阿奇霉素囊泡的制备及处方考察

Preparation of azithromycin niosomes and optimization of the formulation

目的制备阿奇霉素(AZI)囊泡并对处方进行筛选,得到较高包封率的囊泡制剂。方法采用薄膜蒸发-冻融法制备AZI泡囊,反透析法测定包封率,以包封率和载药量为评价指标,单因素考察冻融次数、胆固醇与吐温质量比、十八胺百分含量以及投药量因素对囊泡的影响。结果实验结果表明冻融3次、胆固醇与吐温质量比为1:3、十八胺百分含量为3%和投药量10.0mg时为最佳处方,制得的囊泡包封率由最初的(64.00±1.91)%提高为(92.87±0.77)%,粒径为(5.87±1.18)μm,zeta电位为+(12.5±0.02)mV,室温下稳定。结论最佳处方制得的AZI囊泡的包封率高,重现性好。

Objective To optimize the formulation of prepared azithromycin niosomes and to get high encapsulation efficiency. Methods Azithromycin noisome were prepapared by film-evaporation combining with freeze-thawing method and the encapsulation efficiency was determinated by anti-dialysis method. The single factors such as the times of freeze-thawing, the ratio of cholesterol to tween-80, the percentage of octadecylamine and the dosage of azithromycin were studied. Results The best prescription is as follows： the times of freeze-thawing was 3, the ratio of cholesterol to tween was 1：3, the percentage of octadecylamine was 3% and the dosage of azithromycin was 10.0mg. The final encapsulation efficiency of the niosomes increased from 64.00%±1.91% to 92.87%±0.77%, particle size were （5.87±1.18）μm and zeta potential was ＋（12.5±0.02）mV. Conclusion The formulation was optimized and the azithromycin niosomes is of high encapsulation efficiency and good reproducibility.