Abstract
Itraconazole oral solution (ITCZ-OS) exerts excellent efficacy but causes adverse reactions (gastrointestinal disorders) relatively frequently. To resolve this problem, we devised ITCZ-OS gargle remedy (intake of this drug by means of gargle). The present study was undertaken to evaluate the efficacy of this therapy and to explore the mechanism for action of this preparation through analysis of drug levels in mucosal tissue and plasma. The subjects of this study were 25 patients with oral candidiasis. Each patient took ITCZ-OS by means of gargle for 2 minutes twice daily (after breakfast and supper, 10 mL/dose) for a period of 15 days. Clinical response rate was 72.0%, the Candida eradication rate was 68.0%, and the overall (clinical + mycological) response rate was 88.0%. Adverse reactions were noted in 3 cases. These results suggest that this therapy is useful as a means of treating oral candidiasis. ITCZ was detected in the tissue, and very small amounts of ITCZ and OH-ITCZ were detected from plasma. Therefore, detection of the drug components in plasma, even in small amounts, indicates the necessity of paying attention to possible systemic adverse reactions as well.
