Pharmaceutical Sciences Department, University of Salamanca, C/Licenciado Méndez Nieto s/n, 37007 Salamanca, Spain.
Pharmaceutical Sciences Department, University of Salamanca, C/Licenciado Méndez Nieto s/n, 37007 Salamanca, Spain; Institute of Biomedical Research of Salamanca (IBSAL), Spain.
Eur J Pharm Sci. 2019 Oct 1;138:105019. doi: 10.1016/j.ejps.2019.105019. Epub 2019 Jul 30.
Enteric coating is a common procedure in the development of oral pharmaceutical dosage forms. The main advantage of enteric coating is that it protects the drug from acidic pH and enzymatic degradation in the stomach while protecting it from the undesirable effects of some drugs. There is certain controversy regarding the real influence of enteric coating on the bioavailability of many drugs. Various scientific articles have demonstrated an improvement in the extent of bioavailability of some drugs when enteric coating is used. In recent years, there have been many studies examining different formulation strategies for monolithic and multiparticulate systems, including different pharmaceutical oral dosage forms and delivery systems based on the combined use of enteric coating and other methods that improve the bioavailability of drugs administered orally. However, the real bioavailability, serum levels and therapeutic effect of these drugs may be influenced by gastrointestinal pH values, gastrointestinal environment, inter-individual or intra-individual variability in gastric emptying and gastrointestinal transit time, interpatient variability associated with the type of polymer used for enteric coating or other formulation variables. It deserves special attention to know the real influence of enteric coating on the bioavailability of new oral dosage forms.
肠溶性包衣是口服药物剂型开发中的常见程序。肠溶性包衣的主要优点是它可以保护药物免受胃酸和胃中的酶降解，同时保护药物免受某些药物的不良影响。关于肠溶性包衣对许多药物生物利用度的实际影响存在一定争议。各种科学文章已经证明，在使用肠溶性包衣时，一些药物的生物利用度得到了提高。近年来，有许多研究检查了用于整体和多颗粒系统的不同配方策略，包括基于肠溶性包衣和其他提高口服给药药物生物利用度的方法的联合使用的不同药物口服剂型和给药系统。然而，这些药物的实际生物利用度、血清水平和治疗效果可能会受到胃肠道 pH 值、胃肠道环境、胃排空和胃肠道转运时间的个体间或个体内变异性、与肠溶性包衣或其他制剂变量使用的聚合物类型相关的患者间变异性的影响。值得特别关注的是，要了解肠溶性包衣对新口服剂型生物利用度的实际影响。
