新型替加氟前体脂质体大鼠灌胃给药后的体内分布

Aim To evaluate in vivo distribution characteristics of a novel proliposomal preparation of tegafur in rats.Methods Concentrations 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.Results Following 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.