Abstract: AimTo evaluate in vivo distribution characteristics of a novel proliposomal preparation of tegafur in rats. MethodsConcentrations of tegafur in tissues and plasma were measured by HPLC following intragastric gavage of the proliposomal preparation of tegafur (PL-FT207) or aqueous suspension of tegafur tablet (T-FT207) to rats. And the pharmacokinetic parameters including the area under the concentration-time curve (AUC), relative tissue efficiency and the maximum drug concentration were calculated. ResultsFollowing intragastric gavage of PL-FT207 or T-FT207 to rats, AUC was significantly increased in plasma, liver, kidney, colon and lung (P<0.01) of PL-FT207 group in contrast to that of T-FT207 group, the relative tissue efficiencies of these tissues were 1.36-1.57, the maximum drug concentrations of brain and lung of PL-FT207 group were significantly declined (P<0.005). Conclusion The novel proliposomal preparation of tegafur is able to promote drug absorption in gastro-intestine, increase drug distribution in kidney, liver, colon and lung, and decrease the maximum drug concentration in brain and heart, thus providing scientific basis for further studies on this preparation.