~(99)Tc~m-5-氨基水杨酸包衣片在结肠的定位释药

Examination of Coated Tablet of ~(99)Tc~m-5-aminosalicylic Acid for Delivering Drug in Colon

  • 摘要: 采用放射性核素示踪技术研究了5-氨基水杨酸包衣片对犬结肠的靶向性。用99Tcm标记5-氨基水杨酸后,将标记物制成包衣片;通过在人工胃、肠液中测定放射性泄漏的方法观察包衣片的包衣膜性能;实验犬口服包衣片后,用SPECT显像观察包衣片在犬消化道内的运动过程。结果显示:包衣片在人工胃液中不溶解,外观无变化,无放射性漏出;将包衣片在人工胃液中滞留1h,取出放入人工肠液中3h,包衣膜被部分溶蚀,出现大量孔洞,但无放射性漏出;3.5h后有放射性漏出,表明包衣膜开始破裂释药。犬口服后,包衣片在升结肠开始释药,并在结肠内停留6~7h。表明5-氨基水杨酸包衣片能在结肠定位释药。

     

    Abstract: The radionuclide trace technique is used to examine and determine that ~(99)Tc~m-5-aminosalicylic acid coated tablet delivere drug in colon. 5-aminosalicylic acid labelled with (~(99)Tc~m) is made to be coated tablet. Which character in artificial gastrointestinal liquid is observed by testing radioactivity leakage of the coated tablet, and in dogs vivo motor process by SPECT. Coated tablet is not dissolved in artificial gastric juice and outward appearance of which does not change.Coated tablet is take out after laid in artificial gastric juice for 1 h and placed in artificial intestinal liquid, partial coating is corroded and appears a great quantity of hole in a utensil at 3 h, and coating starts to burst and release at 3.5 h. The coated tablet starts to release drug in ascending colon and remain in colon for 6~7 h after taking orally. Therefore coated tablet of ~(99)Tc~m-5-aminosalicylic acid is able to release drug by location in colon.

     

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