Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, MD 21201, United States.
Shin-Etsu Chemical Co., Ltd., c/o SE Tylose USA, Inc., Totowa, NJ 07512, United States.
Int J Pharm. 2018 May 5;542(1-2):108-116. doi: 10.1016/j.ijpharm.2018.02.025. Epub 2018 Feb 16.
The purpose of this study was to use statistical design of experiments to develop a stable aqueous enteric coating formulation containing stabilizing excipients, such as polyethylene glycol that can minimize hydroxypropyl methylcellulose acetate succinate aggregation and minimize spray-nozzle clogging at elevated processing temperatures. The mechanisms of stabilization (i.e. charge stabilization and molecular interactions) were studied by performing zeta potential and FTIR studies. Electrostatic stabilization by sodium lauryl sulfate and hydrogen bonding by polyethylene glycol provided dispersion stability and yielded a stable aqueous coating formulation that prevented spray-nozzle clogging. An enteric coated tablet with better gastric resistance was obtained by incorporating fumed silica (Aerosil® R972) as the anti-tacking agent instead of talc. Dissolution testing on the riboflavin enteric coated tablets showed a good enteric release profile without releasing riboflavin in 0.1 N HCl, and completely disintegrating within 10 min in phosphate buffer (pH 6.8).
本研究旨在使用实验统计学设计，开发一种含有稳定剂辅料（如聚乙二醇）的稳定水性肠溶包衣配方，以最小化羟丙甲纤维素醋酸琥珀酸酯的聚集，并在较高的加工温度下最小化喷雾嘴堵塞。通过进行zeta 电位和傅里叶变换红外（FTIR）研究，研究了稳定化机制（即电荷稳定和分子相互作用）。十二烷基硫酸钠的静电稳定作用和聚乙二醇的氢键作用提供了分散稳定性，并得到了一种稳定的水性包衣配方，防止了喷雾嘴堵塞。通过将气相法二氧化硅（Aerosil® R972）作为抗粘剂代替滑石粉，来制备具有更好耐胃酸性能的肠溶片剂。核黄素肠溶包衣片剂的溶出度测试表明，在 0.1N HCl 中没有释放核黄素，并且在磷酸盐缓冲液（pH 6.8）中 10 分钟内完全崩解，具有良好的肠溶释放特性。
