制药技术为保护物质免受酸性环境的影响提供了多种选择,例如包封在肠溶胶囊或具有肠溶衣的剂型中。然而,商业肠溶胶囊并不总是满足药典延迟释放的限制,和涂层过程通常是具有挑战性的。制备适合临床使用的小肠批是,因此,一个未解决的问题。该实验提供了基于羟丙甲纤维素(HPMC)和结冷胶的DRcapsTM胶囊的简单包衣方法,以实现小肠给药。此外,将DRcapsTM胶囊与硬明胶胶囊进行比较,以评估包衣方法的适用性。两种胶囊均浸入Eudragit®S100,Acryl-EZE®的分散体中,和浓度为10.0、15.0和20.0%的Cellacefate,并干燥。通过电子显微镜评估包衣胶囊,解体,和溶出试验,用两步pH变化(从1.2到6.8,然后到7.5)模拟通过消化道。涂有Eudragit®S和Cellacefate的DRcapsTM胶囊实现了耐酸性。虽然涂有Eudragit®S的样品在pH6.8(小肠)下在360分钟内释放其内容物,无论聚合物浓度如何,含有15.0%和20.0%Cellsefate包衣的胶囊在pH7.5(结肠)在435和495分钟内释放内容物,分别。
Pharmaceutical technology offers several options for protecting substances from acidic environments, such as encapsulation in enteric capsules or dosage form with enteric coating. However, commercial enteric capsules do not always meet limits for pharmacopeial delayed release, and the coating process is generally challenging. Preparing small enteric batches suitable for clinical use is, therefore, an unsolved problem. This experiment offers a simple coating process of DRcapsTM capsules based on hypromellose (HPMC) and gellan gum to achieve small intestine administration. In addition, DRcapsTM capsules were compared to hard gelatin capsules to evaluate the suitability of the coating method. Both capsules were immersed in dispersions of Eudragit® S 100, Acryl-EZE®, and Cellacefate at concentrations of 10.0, 15.0, and 20.0% and dried. Coated capsules were evaluated by electron microscopy, disintegration, and dissolution test with a two-step pH change (from 1.2 to 6.8, then to 7.5) to simulate passage through the digestive tract. DRcapsTM capsules coated with Eudragit® S and Cellacefate achieved acid resistance. While samples coated with Eudragit® S released their contents within 360 min at pH 6.8 (small intestine), regardless of polymer concentration, capsules with 15.0 and 20.0% coatings of Cellacefate released content at pH 7.5 (colon) within 435 and 495 min, respectively.