Aim To investigate the effects of Xuezhikang (XZK) on low-density lipoprotein (LDL) subfractions and oxidized low-density lipoprotein (ox-LDL) in patients with hyperlipidemia. Methods A total of 40 subjects (20 patients with hyperlipidemia and 20 healthy subjects) who were not treated with lipid-lowering drugs were selected consecutively and divided into the XZK group (n=20) and the control group (n=20). The plasma LDL subfractions, ox-LDL were examined by using the Lipoprint system at baseline and again after 8 weeks. Results Data showed that XZK could significantly decrease not only plasma LDLC levels, total cholesterol, triglycerides, and apolipoprotein B (P＜0.05), but also ox-LDL (P＜0.05). At the same time, XZK reduced the concentration of small LDLC (P＜0.05) and the percentage of the small LDL subfraction (P＜0.05). Conclusion XZK treatment for 8 weeks significantly improved the blood lipid profile, reduced the concentration and percentage of atherogenic small LDLC, and reduced the level of oxidative stress.