Preparation,in Vitro Evaluation and in Vivo Pharmacokinetics of Bioadhesive Controlled-release Tablets with Zein as Main Excipient

Objective:To prepare the bioadhesive controlled-release tablets with zein as main excipient and to evaluate their in vitro adhesive ability and release profile as well as in vivo pharmacokinetics.Methods:The gastrointestinal adhesive controlled-release tablets were prepared using zein as matrix and adhesive material and 5-fluorouracil(5-FU) as model drug.Their in vitro adhesive ability and release profile as well as pharmacokinetics in rats were compared with common market tablets and homemade controlled-release tablets.Results:The 5-FU gastrointestinal adhesive controlled-release tablets had good tissue adhesion.Their in vitro release met zero-order model within 12 h,reaching the controlled-release.Compared with control tablets,their retention in the ratgastrointestinal tract was longer and their release was more stable and sustained.Conclusion:Zein has showed a good bioadhesion in gastrointestinal tract.The bioadhesive controlled-release tablets using zein as main excipient could achieve sustained-and controlled-release in gastrointestinal tract.