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阿奇霉素口服微球的制备与评价
投稿时间:2020-02-05  修订日期:2020-05-18  点此下载全文
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作者单位E-mail
苏日娜 中国药科大学药学院 srnsurina@163.com 
樊万君 中国药科大学药学院  
张自强 南京泽恒医药技术开发有限公司  
何淑旺 山东达因海洋生物制药股份有限公司  
姚 静 中国药科大学药学院 yaojing@cpu.edu.cn 
基金项目:国家科技重大专项(2018ZX09721003-007-005) *
中文摘要:本研究旨在改善阿奇霉素(AZI)苦味与服药顺应性,以乙基纤维素(EC)为载体,采用O/W乳化溶剂挥发法制备载阿奇霉素口服微球(AZI-EC MS),对其释放与掩味效果进行初步考察,并通过差式扫描量热法、红外光谱和扫描电镜表征。本文通过联合应用不同分子量EC解决了微球突释问题,当药载比1:1、混合EC(N22/T10,7/3,m/m)为载体时,微球0.5 h累积释放量小于40 %,8 h累积释放量可达90 %;该微球载药量为(48.95 ± 0.86) %,形态圆整,表面光滑。AZI苦味阈值浓度为9.93 μg/mL,具有强烈苦味,相比之下,AZI-EC MS掩味效果良好。因此,混合EC为载体的AZI-EC MS能够改善AZI苦味,提高患者顺应性,为AZI新制剂的研究奠定基础。
中文关键词:阿奇霉素  微球  苦味阈值  乙基纤维素
 
Preparation and evaluation of azithromycin-loaded microspheres for oral administration
Abstract:To mask the bitterness of azithromycin and improve theSpatient compliance ,a azithromycin-loaded microspheres for oral administration was prepared by O/W solvent evaporation method with ethylcellulose as carrier(AZI-EC MS).In vitro drug release profile and taste masking effect of AZI-EC MS were assessed.Its physical properties and morphology were then investigated by DSC,FTIR and SEM analysis.The results indicated that the polymer weight of EC could influence the drug release behavior. With a drug polymer ratio of 1: 1 and mixed EC (N22 / T10, 7/3, m / m) as the carrier, the cumulative release of AZI-EC MS at 0.5 h was less than 40 % and achieved 90 % at 8 h.Moreover,Its available not only with smooth spherical morphology but also with high drug loading efficiency up to (48.95 ± 0.86) % ,and bitterness score was much lower than AZI according to fitting equation.Therefore, AZI-EC MS prepared in this study reduced bitter taste of AZI, easy to swallow and set the stage for the taste masking product and taste making evaluation of AZI.
keywords:azithromycin  microspheres  threshold  ethylcellulose
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