难溶性药物凝胶制剂研究进展

Research Progress of Insoluble Drug Gel Preparation

凝胶制剂作为透皮给药系统(transdermal drug delivery system,TDDS)的一种新型制剂,经皮肤给药发挥全身或局部治疗作用,有使用方便、安全性好、释药平缓持久等优势,成为近年来药物制剂研发的重点之一。但现有的大多数化合物均为难溶性药物,在凝胶制剂方面的应用受限。近年来,许多新型药物载体包括纳米化技术、包合物、固体分散体等被广泛用于难溶药物增溶以及增强药物皮肤透过能力。文章详细综述了各种药物载体的特点及其在凝胶制剂的应用优势和缺陷,并汇总了现FDA难溶性药物凝胶产品的上市情况以及各种增溶技术在凝胶制剂的具体应用,为凝胶制剂未来的研发方向提供理论基础及实践案例。

As a new type of transdermal drug delivery system(TDDS), gel preparation exerts systemic or local therapeutic effects through skin administration. It has become a key point of researches on pharmaceutical preparation in recent years, with advantages of convenient administration, high safety and controlled release. However, most of the existing compounds are in poor solubility, limiting their applications in gel formulations. Many new medicine carriers, including nanotechnology, inclusion compounds and solid dispersions, have been widely used to increase the solubility and enhance the skin transmissibility of drugs. This paper reviews the characteristics of various drug carriers and their advantages and disadvantages in gel preparation in detail. The marketing status of insoluble drug gel products approved by FDA and the specific application of various solubilization techniques in gel preparation are summarize. This paper provide theoretical basis and practical cases for the future research and development of gel preparation.