Institute of Pharmacy and Biochemistry, Johannes Gutenberg University Mainz , Staudinger Weg 5, 55099 Mainz, Germany.
Department of Pharmaceutical Sciences, University of Michigan , Ann Arbor, Michigan 48109, United States.
Mol Pharm. 2017 Dec 4;14(12):4209-4219. doi: 10.1021/acs.molpharmaceut.6b00877. Epub 2017 Feb 28.
First introduced in the second half of the 19th century, enteric coatings are commonly used to protect acid-labile drugs, reduce the risk of gastric side effects due to irritating drugs, or for local drug delivery to the lower gastrointestinal (GI) tract. The currently available enteric-coatings are based on pH-sensitive weakly acidic polymers. Despite the long history of their use, the causes behind their performance often being unpredictable have not been properly investigated with most of the attention being focused only on the gastric emptying. However, little attention has been given to the postgastric emptying disintegration and dissolution of these dosage forms. This lack of attention has contributed to the difficulty in predicting the in vivo behavior of these dosage forms and to cases of bioavailability problems with some enteric-coated products. Therefore, increased attention needs to be given to this issue.
肠溶包衣于 19 世纪下半叶首次问世，常用于保护对酸不稳定的药物，降低因刺激性药物导致的胃部副作用风险，或用于将药物递送至下胃肠道（GI）。目前可用的肠溶包衣基于 pH 敏感的弱酸性聚合物。尽管其应用已有很长的历史，但由于其性能往往不可预测，因此并未对其进行适当的研究，大多数注意力仅集中在胃排空上。然而，对于这些剂型在胃排空后的崩解和溶解却很少受到关注。这种关注的缺乏导致了难以预测这些剂型的体内行为，以及一些肠溶产品出现生物利用度问题。因此，需要更加关注这个问题。
