阳离子阿奇霉素泡囊的研制及体内评价  

Preparation and evaluation of azithromycin niosomes

作　　者：钟萌[1] 赵德璋[1] 冯悦[2] 张敉[1] 张景勍[1] 

机构地区：[1]重庆医科大学药物高校工程研究中心,重庆400016 [2]泸州医学院附属医院核医学科,泸州646000

出　　处：《中国抗生素杂志》2014年第10期750-753,768,共5页Chinese Journal of Antibiotics

摘　　要：目的制备阿奇霉素泡囊(AZI-NS),并研究其体外释放性质以及体内药动学特征。方法采用薄膜蒸发-冻融法制备阿奇霉素泡囊,动态膜透析法考察其体外释放。单剂量口服给予阿奇霉素泡囊和原料药,HPLC法测定血浆药物含量。结果AZI-NS改善了AZI的溶出行为。单次给药后AZI-NS和AZI的主要药动学参数Cmax为9.20和10.31mg/L,Tmax为4和2h,AUC0-∞为263.16和158.50(mg·h)/L。结论将AZI制备成泡囊后显示出了较好的缓释效果并提高了药物的生物利用度。Objective To study the in vitro release and pharmacokinetics of azithromycin niosomes （AZI- NS）. Methods The film-evaporation combining with freeze-thawing method was used to prepare AZI-NS and drug release in vitro observed by dynamic penetration system. Rats were administrated with AZI-NS and AZI solution. The plasma concentrations of the drugs in ophthalmic vein blood were determined using HPLC. Results AZI-NS improved the dissolution behavior of AZI. The Cmax, T AUC（0-∞） of AZI-NS and AZI were 10.31 and 9.2mg/L, 4 and 2h, 263.159 and 158.498（mg·h）/L, respectively. Conclusion AZI-NS showed better sustained release effect and improved the bioavailability as compared with AZI solution.

关 键 词：阿奇霉素泡囊 体外释放 药动学 

分 类 号：R979.1[医药卫生—药品]