title: Application of ethyl cellulose, microcrystalline cellulose and octadecanol for wax based floating solid dispersion pellets.
abstract: 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 12h 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.
authors.affiliation: Department of Pharmaceutics, China Pharmaceutical University, Nanjing, PR China. Electronic address: ytzjzyc@163.com.
authors.forename: Hong-Xiang
authors.initials: HX
authors.lastname: Yan
authors.affiliation: Department of Pharmaceutics, China Pharmaceutical University, Nanjing, PR China.
authors.forename: Shuang-Shuang
authors.initials: SS
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutics, China Pharmaceutical University, Nanjing, PR China.
authors.forename: Jian-Hua
authors.initials: JH
authors.lastname: He
authors.affiliation: Department of Pharmaceutics, China Pharmaceutical University, Nanjing, PR China. Electronic address: liujianpingljp@hotmail.com.
authors.forename: Jian-Ping
authors.initials: JP
authors.lastname: Liu
mesh_terms: D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations / Q000737:chemistry; D013229:Stearic Acids / Q000737:chemistry*
chemical_list: D003692:Delayed-Action Preparations; D013229:Stearic Acids; C013517:ethyl cellulose; D002482:Cellulose; C109691:microcrystalline cellulose
keywords: Ethanol (PubChem CID: 702); Ethyl cellulose (PubChem CID: 24832091); Floating drug delivery system; Glyceryl monostearate (PubChem CID: 24699); Hexadecanol (PubChem CID: 2682); Hydrochloric acid (PubChem CID: 313); Microcrystalline cellulose (PubChem CID: 14055602); Octadecanol (PubChem CID: 8821); Physicochemical characterization; Polyvinyl pyrrolidone (PubChem CID: 6917); Protocatechuic acid; Protocatechuic acid (PubChem CID: 72); Release mechanism; Solid dispersion pellets; Stearic acid (PubChem CID: 5281); Sustained release