Application of ethyl cellulose, microcrystalline cellulose and octadecanol for wax based floating solid dispersion pellets. (5th September 2016)

• Record Type: Journal Article
• Authors: Yan, Hong-Xiang; Zhang, Shuang-Shuang; He, Jian-Hua; Liu, Jian-Ping
• Is Part Of: Carbohydrate polymers. Volume 148(2016)
• Page Start: 143
• Page End: 152
• Publication Date: 2016-09-05
• Subjects: Protocatechuic acid (PubChem CID: 72) -- Octadecanol (PubChem CID: 8821) -- Hexadecanol (PubChem CID: 2682) -- Stearic acid (PubChem CID: 5281) -- Glyceryl monostearate (PubChem CID: 24699) -- Ethyl cellulose (PubChem CID: 24832091) -- Microcrystalline cellulose (PubChem CID: 14055602) -- Polyvinyl pyrrolidone (PubChem CID: 6917) -- Ethanol (PubChem CID: 702) -- Hydrochloric acid (PubChem CID: 313); Floating drug delivery system -- Solid dispersion pellets -- Sustained release -- Release mechanism -- Physicochemical characterization -- Protocatechuic acid; Polysaccharides -- Periodicals; Polysaccharides -- Periodicals; Polysaccharides -- Périodiques; Electronic journals; 547.78
• DOI: 10.1016/j.carbpol.2016.04.050
• Languages: English
• ISSNs: 0144-8617

Abstract

Highlights: Wax based floating solid dispersion pellets were developed and optimized. Low-density matrix pellet cores were prepared with the floating assistant octadecanol and microcrystalline cellulose. The fourth generation drug/ethyl cellulose dispersion was obtained and layered by single-step technique. Ethyl cellulose of various viscosities (10cp/45cp/100cp) has different sustained release abilities. SEM, DSC, XRD and FTIR were applied for physicochemical characterization. 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 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.