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

摘要:

本实验以联苯苄唑为主药，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的各组分质量分数分别为：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，无黏连。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值为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。

Abstract:

Bifonazole as basic remedy was combined with clobetasol propionate and cinnamaldehyde to make a compound. By drafting the pseudoternary phase diagrams, optimal bifonazole nanoemulsion was chosen for quality evaluation. It was found that the mass fraction of 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, exhibited a spherical shape without adhesion or aggregation, and presented 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 simple to operate, and the quality can be controlled, standing a chance of potential clinical applications.