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4-氨基水杨酸钠结肠黏附微丸的制备及黏附性能考查

Preparation and adhesive characterization of colon adhesive pellets of sodium 4-amino salicylate

  • 摘要: 目的 : 制备4-氨基水杨酸钠(4-ASANa)结肠黏附微丸并考查其黏附性能。 方法 : 采用离心造粒法,以羟丙基甲基纤维素K4M和卡波姆934P为黏附性骨架材料,微晶纤维素为赋形剂制备含药微丸;乙基纤维素水分散体包衣,并将微丸装入结肠溶胶囊,以pH 7.4的磷酸盐缓冲液为释放介质,考查微丸的释放特性。体内评价以黏附聚合物在大鼠肠道内转运速度为指标,考察该微丸的黏附性;体外评价以微丸在离体大鼠结肠组织的滞留率为指标,并采用X线跟踪技术验证4-氨基水杨酸钠结肠黏附微丸在人体内的黏附性。 结果 : 制备的微丸圆整度较好,且粒度均匀,硬度适宜,有较强的结肠黏附性和较好的缓释特性。 结论 : 该制剂工艺简单,经济实用,结肠黏附性、靶向性较好。

     

    Abstract: Aim :To develop a new preparation consisting of colon adhesive pellets of sodium 4-amino salicylate for the treatment of ulcerative colitis,and to characterize the adhesive of the prepared pellets. Methods :Centrifugation-granulation was used to prepare sodium 4-amino salicylate pellets into which HPMC K4M and Carbomer 934P as matrix were incorporated.The pellets were coated with Surlease,and filled into enteric-coated capsules.The release of sodium 4-amino salicylate from the pellets was evaluated in the pH 7.4 buffer.The adhesive property of the pellets was characterized by evaluating the transit rate of the pellets in the rat intestine in vivo,and by determing the remaining(%) of the pellets in the isolated rat colonic segment in vitro.The adhesive of the pellets in vivo was also verified by X-rays. Results :It was shown that the resultant pellets of round shape,good uniformity in size,and favorable rigidity possessed the colon-adhesive and sustained-release properties. Conclusion :The simple,economical and practical approach was sucessfully utilized in the preparation of sodium 4-amino salicylate pellets with the remarked colonic adhesion and targeting.

     

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