Mendonsa Nicole, Almutairy Bjad, Kallakunta Venkata Raman, Sarabu Sandeep, Thipsay Priyanka, Bandari Suresh, Repka Michael A
Department of Pharmaceutics and Drug Delivery, The University of Mississippi, Oxford, MS, 38677, United States.
Pii Center for Pharmaceutical Innovation & Instruction, The University of Mississippi, Oxford, MS, 38677, United States.
J Drug Deliv Sci Technol. 2020 Feb;55. doi: 10.1016/j.jddst.2019.101459. Epub 2019 Dec 11.
Since the past several decades, poor water solubility of existing and new drugs in the pipeline have remained a challenging issue for the pharmaceutical industry. Literature describes several approaches to improve the overall solubility, dissolution rate, and bioavailability of drugs with poor water solubility. Moreover, the development of amorphous solid dispersion (SD) using suitable polymers and methods have gained considerable importance in the recent past. In the present review, we attempt to discuss the important and industrially scalable thermal strategies for the development of amorphous SD. These include both solvent (spray drying and fluid bed processing) and fusion (hot melt extrusion and KinetiSol®) based techniques. The current review also provides insights into the thermodynamic properties of drugs, their polymer miscibility and solubility, and their molecular dynamics to develop stable and more efficient amorphous SD.
在过去几十年中，现有药物以及研发管线中的新药水溶性差一直是制药行业面临的一个具有挑战性的问题。文献中描述了几种提高水溶性差的药物的整体溶解度、溶出速率和生物利用度的方法。此外，使用合适的聚合物和方法开发无定形固体分散体（SD）在最近变得相当重要。在本综述中，我们试图讨论用于开发无定形SD的重要且可工业规模放大的热策略。这些策略包括基于溶剂的技术（喷雾干燥和流化床工艺）以及基于熔融的技术（热熔挤出和KinetiSol®）。本综述还深入探讨了药物的热力学性质、它们与聚合物的混溶性和溶解性，以及它们的分子动力学，以开发稳定且更高效的无定形SD。
