Pinelliae Rhizoma Praeparatum (PRP) as traditional Chinese medicine had been used for hepatic diseases in combinative forms.But the effect of PRP was not clear when used as single.So to explore the hepatoprotective/hepatotoxin of PRP is necessary.The activities of PRP were investigated in acetaminophen-induced hepatic injury mice.Liver function markers, hepatic oxidative stress markers were evaluated.Bile acids metabolic transports and Nrf2 were detected.As a drug for liver diseases, PRP slightly restored the parameters towards normal in model mice only in low dosage, also no antioxidant activity and effect on Nrf2.Cholestasis was significantly elevated in model mice when pretreatment with routine or high dosage of PRP, but had no effect on normal mice.Bsep and Mrp2 in model mice were markedly increased when pretreatment of low dose PRP, but significantly decreased in routine or high dosage.Mrp3 was significantly induced in model mice after pretreatment of PRP.But the adjustment effect to bile acids transporters by PRP was not significant in normal mice.These results reveal that PRP has the different effects on bile acids transporter in hepatic injury mice,so the dosage of PRP was need to pay attention when used in clinical hepatic injury.