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目的:初步研究W/O/W型自乳化复乳给药系统形成机制及筛选最优处方和配比。方法:通过简单的油相和小分子乳化剂在适当条件下形成W/O/W型自乳化复乳给药系统,计算简单油相和小分子乳化剂的物理化学参数。通过处方优化,考察各组分含量、空间立体效应、偶极距、电荷效应等对自乳化复乳乳化面积和粒径的影响,筛选出最优处方和配比。结果:最优处方为肉豆蔻酸异丙酯(IPM)为油相,山梨糖醇酐单油酸酯(Span-80)为亲脂乳化剂,聚山梨酯80(Tween-80)为亲水乳化剂;油相和小分子乳化剂的空间立体效应是影响自乳化复乳自乳化面积的主要因素,由于IPM的短直链结构更容易与非支链结构Span-80在初乳界面形成空间规则排列的界面膜,降低界面张力,增加膜强度,形成稳定的初乳,再加入支链结构的Tween-80在复乳界面形成致密排列的界面膜,防止内外水相合并,增加复乳的稳定性,从而增加自乳化面积;乳化剂含量对复乳粒径的影响较大,随着亲脂乳化剂在油相中的含量增加,粒径减小,而偶极距对复乳粒径影响较小。结论:最终获得自乳化复乳最优处方的的最佳配比为油相IPM:Span-80为7∶3(w/w);W/O初乳:Tween-80为7.25∶2.75(w/w)时,粒径最小(12.28±0.24)μm,乳化面积百分比最大17.14%。
OBJECTIVE: To study the formation mechanism of W / O / W self-emulsifying multiple emulsion delivery system and screen the optimal formulation and ratio. Methods: W / O / W self-emulsifying multiple emulsion delivery system was formed by simple oil phase and small molecule emulsifier under proper conditions, and the physicochemical parameters of simple oil phase and small molecule emulsifier were calculated. Through prescription optimization, the influence of the content of each component, spatial stereoscopic effect, dipole distance, charge effect on the emulsification area and particle size of self-emulsifying double emulsion was investigated, and the optimal formulation and ratio were screened out. Results: The best prescriptions were isopropyl myristate (IPM) as oil phase, sorbitan monooleate (Span-80) as lipophilic emulsifier and Tween-80 as hydrophilic Emulsifier; oil phase and small molecule emulsifier spatial three-dimensional effect of self-emulsifying double emulsion self-emulsifying area of the main factors, due to the IPM short straight chain structure and non-branched structure Span-80 in the colostrum interface to form space Regularly arranged interface membrane, reduce the interfacial tension, increase the membrane strength, the formation of a stable colostrum, and then add Tween-80 branched chain structure in the double emulsion interface to form a dense interface film to prevent the merger of internal and external water phase, Stability, thereby increasing the self-emulsifying area; emulsifier content on the secondary particle size greater impact, with the lipophilic emulsifier content in the oil phase increases, the particle size decreases, while the dipole distance of the secondary particle diameter Less affected. CONCLUSION: The optimal ratio of final formulation of self-emulsified double emulsion is 7: 3 (w / w) for oil phase IPM: Span-80 and 7.25: 2.75 for w / o colostrum: Tween- / w), the smallest particle size (12.28 ± 0.24) μm, the largest percentage of emulsion area 17.14%.