结肠菌群触发型5-氟尿嘧啶包衣微丸的体外释放及大鼠体内吸收与分布.docVIP

芇螄肆膇蚅螃袅莂薁螂羈芅蒇螁肀蒀莃螀膂芃蚂蝿袂肆薈袈羄芁蒄袈肇肄莀袇螆芀芆袆罿肃蚄袅肁莈薀袄膃膁蒆袃袃莆莂袂羅腿蚁羂肇莅薇羁膀膇蒃羀衿莃荿薆肂膆莅薆膄蒁蚄薅袄芄薀薄羆葿蒆薃肈节莁蚂膁肅蚀蚁袀芁薆蚀羃肃薂蚀膅艿蒈虿袄膂莄蚈羇莇蚃蚇聿膀蕿蚆膁莅蒅螅袁膈莁螄羃莄芇螄肆膇蚅螃袅莂薁螂羈芅蒇螁肀蒀莃螀膂芃蚂蝿袂肆薈袈羄芁蒄袈肇肄莀袇螆芀芆袆罿肃蚄袅肁莈薀袄膃膁蒆袃袃莆莂袂羅腿蚁羂肇莅薇羁膀膇蒃羀衿莃荿薆肂膆莅薆膄蒁蚄薅袄芄薀薄羆葿蒆薃肈节莁蚂膁肅蚀蚁袀芁薆蚀羃肃薂蚀膅艿蒈虿袄膂莄蚈羇莇蚃蚇聿膀蕿蚆膁莅蒅螅袁膈莁螄羃莄芇螄肆膇蚅螃袅莂薁螂羈芅蒇螁肀蒀莃螀膂芃蚂蝿袂肆薈袈羄芁蒄袈肇肄莀袇螆芀芆袆罿肃蚄袅肁莈薀袄膃膁蒆袃袃莆莂袂羅腿蚁羂肇莅薇羁膀膇蒃羀衿莃荿薆肂膆莅薆膄蒁蚄薅袄芄薀薄羆葿蒆薃肈节莁蚂膁肅蚀蚁袀芁薆蚀羃肃薂蚀膅艿蒈虿袄膂莄蚈羇莇蚃蚇聿膀蕿蚆膁莅蒅螅袁膈莁螄羃莄芇螄肆膇蚅螃袅莂薁螂羈芅蒇螁肀蒀莃螀膂芃蚂蝿袂肆薈袈羄芁蒄袈肇肄莀袇螆 结肠菌群触发型5-氟尿嘧啶包衣微丸的体外释放及大鼠体内吸收与分布的研究 何 伟，杜 青﹡，范丽芳 （河北医科大学药学院药剂学教研室 河北 石家庄 050017） 摘要：目的 探讨5-氟尿嘧啶包衣微丸在大鼠体内的吸收与分布。方法 以果胶-乙基纤维素水分散体混合物为包衣材料，制备5-氟尿嘧啶包衣微丸。在轻度乙醚麻醉下通过聚乙烯管给大鼠口服5-氟尿嘧啶包衣微丸，对照组口服5-氟尿嘧啶未包衣微丸。HPLC法考察血液、胃、小肠、盲肠、结肠和结肠内容物中5-氟尿嘧啶的分布情况。结果 5-氟尿嘧啶包衣微丸口服给药后血液、胃、小肠和盲肠中5-氟尿嘧啶的浓度明显低于对照组，口服给药12h后，结肠和结肠内容物中药物浓度分别为：480.5±70.2, 250.5±40.2μg·g-1；口服给药24h后，结肠和结肠内容物中药物浓度分别为330.5±100.2，180.5±150.2μg·g-1，5-氟尿嘧啶主要分布于结肠和结肠内容物中，而在上消化道中检测不到药物释放。结论 果胶-乙基纤维素水分散体包衣微丸，可以明显减少5-氟尿嘧啶在上消化道的吸收，将药物特异地转运到结肠部位，提高结肠局部药物浓度，具有良好的结肠靶向性，是一种具有良好应用前景的治疗结肠癌的药物。 关键词：5-氟尿嘧啶；结肠靶向；吸收；分布；果胶 中图分类号：R944.9 文献标示码： A 文章编号： The absorption and distribution of pellets of 5-fluorouracil degraded degraded by colon bacteria-released enzymes in rats and its in vitro release He Wei ， Du Qing﹡， Li-Fang Fan (School of Pharmaceutical Science, Hebei Medical University, Hebei, ShiJiaZhuang 050017) 【Abstract 】OBJECTTIVE: To study the absorption and distribution of pectin-surelease coated pellets in rats METHODS: Prepare coated pellets for 5-FU using pectin combined with an ethylcellulose as a film coat. Coated pellets of 5-FU were administered orally in rats via a polyethylene cannula under light ether anesthesia. The rats in control group were given uncoated pellets. Distribution of 5-FU in plasma and luminal contents of GI tract was measured by HPLC.RESULTS: Concentration of 5-FU in plasma, stomach, small intestine and cecum were significantly lower than control group after oral administration. Concentration of 5-FU in colon and its contents were：480.5±70.2, 250.5±40.2;330.5±100.2 μg·g-1，180.5±150.2