口腔黏膜给药制剂的质量评价研究

Characterization methods for transmucosal drug delivery

在非胃肠道给药系统中,口腔黏膜给药制剂由于具有便于服用及提高患者顺应性等优势,成为近年来研究较为广泛的给药途径。但目前各国上市的口腔黏膜制剂非常有限,很大程度上是由于缺乏统一的、符合口腔生理状况的质量评价体系。口腔黏膜制剂除考察制剂的理化特性外,还需评估与制剂有效性、安全性密切相关的黏附时间、黏附强度、黏膜渗透性、体外释放以及体内药动学特性。研究者对这些指标的评价方法各不相同,如离体组织可以是猪颊黏膜、犬口腔黏膜、鼠黏膜等;渗透性可通过Franz扩散池、Flow-through流通池、尤斯灌流室等方法进行检测,但不同的检测方法其结果各不相同,严重阻碍了口腔黏膜制剂的质量评价。本文综述了目前主要采用的评价方法,为制定一致的、合理的口腔黏膜剂质量评价提供理论基础。

Among the non-gastrointestinal routes,transmucosal drug delivery preparations have been extensive researched in recent years due to their advantages of being convenient to take and improving patient compliance.However,currently there are very limited oral mucosa preparations on the market in various countries,which is largely due to the lack of a unified quality evaluation system in line with the oral physiological conditions.In addition to the physical and chemical properties of the formulations,it is also necessary to evaluate the adhesion time,mucoadhesion strength,mucocal permeability,in vitro dissolution and pharmacokinetic properties which are closely related to their efficacy and safety.The evaluation methods of these indicators vary from researcher to researcher.For example,in vitro buccal tissues can be from pigs,dogs,mouse,etc.In vitro permeability can be detected by Franz diffusion cell,flow-through diffusion cell and Ussing chambers,but the results of different detection methods are different,which seriously hinder the quality evaluation of oral mucosa preparations.Thus this article reviews the current characterization methods and provides a theoretical basis for the development of standardized quality evaluation methods.