Drug Discovery, Delivery and Patient Care (DDDPC) Theme, School of Life Sciences, Pharmacy and Chemistry, Kingston University London, Kingston Upon Thames, London, United Kingdom.
Friedrich-Alexander University Erlangen-Nürnberg (FAU), Erlangen, Germany; School of Pharmacy and Biomedical Sciences, University of Central Lancashire, Preston PR1 2HE, United Kingdom.
Int J Pharm. 2020 Jun 30;584:119392. doi: 10.1016/j.ijpharm.2020.119392. Epub 2020 May 4.
In this study, enteric coatings based exclusively on naturally occurring ingredients were reported. Alginate (Alg) and pectin (Pec) blends with or without naturally occurring glyceride, glycerol monostearate (GMS), were initially used to produce solvent-casted films. Incorporating GMS in the natural polymeric films significantly enhanced the acid-resistance properties in gastric medium. Theophylline tablets coated with Alg-Pec blends without GMS disintegrated shortly after incubation in gastric medium (pH 1.2), leading to a premature and complete release of theophylline. Interestingly, tablets coated with Alg-Pec blends that contain the natural glyceride (GMS) resisted the gastric environment for 2 h with minimal drug release (<5%) and disintegrated rapidly following introduction to the intestinal medium, allowing a fast and complete drug release. Furthermore, the coating system proved to be stable for six months under accelerated conditions. These findings are particularly appealing to nutraceutical industry as they provide the foundation to produce naturally-occurring GRAS based enteric coatings.
在这项研究中，报告了完全基于天然成分的肠溶包衣。藻酸盐（Alg）和果胶（Pec）与或不与天然甘油酯、单硬脂酸甘油酯（GMS）混合，最初用于制备溶剂浇铸薄膜。在天然聚合物薄膜中加入 GMS 显著提高了在胃酸介质中的耐酸性。用不含 GMS 的 Alg-Pec 混合物包衣的茶碱片在胃介质（pH 1.2）中孵育后很快崩解，导致茶碱过早且完全释放。有趣的是，用含有天然甘油酯（GMS）的 Alg-Pec 混合物包衣的片剂在胃环境中抵抗 2 小时，药物释放量最小（<5%），并在引入肠道介质后迅速崩解，使药物快速完全释放。此外，该涂层系统在加速条件下经过六个月的时间仍保持稳定。这些发现对营养保健品行业特别有吸引力，因为它们为生产天然、GRAS 肠溶性包衣提供了基础。
