Department of Pharmaceutics, School of Pharmaceutical Sciences, Sardar Bhagwan Singh University, Balawala, Dehradun, India.
School of Pharmacy, Adarsh Vijendra Institute of Pharmaceutical Sciences, Shobhit University Gangoh, Saharanpur, India.
Curr Drug Targets. 2019;20(14):1434-1446. doi: 10.2174/1389450120666190717114521.
The Biopharmaceutical classification system (BCS) classifies the drugs based on their intrinsic solubility and intestinal permeability. The drugs with good solubility and intestinal permeability have good bioavailability. The drugs with poor solubility and poor permeability have solubility dependent and permeability dependent bioavailability, respectively. In the current pharmaceutical field, most of the drugs have poor solubility. To solve the problem of poor solubility, various solubility enhancement approaches have been successfully used. The effects of these solubility enhancing approaches on the intestinal permeability of the drugs are a matter of concern, and must not be overlooked. The current review article focuses on the effect of various solubility enhancing approaches viz. cyclodextrin, surfactant, cosolvent, hydrotropes, and amorphous solid dispersion, on the intestinal permeability of drugs. This article will help in the designing of the optimized formulations having balanced solubility enhancement without affecting the permeability of drugs.
生物药剂分类系统 (BCS) 根据药物的内在溶解度和肠道通透性对药物进行分类。溶解度和肠道通透性好的药物具有良好的生物利用度。溶解度和通透性差的药物分别具有溶解度依赖性和通透性依赖性生物利用度。在当前的制药领域，大多数药物的溶解度都较差。为了解决溶解度差的问题，已经成功地使用了各种提高溶解度的方法。这些提高溶解度的方法对药物肠道通透性的影响是值得关注的，不容忽视。本文综述了各种提高溶解度的方法（如环糊精、表面活性剂、共溶剂、增溶剂和无定形固体分散体）对药物肠道通透性的影响。本文将有助于设计具有平衡溶解度增强作用而不影响药物通透性的优化配方。
