Leuner C, Dressman J
Johann Wolfgang Goethe University, Frankfurt am Main, Germany.
Eur J Pharm Biopharm. 2000 Jul;50(1):47-60. doi: 10.1016/s0939-6411(00)00076-x.
The solubility behaviour of drugs remains one of the most challenging aspects in formulation development. With the advent of combinatorial chemistry and high throughput screening, the number of poorly water soluble compounds has dramatically increased. Although solid solutions have tremendous potential for improving drug solubility, 40 years of research have resulted in only a few marketed products using this approach. With the introduction of new manufacturing technologies such as hot melt extrusion, it should be possible to overcome problems in scale-up and for this reason solid solutions are enjoying a renaissance. This article begins with an overview of the historical background and definitions of the various systems including eutectic mixtures, solid dispersions and solid solutions. The remainder of the article is devoted to the production, the different carriers and the methods used for the characterization of solid dispersions.
药物的溶解性是制剂研发中最具挑战性的方面之一。随着组合化学和高通量筛选的出现，难溶性化合物的数量急剧增加。尽管固体溶液在改善药物溶解性方面具有巨大潜力，但40年的研究仅产生了少数采用这种方法的上市产品。随着热熔挤出等新制造技术的引入，应该有可能克服放大生产中的问题，因此固体溶液正在复兴。本文首先概述了包括低共熔混合物、固体分散体和固体溶液在内的各种体系的历史背景和定义。本文的其余部分致力于固体分散体的生产、不同载体以及用于表征固体分散体的方法。
