胸腺五肽油包水型口服微乳的处方设计与评价

Formulation and characterization of water-in-oil microemulsions for oral delivery of thymopentin

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.