Aim: Stains and cholesterol absorption inhibitors are frequently co-administered to treat patients with dyslipidemia. This study aimed to evaluate the pharmacokinetic (PK) interaction between atorvastatin and hybutimibe in healthy Chinese subjects. Methods: A randomized, open-label, three-treatment, six-period crossover study was conducted in 24 healthy Chinese subjects. Subjects received once-daily treatments for 14 days per period (14-day washout): atorvastatin 20 mg, hybutimibe 10 mg, or both combined. Geometric mean ratios (GMRs) and their 90% confidence intervals (CI) for the maximum plasma concentration (Cmax), and the area under the time-concentration curve (AUC) of atorvastatin, hybutimibe, and their metabolites between combination therapy and monotherapy were estimated. Furthermore, population pharmacokinetic (PopPK) analysis was conducted to evaluate the effect of combination therapy and other potential covariates on the PK parameters. Results: The GMRs and 90% CI of Cmax and AUC0-∞ were 0.899(74.63, 108.24) and 1.032(95.48, 111.61) respectively for atorvastatin at steady state. And the corresponding values for hybutimibe were 1.370 (116.95, 160.45) and 1.099(100.43-120.31) respectively. The PK profiles of hybutimibe and atorvastatin, as well as their metabolites were well described by the PopPK models. Covariate screening demonstrated that atorvastatin coadministration only selectively influenced hybutimibe’s apparent distribution volume (Vp/F). For atorvastatin, hybutimibe combination was included in the final model as a significant covariate on Vp/F of the parent drug with moderate difference (2620 L vs 2930 L). Conclusions: Considering the limited PK changes, therapeutic benefits and good safety profiles of the components, the interaction between atorvastatin and hybutimibe is likely to have no significant clinical impact.