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The main purpose of the present study was to investigate the intestinal absorption activities and hepatoprotective effect of herpetrione nanosuspensions (H1NS).HINS were prepared using pH-dependent dissolving-precipitating/ homogenization process and then transformed into solid products using lyophilization.The characterizations of HNS were analysized by photon correlation spectroscopy (PCS),scanning electron microscopy (SEM) and X-ray powder diffraction (XRPD).To investigate the intestinal absorption activities of HINS,the in situ intestinal perfusion experimem was performed using the recirculating perfusion technique and make a comparison with herpetrione coarse suspensions (HCS) and pure herpetrione.The protective effect of HNS against acute liver injury induced by carbon tetrachloride (CCl4) in mice was also investigated and compared to that of HCS.The mean particle size of HINS was 269±7 nm with a polydispersity index of 0.187±0.021.The particle size and Zeta potential of HNS did not show significant changes before and after water removal.The result of XRPD indicated that herpetrione was amorphous state in both coarse powder and nanosuspensions.Thein situ intestine perfusion experiments had demonstrated a significant superiority in intestinal absorption activities for HNS compared to the HCS and pure herpetrione.As evidenced by the lower of serum aminotransferase levels and the improvement of the degree of liver lesion,pretreatnent with HNS markedly enhanced the hepatoprotective effect of herpetrione against acute liver injury induced by CCl4 in mice.We could easily conclude that HNS prepared by a high pressure homogenization technique are able to significantly enhance the intestinal absorption activities and the hepatoprotective effect of herpetrione and might have the prospects of development and application.