应用生物可降解材料玉米醇溶蛋白制备胃肠道生物黏附控释片

背景：胃肠道生物黏附控释制剂能延长药物制剂在胃肠道的停留时间,提高药物的生物利用度。 目的：制备5-氟尿嘧啶胃肠道生物黏附控释片。 方法：利用生物可降解性玉米醇溶蛋白为骨架材料和黏附材料,氟尿嘧啶为模型药,制备氟尿嘧啶胃肠道黏附控释片。对片芯工艺进行正交设计,优化包衣液的选择,观察生物黏附缓释片的体外黏附力及体内外相关性。 结果与结论：5-氟尿嘧啶玉米醇溶蛋白生物黏附片体外释放10 h内均符合零级释放特征,片剂具有较好的体外黏附力,且在2~8 h 内体内血药浓度较为平稳,没有明显峰谷现象,体内外释放吸收具有良好的相关性。

Preparation of gastrointestinal bioadhesive controlled release tablets using biodegradable Zein

BACKGROUND:Gastrointestinal bioadhesive controlled release tablets can extend the residence time of pharmaceutical preparations in gastrointestinal tract, and increase drug bioavailability. OBJECTIVE:To prepare 5-fluorouracil gastrointestinal bioadhesive controlled release tablets. METHODS:Taking biodegradable Zein as stent material and adhesive material, fluorouracil as model drug, the gastrointestinal controlled release tablets were prepared. The chip technology was orthogonally designed to optimize the choice of coating solution, the in vitro bioadhesion of controlled release tablets and the correlation of in vivo and in vitro were also been studied. RESULTS AND CONCLUSION:The fluorouracil Zein bioadhesive tablets were in line with zero-grade release characteristic in vitro within 10 hours. The prepared gastrointestinal bioadhesive controlled release tablets have good adhesive properties. Moreover, the blood drug concentration in vivo within 2-8 hours was relatively stable, without obvious peak valley, and there was a good correlation of the release and absorption in vivo and in vitro.