Application of ethyl cellulose, microcrystalline cellulose and octadecanol for wax based floating solid dispersion pellets

作者：Yan, Hong-Xiang; Zhang, Shuang-Shuang; He, Jian-Hua; Liu, Jian-Ping^*

来源：Carbohydrate Polymers, 2016, 148: 143-152.

DOI：10.1016/j.carbpol.2016.04.050

• Floating drug delivery system
• Solid dispersion pellets
• Sustained release
• Release mechanism
• Physicochemical characterization
• Protocatechuic acid

The present study aimed to develop and optimize the wax based floating sustained-release dispersion pellets for a weakly acidic hydrophilic drug protocatechuic acid to achieve prolonged gastric residence time and improved bioavailability. This low-density drug delivery system consisted of octadecanol/microcrystalline cellulose mixture matrix pellet cores prepared by extrusion-spheronization technique, coated with drug/ethyl cellulose 100cp solid dispersion using single-step fluid-bed coating method. The formulation-optimized pellets could maintain excellent floating state without lag time and sustain the drug release efficiently for 12 h based on non-Fickian transport mechanism. Observed by SEM, the optimized pellet was the dispersion-layered spherical structure containing a compact inner core. DSC, XRD and FTIR analysis revealed drug was uniformly dispersed in the amorphous molecule form and had no significant physicochemical interactions with the polymer dispersion carrier. The stability study of the resultant pellets further proved the rationality and integrity of the developed formulation.

• 出版日期2016-9-5
• 单位中国药科大学