高级检索

5-氨基水杨酸结肠定位黏附微丸的制备及评价

Preparation and evaluation of colon adhesive pellets of 5-amino salicylic acid

  • 摘要: 制备5-氨基水杨酸结肠定位黏附微丸。以CP 940和HPC为黏附性材料,挤出滚圆工艺制备载药丸芯。考察丸芯最大载药量、赋形剂以及挤出滚圆工艺对成型性的影响。采用体外黏附性实验考察两种黏附性材料的比例对黏附性的影响。制备好的黏附性丸芯采用流化床包衣,乙基纤维素作为缓释防水内层,Eudragit®; S100作为pH敏感外层,在不同pH释放介质中进行溶出研究,评价微丸在结肠环境的释药性能。实验表明:丸芯最大载药量为70%,使用PH301作为赋形剂,CP 940与HPC质量比为1∶1时,黏附效果最佳;EC增重为16%~20%,S100增重为28%时,在盐酸溶液中有良好的耐酸性,在pH 6.0磷酸盐缓冲液中5 h的释放量小于10%,而在pH 7.4结肠液中迅速释放药物和发挥黏附作用。实验结果表明,5-氨基水杨结肠定位黏附微丸是一种良好的结肠定位黏附给药系统。

     

    Abstract: This study was to develop 5-aminosalicylic acid pellets preparation to achieve colon adhesive. 5-amino salicylic acid loaded pellet cores using Carbomer 940 and HPC as bioadhesive agents were prepared by extrusion spheronization. The maximum drug load, different forming agents and process parameters of the pellet cores were studied with the formability as an indicator. The bioadhesion effect of different proportions of two bioadhesive agents was investigated by in vitro adhesion experiments. The pellets core was coated with Surelease® as inner layer for waterproof and Eudragit® S100 as outer layer for pH control. The in vitro release of the 5-amino salicylic acid pellets was studied in media of different pH. The maximum drug load of the pellets was 70% and PH301 was the best forming agent. The weight ratio of Carbomer 940 to hydroxypropyl cellulose should be kept 1 ∶1 to achieve high bioadhesion. The amount of Surelease® was 16% to 20% and Eudragit® S100 was 28%. Dissolution profiles of coated pellets revealed no drug release in the artificial gastric fluid within 2 h and released less than 10% in pH 6. 0 phosphate buffer within 5 h, while the coated pellets dissolved quickly in pH 7. 4 colonic fluid with a good adhesion effect. This approach was successfully utilized in the preparation of 5-amino salicylic acid pellets with the good colonic adhesion.

     

/

返回文章
返回