复方联苯苄唑纳米乳的制备及其质量评价

Preparation and Quality Evaluation of Compound Bifonazole Nanoemulsion

以联苯苄唑为主药,辅以丙酸氯倍他索以及肉桂醛制成复方。通过绘制伪三元相图筛选处方研制复方联苯苄唑纳米乳,并对其进行质量评价。结果表明,复方联苯苄唑纳米乳最佳配方为:w(联苯苄唑)=1.6%,w(丙酸氯倍他索)=0.05%,w(肉桂醛)=0.15%,w(吐温-80)=29.5%,w(无水乙醇)=9.8%,w(乙酸乙酯)=13.6%,w(蒸馏水)=45.3%。该纳米乳为水包油型纳米乳,可用水无限稀释。透射电镜下,纳米乳呈圆球形,无粘连。平均粒径(Z-Average)为10.4 nm,多分散系数(PDI)为0.196。在25℃时,稀释5倍后的复方联苯苄唑纳米乳的平均pH=6.1±0.3,对应的平均Zeta电位为(-9.18±0.2)mV。复方联苯苄唑纳米乳制备工艺简单且质量可控,有望应用于临床。

Bifonazole, as basic remedy, was combined with clobetasol propionate and cinnamaldehyde to make a compound. By drafting the pseudoternary phase diagrams, the optimal bifonazole nanoemulsion was chosen for quality evaluation. It was found that the mass fraction of the various constituents of the optimal bifonazole nanoemulsion was as follows, w （ bifonazole ） = 1.6%, w （clobetasol propionate ） = 0. 05%, w （ cinnamaldehyde ） = 0. 15%, w （ Tween - 80 ） = 29.5%, w （ethanol）= 9. 8%, w （ acetic ether） = 13.6%, and w （ distilled water） = 45.3%. This oil-in-water nanoemulsion could be easily diluted by water, assuming a spherical shape without adhesion or aggregation, and having a Z-average diameter of 10.4 nm and a polydispersity index（PDI） of 0. 196. After a 5-fold dilution, the average pH value was 6. 1 ± 0.3, and the corresponding zeta potential was （9. 18±0.2） mV at 25 ℃. The preparation process of this compound bifonazole nanoemulsion is easy to carry out, and the quality can be controlled, standing a chance of potential clinical applications.