Abstract

1.In this study, the pharmacokinetics of new triazole antifungal iodiconzole creams at target sites after single-dose topical application was investigated.

2.30 healthy Chinese volunteers were randomly divided into three groups after being stratified by sex, each group was given a single topical dose of 1%, 2%, 4% iodiconazole cream (0.4 g). Stratum corneum (SC) samples of treated sites were collected by tape-stripping method after the chosen contact times, and were extracted and analysed by a validated LC-MS method.

3.After single-dose topical application of 1%, 2%, 4% iodiconazole creams, the C_max of iodiconazole in SC was 1.2 ± 0.7, 2.2 ± 1.0, 2.4 ± 1.0 mg/g; T_max was 3.3 ± 1.1, 2.9 ± 1.1, 3.8 ± 0.4 h; t_1/2 was 6.6 ± 3.4 h, 7.2 ± 4.1 h, 5.9 ± 2.9 h; AUC_0-t was 10.9 ± 3.0, 20.8 ± 10.4, 20.9 ± 7.9 mg·h/g; AUC_0-∞ was 11.6 ± 2.9, 23.5 ± 14.4, 22.2 ± 8.9 mg·h/g, respectively. The results showed that C_max, AUC_0-t and AUC_0-∞ did not increase proportionately with dose, which could also be due to the drug being saturated in the formulation at ∼2%.

4.The results of this study could provide reference for the clinical medication and further study of the formulations.