新型替加氟前体脂质体大鼠灌胃给药后的体内分布

前体脂质体(proliposome),又称重建脂质体,系脂质体的前体形式,用前与水水合即可分散成脂质体[1]。经十几年的努力,已有多种抗肿瘤药、抗生素、消炎镇痛药、生物制品、心血管系统用药及中药等制成前体脂质体制剂,并取得良好效果。这些前体脂质体制剂主要是通过两种途径解决问题

In vivo distribution of a novel proliposomal preparation of tegafur following intragastric gavage to rats

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.