双螺杆挤出技术制备双氯芬酸钠肠溶制剂的研究  

Preparation of diclofenac sodium enteric by twin-screw extrusion technology

作　　者：王艳 袁梦 夏毓龙 曹杰 柯学 WANG Yan;YUAN Meng;XIA Yu-long;CAO Jie;KE Xue(School of Pharmacy,China Pharmaceutical University,Jiangsu Public Technical Service Center for Nanometer Drug Preparation and Biological Evaluation,Nanjing 210009)

机构地区：[1]中国药科大学药学院药剂系江苏省纳米药物制备与生物学评价公共服务中心,南京210009

出　　处：《中南药学》2021年第9期1816-1822,共7页Central South Pharmacy

摘　　要：目的制备一种不含肠溶包衣的双氯芬酸钠肠溶片。方法以双氯芬酸钠(DS)为模型药物,以Eudragit L100-55为肠溶性材料,通过双螺杆挤出技术,制备双氯芬酸钠肠溶颗粒,随之压制成片;并以市售双氯芬酸钠肠溶片为参比制剂,考察自研制剂的溶出行为及体内药动学行为。结果溶出结果显示自研制剂在胃内不溶,肠内以溶蚀型方式释放。家兔药动学实验结果显示,自研制剂的平均滞留时间和达峰时间长于参比制剂,血药浓度峰值略低于参比制剂,结合溶出结果可知,自制制剂在体内具有一定的缓释效果。结论采用双螺杆挤出技术制备肠溶制剂,工艺简单、操作易行、可实现颗粒连续式生产,为肠溶制剂的制备提供了新思路。Objective To prepare diclofenac sodium enteric tablets without enteric coating.Methods Diclofenac sodium was used as a model drug and Eudragit L100-55 as enteric material to prepare a diclofenac sodium enteric-coated tablets by twin-screw extrusion technology.Commercial diclofenac sodium enteric-coated tablets were used as the reference preparation to determine the dissolution behaviors and pharmacokinetic behaviors of the self-made tablets.Results The selfmade tablets were insoluble in the stomach and the intestinal dissolution type was gradually released.The pharmacokinetic results of rabbits showed that the average retention time and the peak time of the self-made tablets were longer than that of the reference preparation,while the peak blood concentration was lower than that of the reference preparation.The self-made tablets had a certain sustained-release effect in vivo.Conclusion The preparation of enteric-coated preparation by twinscrew extrusion technology is simple and easy with continuous grain production,providing a new research idea for enteric-coated preparations.

关 键 词：双螺杆挤出技术 双氯芬酸钠 肠溶制剂 溶出度 药动学 

分 类 号：R94[医药卫生—药剂学]