Hülsewede J W, Dermoumi H, Ansorg R
Institute of Medical Microbiology, University of Essen, Germany.
Zentralbl Bakteriol. 1995 Oct;282(4):457-64. doi: 10.1016/s0934-8840(11)80719-x.
The concentrations of itraconazole and its active metabolite, hydroxy-itraconazole, were determined in the sera of 49 patients having received itraconazole for therapeutic or prophylactic purposes. Measurements by HPLC were compared with a biological assay using a strain of Paecilomyces variotii as test organism and itraconazole as standard. The concentration of hydroxy-itraconazole in serum was on average 1.6 times higher than the concentration of itraconazole. The sum of itraconazole and hydroxy-itraconazole concentrations determined by HPLC showed a linear relationship with the concentrations obtained by the bioassay (r = 0.94). The biological method gives approximately 20% higher values than the HPLC method indicating that hydroxy-itraconazole is biologically more active than itraconazole. As the values of the Paecilomyces variotii bioassay are in the same range as the HPLC measurements, it is concluded that both methods are suitable for the monitoring of itraconazole medication.
在49例接受伊曲康唑治疗或预防的患者血清中测定了伊曲康唑及其活性代谢产物羟基伊曲康唑的浓度。采用高效液相色谱法（HPLC）的测定结果与使用一株变幻青霉作为测试菌株、伊曲康唑作为标准品的生物测定法进行了比较。血清中羟基伊曲康唑的浓度平均比伊曲康唑的浓度高1.6倍。HPLC测定的伊曲康唑和羟基伊曲康唑浓度之和与生物测定法获得的浓度呈线性关系（r = 0.94）。生物方法得出的值比HPLC方法高出约20%，这表明羟基伊曲康唑在生物学上比伊曲康唑更具活性。由于变幻青霉生物测定法的值与HPLC测量值处于同一范围，因此得出结论，两种方法均适用于监测伊曲康唑用药情况。
