阿奇霉素囊泡的制备及处方考察

摘要

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)mY,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.