5 ng mL"1. Plasma is treated with an octadecyl solid-phase extraction column prior to HPLC analysis.

Econazole in serum is determined with an ODS column using a mobile phase of 0.01 mol L"1 potassium dihydrogen phosphate-methanol (3 : 7), with the pH being adjusted to 4.5. Econazole is detected at 220 nm with a detection limit of 40 ng mL"1.

Sulconazole in plasma is analysed with an ODS column using a mobile phase of acetonitrile-0.01 mol L"1 phosphate buffer (pH 8, 66 : 34). Sul-conazole is detected at 229 nm with a detection limit of less than 0.5 igmL"1.

Some of the azole antifungals are used clinically as the racemates, and the enantio-specific HPLC conditions with a chiral stationary phase, tris(chloro-methylphenylcarbamate)s of cellulose, are reported. The mobile phase is w-hexane-2-propanol (85 : 15) for separation of enantiomers of enilconazole, econazole, miconazole and ornidazole, and w-hexane-2-propanol (9:1) for bifonazole enantiomers. A similar type of cellulosic chiral stationary phase (Chiralcel-OD) with a mobile phase of n-hexane-2-propanol (9 : 1) is used for separation of sulconazole enantiomers.

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