Wildfeuer A, Laufen H, Yeates R A, Zimmermann T
Mycoses. 1996;39 Suppl 1:123-6. doi: 10.1111/j.1439-0507.1996.tb00518.x.
Administration of fluconazole capsules is of proven worth in the treatment of candidosis of the mucous membranes, particularly in immunocompromised patients. An additional topical effect on the course of oropharyngeal and oesophageal candidosis can be expected when fluconazole is administered as a suspension. For this reason a crossover pharmacokinetic study with 12 healthy volunteers was carried out, in which the concentrations of the antimycotic were measured in saliva and plasma, after oral administration of 100 mg fluconazole as either a capsule or as a suspension. The time-courses of the concentration of fluconazole after the two formulations were very similar in plasma, but significantly different in saliva. The mean Cmax for fluconazole in saliva was 551 micrograms/ml 5 min after ingestion of the suspension and 3 micrograms/ml 4 h after taking the capsule. Over the observation time (0-96 h) the concentration of the antimycotic in saliva was more than 80% higher with the suspension than with the capsule.
氟康唑胶囊在治疗粘膜念珠菌病方面已被证明具有价值，尤其适用于免疫功能低下的患者。当氟康唑以混悬液形式给药时，预计对口腔和食管念珠菌病的病程会有额外的局部作用。因此，对12名健康志愿者进行了一项交叉药代动力学研究，在口服100mg氟康唑胶囊或混悬液后，测量唾液和血浆中抗真菌药的浓度。两种制剂给药后，氟康唑在血浆中的浓度-时间曲线非常相似，但在唾液中则有显著差异。服用混悬液后5分钟，唾液中氟康唑的平均Cmax为551微克/毫升，服用胶囊后4小时为3微克/毫升。在观察期（0-96小时）内，混悬液给药后唾液中抗真菌药的浓度比胶囊给药高80%以上。
