阿奇霉素囊泡体外释放行为的初步研究  

Preliminary study on the release of azithromycin niosomes in vitro

作　　者：钟萌[1] 谭群友[2] 冯悦[1] 廖红[1] 张景勍[1] 

机构地区：[1]重庆医科大学高校药物工程研究中心和生物化学与分子药理重点实验室,重庆400016 [2]第三军医大学大坪医院野战外科研究所胸外科,重庆400042

出　　处：《中国抗生素杂志》2012年第6期476-480,共5页Chinese Journal of Antibiotics

摘　　要：目的研究阿奇霉素囊泡(AM-NS)在不同释放介质中的体外释药规律。方法采用动态透析技术研究阿奇霉素囊泡在不同释放介质中的体外释药特性,并对其释放模型进行拟合,计算不同释药曲线间的相似因子。结果 AM-NS在pH7.4的PBS溶液、pH6.8的PBS溶液、0.1mol/L盐酸溶液(前2h)和pH 6.8的PBS溶液(2h后)中的释药符合Weibull模型,但在0.1mol/L盐酸溶液中释药符合Retrer-Peppas模型。AM-NS之间在各种释放介质中的释放曲线间的相似因子都大于50,但是其与AM在各种释放介质中的释放曲线间的相似因子也均小于50。结论 AM-NS在不同释放介质中的释放行为相似,没有显著性差别。与AM相比,AM-NS在各种释放介质中的释放行为存在显著性差别,说明AM-NS改变了AM的释放行为,具有良好的缓释效果。Objective To study the in vitro release of azithromycin （AM） from AM niosomes （AM-NS） in different media. Methods The dynamic dialysis method was used to evaluate the in vitro release of AM from AMNS. The release data were fitted by different kinetic models. The similarity factors （f2 values） between every two release curves were calculated and compared. Results The Weibull models could fit the release curves of AM-NS in pH7.4 PBS, pH6.8 PBS, and 0.1mol/L HCL（2h before）and pH 6.8 PBS（2h later） better, while the Retrer-Peppas model could fit the release profile of AM-NS in 0.1 mol/L HCL better. The f2 values of AM-NS in every two released medium were more than 50. On the other hand, thef2 values of AM-NS and free AM were all less than 50 in different dissolution conditions. Conclusion There was no difference between every two in vitro release curves of AM-NS in different release media, but the dissolution behaviors of AM-NS were obvious different from that of free AM when they were in the same release media. The in vitro release of AM from AM-NS was much slower than that of free AM.

关 键 词：阿奇霉素 囊泡 累积释放度 相似因子 

分 类 号：R972.6[医药卫生—药品]