Objective:To observe the dynamic effects of Guanxinkang on the molecule expression of hepatic cholesterol homeostasis in hyperlipidemia rats. Methods96 SD rats were randomly divided,among which 24 rats were set as the normal control group and treated with normal diet,72 rats were treated with high cholesterol diet to induce hyperlipidemia and then randomly divided into the model group, simvastatin group, Guanxinkang group. Rats were sacrificed at 4th,8th and 12th week. The levels of blood lipid were detected by biochemistry, the gene and protein expression levels of low-density lipoprotein receptor(Ldlr),scavenger receptor class B type 1(Srb1),HMG-CoA Reductase(Hmgcr) and sterol regulatory element-binding protein 2(Srebp2)were determined by real-time fluorescence quantitative PCR and Western-blot.  Results:Compared with the model group, the serum levels of cholesterol and low density lipoprotein were decreased after the treatment with Guanxinkang for 4 weeks, 8 weeks and 12 weeks, but the difference was not statistically significant (P>0.05). Compared with the model group,Guanxinkang significantly up-regulated the gene and protein expression level of Ldlr in the liver of hyperlipidemia rat (P<0.05),and significantly up-regulated the gene and protein expression level of Srebp2 in the liver of hyperlipidemia rat after treatment for 4-8 weeks and 8-12 weeks(P<0.05),with a time-dependent manner.  Conclusion:Guanxinkang can dynamically regulate the gene and protein expression of Ldlr in the liver of hyperlipidemia rats to control the blood lipid level,and may regulate the cholesterol homeostasis by adjusting the gene and protein level of Srebp2.