Rump Adrian, Kromrey Marie-Luise, Scheuch Eberhard, Jannin Vincent, Rehenbrock Lara, Tzvetkov Mladen Vassilev, Weitschies Werner, Grimm Michael
Department of Biopharmaceutics and Pharmaceutical Technology, University of Greifswald, 17489 Greifswald, Germany.
Department of Diagnostic Radiology and Neuroradiology, University Hospital Greifswald, 17475 Greifswald, Germany.
Pharmaceutics. 2022 Sep 21;14(10):1999. doi: 10.3390/pharmaceutics14101999.
Many orally dosed APIs are bioavailable only when formulated as an enteric dosage form to protect them from the harsh environment of the stomach. However, an enteric formulation is often accompanied with a higher development effort in the first place and the potential degradation of fragile APIs during the coating process. Ready-to-use enteric hard capsules would be an easily available alternative to test and develop APIs in enteric formulations, while decreasing the time and cost of process development. In this regard, Lonza Capsugel Next Generation Enteric capsules offer a promising approach as functional capsules. The in vivo performance of these capsules was observed with two independent techniques (MRI and caffeine in saliva) in eight human volunteers. No disintegration or content release in the stomach was observed, even after highly variable individual gastric residence times (range 7.5 to 82.5 min), indicating the reliable enteric properties of these capsules. Seven capsules disintegrated in the distal part of the small intestine; one capsule showed an uncommonly fast intestinal transit (15 min) and disintegrated in the colon. The results for this latter capsule by MRI and caffeine appearance differed dramatically, whereas for all other capsules disintegrating in the small intestine, the results were very comparable, which highlights the necessity for reliable and complementary measurement methods. No correlation could be found between the gastric residence time and disintegration after gastric emptying, which confirms the robust enteric formulation of those capsules.
许多口服给药的活性药物成分（API）只有制成肠溶剂型才能被吸收，以保护它们免受胃部恶劣环境的影响。然而，肠溶制剂首先往往需要付出更高的研发努力，而且在包衣过程中脆弱的API可能会降解。即用型肠溶硬胶囊将是一种易于获得的替代品，用于测试和开发肠溶制剂中的API，同时减少工艺开发的时间和成本。在这方面，龙沙胶囊公司的下一代肠溶胶囊作为功能性胶囊提供了一种很有前景的方法。在八名人类志愿者中，用两种独立技术（磁共振成像和唾液中的咖啡因）观察了这些胶囊的体内性能。即使在个体胃滞留时间差异很大（范围为7.5至82.5分钟）之后，也未观察到这些胶囊在胃中崩解或内容物释放，这表明这些胶囊具有可靠的肠溶特性。七粒胶囊在小肠远端崩解；一粒胶囊显示出异常快速的肠道转运（15分钟）并在结肠中崩解。通过磁共振成像和咖啡因出现情况对后一粒胶囊的结果差异很大，而对于所有其他在小肠中崩解的胶囊，结果非常可比，这突出了可靠且互补的测量方法的必要性。胃滞留时间与胃排空后的崩解之间未发现相关性，这证实了那些胶囊强大的肠溶制剂性能。
