Noida Institute of Engineering and Technology (Pharmacy Institute), Greater Noida, India.
Drug Dev Ind Pharm. 2021 Oct;47(10):1523-1534. doi: 10.1080/03639045.2022.2042554. Epub 2022 Feb 21.
Most of the widely used drugs have problems associated with their oral bioavailability either due to their poor aqueous solubility or due to their poor permeability. Co-crystallization is an efficient and economically feasible approach that offers a great opportunity for improvement in physicochemical properties such as solubility, stability, and bioavailability of such type of therapeutic agent. Selection of the best co-former plays a major role in co-crystallization. Various approaches have been developed for the selection of suitable co-formers with API. In recent years screening, a computational tool paying more attention for screening of co-formers has been developed. Numerous approaches can be used for screening such as the Autodocking tool, COSMORS, COSMOTHERM, etc. Autodocking can predict several numbers of co-former effectively screened method to identify a suitable co-former with an API. Prediction of solubility and dissolution is also important for the development of co-crystal. In this review, we discuss screening of coformer and thermodynamic approaches to determine the dissolution and solubility of co-crystal specially with reference to the drugs belonging to BCS class II group.
大多数广泛使用的药物都存在与其口服生物利用度相关的问题,这要么是由于其较差的水溶性,要么是由于其较差的渗透性。共结晶是一种有效且经济可行的方法,为改善此类治疗剂的物理化学性质(如溶解度、稳定性和生物利用度)提供了巨大的机会。选择最佳共晶形成剂在共结晶中起着主要作用。已经开发了各种方法来选择与 API 相容的合适共晶形成剂。近年来,筛选,一种更注重筛选共晶形成剂的计算工具已经被开发出来。可以使用许多方法进行筛选,例如 Autodocking 工具、COSMORS、COSMOTHERM 等。Autodocking 可以有效地预测多个共晶形成剂的数量,筛选方法可以识别与 API 相容的合适共晶形成剂。预测溶解度和溶解也是共晶开发的重要因素。在这篇综述中,我们讨论了共晶形成剂的筛选和热力学方法来确定共晶的溶解和溶解度,特别是参考属于 BCS 类 II 组的药物。