崔丽莉,邓英杰,张勇,莫文纹
CUI Li-li,DENG Ying-jie,ZHANG Yong,MO Wen-wen (School of Pharmacy

• 1:沈阳药科大学药学院

摘要(Abstract)：

目的对胸腺五肽油包水(W/O)型口服微乳进行处方设计及评价。方法 Km值(Km=m乳化剂∶m助乳化剂)滴定法制备伪三元相图,考察油相、乳化剂、助乳化剂、Km值、温度和药物对W/O微乳区域面积和载水量的影响,求出W/O型微乳的最佳处方组合。结果物理化学性质稳定且W/O区域面积和载水量均较高的W/O型微乳的最佳处方组合为蒸馏水/豆磷脂/无水乙醇/辛癸酸三甘油酯(Km=1∶1),制备温度为室温(20±1)℃。根据最佳处方组合,将水溶性药物胸腺五肽溶于水相中,制备了含药微乳的伪三元相图。结论蒸馏水/豆磷脂/无水乙醇/辛癸酸三甘油酯(Km=1∶1)组合具有较大W/O区域面积和载水量,可成功地将水溶性肽类药物包载于水相,并可将其应用于口服药物传递载体。
Objective To formulate the water-in-oil microemulsions for oral delivery of thymopentin.Methods Effect of oil,emulsifier,coemulsifier,Km value,temperature and drug on the mass ratio of water loaded in water-in-oil microemulsions and the area sizes of water-in-oil microemulsions,was studied by constructing pseudo-ternary phase diagram using traditional Km titration,in order to get the best combination of various ingredients.Results Water/soybean lecithin/absolute ethanol/caprylic/capric triglyceride(Km equals one to one)was distillated at room temperature and a stable water-in-oil microemulsion formulation with a higher water content and area sizes of water-in-oil microemulsions was obtained.In addition,thymopentin was incorporated into the aqueous phase and then pseudo-ternary phase diagram of TP5-loaded water-in-oil(W/O)microemulsion with was constructed.Conclusions Microemulsions based on combinations of distilled water/soybean lecithin/absolute ethanol/caprylic/capric triglyceride(Km equals one to one)at room temperature have a higher water content and area sizes of water-in-oil microemulsions and is a potential carrier for oral delivery of peptides.

关键词(KeyWords)： 肽类药物;油包水型微乳;Km值滴定法;伪三元相图
peptide drug;water-in-oil microemulsion;Km titration;pseudo-ternary phase diagram

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金资助项目(30672555)

作者(Author): 崔丽莉,邓英杰,张勇,莫文纹
CUI Li-li,DENG Ying-jie,ZHANG Yong,MO Wen-wen (School of Pharmacy

DOI: 10.14066/j.cnki.cn21-1349/r.2010.08.016

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