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).

CONCLUSIONThe 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.

Animals ; Antimetabolites, Antineoplastic ; administration & dosage ; pharmacokinetics ; Area Under Curve ; Drug Carriers ; Drug Stability ; Female ; Liposomes ; Male ; Random Allocation ; Rats ; Rats, Wistar ; Tegafur ; administration & dosage ; pharmacokinetics ; Tissue Distribution