Seo M, iida H, Miura Y
Curr Med Res Opin. 1977;5(2):169-78. doi: 10.1185/03007997709110160.
A series of experiments was carried out with the antimycotic agent clotrimazole to establish MICs against a number of different yeasts and to estimate its blood levels following oral administration. Marked differences were noted between the MIC against A and B serotypes of Candida albicans in its yeast-like cell form, that against Type B being nearly 10-times higher than against Type A. Against the mycelial form, however, the MIC was much lower and there was little difference between the levels for the two serotypes. Clotrimazole administered in oral tablet form appeared to be poorly absorbed, little being transferred to the blood. Urinary levels were low and large amounts of the drug were detected in the faeces. Serum levels were below MIC levels in all cases examined. Blood levels 3-times as great as those after the same dosage in tablet form were produced when clotrimazole was given in oil solution and even with 250 mg, effective blood levels were achieved and maintained.
使用抗真菌剂克霉唑进行了一系列实验，以确定其对多种不同酵母的最低抑菌浓度（MIC），并估计口服给药后的血药浓度。观察到克霉唑对白色念珠菌酵母样细胞形态的A和B血清型的MIC存在显著差异，对B型的MIC比对A型的高近10倍。然而，对于菌丝体形态，MIC要低得多，两种血清型的水平差异不大。口服片剂形式的克霉唑吸收似乎很差，很少转移到血液中。尿液中的浓度很低，粪便中检测到大量药物。在所有检查的病例中，血清浓度均低于MIC水平。当克霉唑以油溶液形式给药时，产生的血药浓度是相同剂量片剂给药后血药浓度的3倍，即使使用250毫克，也能达到并维持有效的血药浓度。
