软胶囊胶皮交联的预防措施和评价方法的研究进展  

Progress of Preventive Measures and Evaluation Methods of Cross-linking in Soft Gelatin Capsule Shells

作　　者：杨霏霏[1] 马晋隆[1] 倪睿[1] 史家骏[1] 黄乐乐[1] 

机构地区：[1]中国医药工业研究总院药物制剂国家工程研究中心,上海201203

出　　处：《中国医药工业杂志》2017年第3期442-448,共7页Chinese Journal of Pharmaceuticals

摘　　要：软胶囊在贮存期间出现崩解或溶出迟缓的现象已受到广泛关注,产生这种现象的主要原因为囊壳材料明胶发生交联老化。明胶发生交联的机制主要是其分子内或两个相邻明胶分子间肽链的氨基酸残基间形成共价键,从而使明胶分子相互链接,形成巨大网状结构,阻碍水分子进入。要防止明胶交联老化,首先应最大限度地减少醛类物质的引入,其次还要注意囊壳中增塑剂、水分、色素、遮光剂等辅料对胶皮交联老化的影响。评价明胶交联程度的指标一般为平衡溶胀量(Seq)、ε-氨基酸残基含量、热稳定性和崩解时间等。一些新型检测方法,如圆二色谱(CD)、傅里叶变换红外光谱(FTIR)、扫描电镜(SEM)可从明胶胶皮的光学变化、化学官能团变化及形态变化等方面辅助评价其交联程度的大小。Delayed disintegration and dissolution of soft gelatin capsules during storage have been widely concerned. The main reason for this phenomenon is the cross-linking and aging of gelatin. The main mechanism of cross-linking is that the amino groups of gelatin molecules form covalent bonds intra- or intermolecularly. Thus gelatin molecular chains link up and form a huge network structure, which keeps water molecules out of capsule shell. To prevent the cross-linking of gelatin, the foremost strategy is to avoid the introduction of aldehydes as much as possible; secondly to notice the influence of additives, such as plasticizer, water, pigment, opacifying agent. The general indexes for evaluating the degree of cross-linking of gelatin are equilibrium swelling quantity （Soq）, e-amino groups present in the gelatin chains, thermal stability and disintegration time, etc. Some noval evaluation methods, such as circular dichroism spectroscopy （CD）, Fourier transform infrared spectrometry （FTIR） and scanning electron microscopy （SEM） can be used as auxiliaries to evaluate the degree of cross-linking by observing the changes of optics, functional groups and ultrastructures of gelatin films.

关 键 词：软胶囊 明胶 交联 抗老化 评价方法 综述 

分 类 号：R944.9[医药卫生—药剂学]