Nanomedicine Research Lab, Department of Pharmaceutics, ISF College of Pharmacy, Moga, India.
Crit Rev Ther Drug Carrier Syst. 2013;30(3):217-56. doi: 10.1615/critrevtherdrugcarriersyst.2013005964.
Poor aqueous solubility impedes a drug's bioavailability and challenges its pharmaceutical development. Pharmaceutical development of drugs with poor water solubility requires the establishment of a suitable formulation layout among various techniques. Various approaches have been investigated extensively to improve the aqueous solubility and poor dissolution rate of BCS class II and IV drugs. In this literature review, novel formulation options, particularly for class II drugs designed for applications such as micronization, self-emulsification, cyclodextrin complexation, co-crystallisation, super critical fluid technology, solubilisation by change in pH, salt formation, co-solvents, melt granulation, and solid dispersion, liposomal/niosomal formulations, are discussed in detail to introduce biopharmaceutical challenges and recent approaches to facilitate more efficient drug formulation and development.
水溶性差会阻碍药物的生物利用度，并对其药物开发带来挑战。对于水溶性差的药物，药物开发需要在各种技术之间建立合适的制剂方案。为了提高 BCS 类 II 型和 IV 型药物的水溶性和差的溶解速率，已经广泛研究了各种方法。在这篇文献综述中，详细讨论了新的制剂选择，特别是对于设计用于微粉化、自乳化、环糊精络合、共结晶、超临界流体技术、通过 pH 值变化增溶、盐形成、共溶剂、熔融造粒和固体分散体等应用的 II 型药物的制剂选择，以介绍生物制药方面的挑战和最近的方法，以促进更有效的药物制剂和开发。
