Background: Cilostazol is widely used as an antiplatelet drug in patients with intermittent claudication and peripheral arterial disease. Ginkgo biloba extract is prescribed in the management of circulatory disorders in peripheral arteries. Thus a fixed-dose combination of the two drugs has been under clinical development. The pharmacokinetics of cilostazol and safety profiles were compared between coadministration of cilostazol and Ginkgo biloba extract, and that of a fixed-dose combination of the two drugs. Methods: A randomized, open-label, single-dose, two-treatment, two-period, two-sequence crossover study was conducted in 26 healthy male volunteers. Subjects were administered cilostazol 100 mg and Ginkgo biloba extract 80 mg concomitantly and a fixed-dose combination of the two drugs with a 7-day washout in between. Plasma concentrations of cilostazol were determined by liquid chromatography-tandem mass spectrometry. Safety profiles were assessed by physical examinations, electrocardiograms, vital signs, laboratory testings, and monitoring adverse events. Results: Median $T_{max}$ of cilostazol was 3.0 and 4.0 hours after administration of cilostazol and Ginkgo biloba extract concomitantly and fixed-dose combination of the two drugs, respectively. The geometric mean ratio (90% confidence intervals) of the fixed dose combination to the coadministration for $C_{max}$ was 0.95 (0.87-1.05) and that for $AUC_{last}$ was 1.03 (0.96-1.10). The most frequently reported adverse event was headache, reported by 14 subjects. There was no difference of adverse event occurrences between two treatment groups. No serious adverse events were reported. Conclusion: Pharmacokinetics of cilostazol and safety were comparable between coadministration of cilostazol and Ginkgo biloba extract, and administration of a fixed-dose combination of the two drugs.