Graybill J R, Ahrens J
Sabouraudia. 1984;22(6):445-53. doi: 10.1080/00362178485380721.
A new antifungal triazole, itraconazole (R51211), was compared with ketoconazole in treatment of murine cryptococcosis. Itraconazole is sparingly soluble in water, and must be administered orally in solvents such as polyethylene glycol. Serum concentrations are lower than those achieved with ketoconazole, but sustained for longer periods. Itraconazole was more effective than ketoconazole by MIC, but was similar to ketoconazole by minimum fungicidal concentration. Both drugs prolonged equally survival after intraperitoneal or intracerebral challenge with Cryptococcus neoformans. Tissue counts of C. neoformans were similar in mice treated with either drug. Neither drug sterilized brains of mice challenged intracerebrally. Itraconazole appears equally potent as ketoconazole, but in this model does not appear to offer any therapeutic advantage over ketoconazole.
一种新型抗真菌三唑类药物伊曲康唑（R51211）与酮康唑用于治疗小鼠隐球菌病的效果进行了比较。伊曲康唑在水中溶解度低，必须以聚乙二醇等溶剂口服给药。其血清浓度低于酮康唑，但持续时间更长。就最低抑菌浓度（MIC）而言，伊曲康唑比酮康唑更有效，但就最低杀菌浓度而言，二者相似。用新型隐球菌进行腹腔或脑内攻击后，两种药物延长小鼠存活时间的效果相同。用这两种药物治疗的小鼠体内新型隐球菌的组织计数相似。两种药物均不能使脑内攻击小鼠的脑部除菌。伊曲康唑似乎与酮康唑效力相当，但在该模型中，与酮康唑相比似乎没有任何治疗优势。
