A novel gastro-floating multiparticulate system for dipyridamole (DIP) based on a porous and low-density matrix core: In vitro and in vivo evaluation

作者：Li, Zhao; Xu, Heming; Li, Shujuan; Li, Qijun; Zhang, Wenji; Ye, Tiantian; Yang, Xinggang; Pan, Weisan^*

来源：International Journal of Pharmaceutics, 2014, 461(1-2): 540-548.

DOI：10.1016/j.ijpharm.2013.12.024

• Dipyridamole
• Gastro-floating
• Sustained release pellets
• Porous matrix cores
• Bioavailability

The study was aimed to develop a novel gastro-floating multiparticulate system based on a porous and low-density matrix core with excellent floatability.
The gastro-floating pellets (GFP) were composed of a porous matrix core, a drug loaded layer (DIP and HPMC), a sub-coating layer (HPMC) and a retarding layer (Eudragit NE 30D). The porous matrix cores were evaluated in specific. EC was chosen as the matrix membrane for its rigidity and minimal expansion to large extent. The porous matrix core was achieved by the complete release of the bulk water soluble excipient from the EC coated beads, and mannitol was selected as the optimal water soluble excipient. SEM photomicrographs confirmed the structure of porous matrix cores. The compositions of GFP were investigated and optimized by orthogonal array design. The optimized formulation could sustain the drug release for 12h and float on the dissolution medium for at least 12h without lag time to float. The pharmacokinetic study was conducted in beagle dogs, and the relative bioavailability of the test preparation was 193.11 +/- 3.43%.
In conclusion, the novel gastro-floating pellets can be developed as a promising approach for the gastroretentive drug delivery systems.

• 出版日期2014-1-30
• 单位沈阳药科大学