IM To compare the pharmacokinetic characteristics of four kinds of fluorouracil (5FU) preparations rectally administered to animals.METHODS The concentrations of 5FU in the plasma, rectal wall and lymph tissues of m...IM To compare the pharmacokinetic characteristics of four kinds of fluorouracil (5FU) preparations rectally administered to animals.METHODS The concentrations of 5FU in the plasma, rectal wall and lymph tissues of mesentery were determined by HPLC assay, and the main pharmacokinetic parameters were calculated by the data procession software package.RESULTS The 5FU concentrations in the rectal wall and lymph tissues of rats were significantly higher than that in blood of the animals administered rectally with the four kinds of preperations (P<001). The drug level in rectal wall was higher in emulsion groups than that in suppository groups (P<005). The drug level in plasma was lower in lipophilbase suppository group than that in hydrophilbase suppository group, and than in the simple (o/w) emulsion group was lower than in the complex (w/o/w) emulsion group, and the in vivo differences were found statistically significant in rabbits (P<001).CONCLUSION The lipophilbase suppository and the simple emulsion of 5FU might be more suitable for rectal administration in the treatment of the rectal cancers.展开更多
文摘IM To compare the pharmacokinetic characteristics of four kinds of fluorouracil (5FU) preparations rectally administered to animals.METHODS The concentrations of 5FU in the plasma, rectal wall and lymph tissues of mesentery were determined by HPLC assay, and the main pharmacokinetic parameters were calculated by the data procession software package.RESULTS The 5FU concentrations in the rectal wall and lymph tissues of rats were significantly higher than that in blood of the animals administered rectally with the four kinds of preperations (P<001). The drug level in rectal wall was higher in emulsion groups than that in suppository groups (P<005). The drug level in plasma was lower in lipophilbase suppository group than that in hydrophilbase suppository group, and than in the simple (o/w) emulsion group was lower than in the complex (w/o/w) emulsion group, and the in vivo differences were found statistically significant in rabbits (P<001).CONCLUSION The lipophilbase suppository and the simple emulsion of 5FU might be more suitable for rectal administration in the treatment of the rectal cancers.
