新型替加氟前体脂质体大鼠灌胃给药后的体内分布

• 作 者: 高晓黎 木拉提·克扎衣别克 温浩
• 机 构: 新疆医科大学药剂学教研室,新疆中药民族药研究所,新疆医科大学药剂学教研室 新疆乌鲁木齐830054,新疆乌鲁木齐830002,新疆乌鲁木齐830054
• 出 处: 药学学报
• 发表日期: 2005年12期
• 关键词: 脂质体 前体脂质体 前体 片剂 替加氟 HPLC 体内分布 大鼠 药物浓度 血浆

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.

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 groups were significantly declined (P <0.005) .Conclusion The novel proliposomal preparation of tegafur is able to promote drug absorption in gastro-intestine, increase drug dis tribution 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.