Objective To investigate the pharmacokinetic profiles and safety of clevidipine butyrate injectable emulsion in Chinese healthy subjects, following intravenous administration with gradually increasing doses. Methods From June to July 2020, 12 Chinese healthy adult subjects were enrolled in the single-center, single-arm, open-label clinical trial. The gradually increasing doses were 1, 2, 4 and 6 mg/h, starting with the initial infusion rate of 1 mg/h. Each dose was infused for 2 min before increasing to the next dose. After reaching 6 mg/h, the infusion rate was maintained for 20 min. Plasma concentrations of clevidipine and its metabolite H152/81 were detected using high performance liquid chromatography-tandem mass spectrometry. Pharmacokinetic parameters were calculated by non-compartmental analysis using WinNonlin 8.0. Data following a normal distribution were presented as mean ± standard deviation, while data following a log-normal distribution were presented as geometric mean ×/÷ geometric standard deviation. Results Pharmacokinetic parameters of clevidipine were as follows: elimination half-life (t1/2) (3.79×/÷2.35) min, peak concentration (Cmax) (11.71±3.79) ng/mL, area under concentration-time curve from time 0 to the last measurable concentration (AUC0–t) (222.89±61.79) min·ng/mL, area under concentration-time curve from time 0 extrapolated to infinite time (AUC0–∞) (233.35±78.64) min·ng/mL, and median time to peak concentration (Tmax) 18.00 min. Pharmacokinetic parameters of H152/81 were as follows: t1/2 (194.68×/÷1.42) min, Cmax (162.00±23.35) ng/mL, AUC0–t (12794.40±1976.56) min·ng/mL, AUC0–∞ (41215.86±10110.90) min·ng/mL, and median Tmax 31.00 min. Following the administration, clevidipine rapidly affected heart rate and blood pressure. The heart rates of subjects increased slightly, and the decrease in diastolic blood pressure was greater than that in systolic blood pressure. The effects disappeared within 4 min after the infusion ended. Only 1 mild adverse event was reported. Conclusion Clevidipine shows a short half-life, as well as good safety and tolerability in Chinese healthy subjects.