CAJ | 학술논문

以一系列难溶性的二氢吡啶类钙离子通道阻滞剂作为模型药物，以自乳化面积和药物在自乳化给药系统( SEDDS)中的溶解度作为自乳化评价指标，建立各组分的分子描述参数与自乳化性质之间的定量函数关系，通过模型讨论分子结构对自乳化形成机理的影响。结果表明，自乳化的发生是各组分含量、分子间作用力、亲脂性和分子大小等多方面因素综合作用的结果。当混合表面活性剂分子较大且药物脂溶性较好时， SEDDS对难溶性药物的增溶能力较强；表面活性剂与助表面活性剂的质量比较大，混合表面活性剂的分子较大时， SEDDS的稀释稳定性较好。
이일계렬난용성적이경필정류개리자통도조체제작위모형약물，이자유화면적화약물재자유화급약계통( SEDDS)중적용해도작위자유화평개지표，건립각조분적분자묘술삼수여자유화성질지간적정량함수관계，통과모형토론분자결구대자유화형성궤리적영향。결과표명，자유화적발생시각조분함량、분자간작용력、친지성화분자대소등다방면인소종합작용적결과。당혼합표면활성제분자교대차약물지용성교호시， SEDDS대난용성약물적증용능력교강；표면활성제여조표면활성제적질량비교대，혼합표면활성제적분자교대시， SEDDS적희석은정성교호。
Several self-emulsifying drug delivery systems( SEDDS) were constructed, using a series of poorly water-soluble dihydropyridines of calcium channel blockers( DHPs-CCBs) as the model drugs, and characte- rized them with regards to self-emulsification area and solubility of the payloads. By establishing multiple linear regression( MLR) models between the molecular descriptors of building components and characteristics of the emulsions formed eventually, we then tried to reveal the formation mechanisms under self-emulsification process. It was found that emulsification process was primarily initialized by the intermolecular forces but simultaneously affected by the proportion of components, lipophilicity and molecular size. Larger molecular size of the mixed surfactants and better lipophilicity of drug contributed to higher drug solubility. Also, the stability of SEDDS after dilution correlated positively with the mass ratio of surfactants and co-surfactants and the molecular size of mixed surfactants. It is supposed that this work could generally be used as guidelines to screen the formulas of SEDDS.