Abstract: A quantitative analysis method of iodiconazole concentrations in human stratum corneum was established. Human superficial skin samples were obtained by tape stripping technique and iodiconazole concentrations were determined by LC-MS method after extraction. Ketoconazole was used as the internal standard(IS). The analytes were chromatographically separated on a Shim-pack VP-ODS C₁₈ column with the mobile phase consisting of methanol and 0. 01% formic acid aqueous solution(65 ∶35). Mass spectrometer was operated in positive ion and selective ion monitoring(SIM)mode using electrospray ionization(ESI)technique. The method showed excellent linearity over the concentration range of 0. 6-1 800 ng/mL. The recovery and the intra- and inter-batch precisions met the requirements for the determination of biological samples. The dynamic process of intradermal drug concentrations in 10 healthy volunteers after topical application of iodiconazole cream was investigated using this method. The method proved to be selective and sensitive, and suitable for the determination of iodiconazole concentration in human stratum corneum and the pharmacokinetic study after topical application of iodiconazole cream.