School of Pharmacy and Biomedical Sciences, University of Central Lancashire, Preston PR1 2HE, UK.
Drug Discovery, Delivery and Patient Care (DDDPC) Theme, School of Life Sciences, Pharmacy and Chemistry, Kingston University London, Kingston Upon Thames, London, UK.
Int J Pharm. 2020 Dec 15;591:119935. doi: 10.1016/j.ijpharm.2020.119935. Epub 2020 Oct 1.
In this work, a novel enteric coating based on natural waxes and alginate was reported. Initially, theophylline tablets were coated with emulsified ceresin wax in heated aqueous alginate solution using a fluidised bed coating technology. A coating level of 10% proved sufficient to prevent tablets from uptaking gastric medium (<5%) and produced a delayed release profile that complies to the pharmacopeial criteria of enteric coating release. Then, a wide range of emulsions based on other natural waxes (white beeswax, yellow beeswax, cetyl palmitate, carnauba wax or rice bran wax) yielded coatings with similar disintegration times and release profiles. Interestingly, the ceresin-based coating showed a superior performance at inhibiting acid uptake and enabling highly pH-responsive drug release in comparison to different commercially available GRAS enteric coating products (Eudraguard® Control, Swanlac® ASL10, and Aquateric™ N100). The coating was stable for 6 months at 30 °C and 65% RH. This innovative approach of applying hot O/W emulsion of natural waxes yielded an aesthetically attractive and stable coating with gastric protection and pH-sensitive release properties. The novel coating can be an efficient and promising alternative to overcome the shortcomings of current GRAS grade enteric coating products.
本工作报道了一种基于天然蜡和海藻酸钠的新型肠溶包衣。最初，茶碱片在流化床包衣技术中用加热的海藻酸钠溶液中的乳化蜂蜡进行包衣。10%的包衣水平足以防止片剂吸收胃介质（<5%），并产生符合肠溶性释放药典标准的延迟释放曲线。然后，一系列基于其他天然蜡（白蜂蜡、黄蜂蜡、十六烷棕榈酸酯、巴西棕榈蜡或米糠蜡）的乳液产生了具有相似崩解时间和释放曲线的涂层。有趣的是，与不同的商业可得的 GRAS 肠溶包衣产品（Eudraguard® Control、Swanlac® ASL10 和 Aquateric™ N100）相比，虫胶基包衣在抑制酸吸收和实现高度 pH 响应性药物释放方面表现出卓越的性能。该涂层在 30°C 和 65%RH 下稳定 6 个月。这种应用天然蜡的热 O/W 乳液的创新方法产生了一种具有美学吸引力和稳定的包衣，具有胃保护和 pH 敏感释放性能。新型包衣可以有效地替代当前的 GRAS 级肠溶性包衣产品，克服其缺点。
