高等学校化学学报

高等学校化学学报

• 研究论文 • 上一篇    下一篇

克拉霉素漂浮-生物粘附微囊的制备及性能研究

郑建华1; 刘朝武1; 包德才1,2; 赵燕军1; 马小军1   

  1. 1. 中国科学院大连化学物理研究所, 中国科学院研究生院, 大连 116023;
    2. 渤海大学化学与化工学院, 锦州 121000
  • 收稿日期:2005-06-02 修回日期:1900-01-01 出版日期:2006-06-10 发布日期:2006-06-10
  • 通讯作者: 马小军

Preparation and Characteristics of Floating-bioadhesive Microcapsules Containing Clarithromycin

ZHENG Jian-Hua1; LIU Chao-Wu1; BAO De-Cai1,2; ZHAO Yan-Jun1; MA Xiao-Jun1*   

  1. 1. Dalian Institute of Chemical Physics, Chinese Academy of Sciences,
    Graduate School of Chinese Academy of Sciences, Dalian 116023, China;
    2. College Chemical and Chemical Engineering, Bohai University, Jinzhou
    121000, China
  • Received:2005-06-02 Revised:1900-01-01 Online:2006-06-10 Published:2006-06-10
  • Contact: MA Xiao-Jun

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被引次数

32

摘要： 选用乳化-溶剂挥发法制备乙基纤维素载药微球(EMs), 并通过内部凝胶化法进行包衣制得海藻酸钠-乙基纤维素载药微囊(AEMs), 最后通过离子交联法进一步包衣制得壳聚糖-海藻酸钠-乙基纤维素载药微囊(CAEMs). 研究克拉霉素漂浮\|生物粘附微囊的制备工艺, 并考察微囊的体外漂浮性能、 粘附性能及体内滞留性能. 结果表明, CAEMs球形度较好, 药物包封率为72.3%~78.2%, 载药量为7.1%~12.7%. 在pH=5的醋酸缓冲液中, 6 h时的累积释放率为56.6%~70.6%, 漂浮率大于70%, 4 h时的体内滞留率为60.5%. CAEMs有望通过延长药物胃内滞留时间, 在临床用于根除幽门螺旋杆菌, 从而降低消化道溃疡的复发率.

关键词: 克拉霉素, 漂浮-生物粘附微囊, 体外漂浮性能, 胃内滞留性能, 幽门螺旋杆菌

Abstract: Floating-bioadhesive microcapsules containing clarithromycin were prepared by a combined method of emulsion solvent diffusion and internal/ion gelation for the treatment of Helicobacter pylori. Ethylcellulose microsphers(EMs) were prepared by the emulsion solvent diffusion method. EMs were coated with alginate and chitosan by the internal/ion gelation method to get alginate-ethylcellulose microcapsules(AEMs) and chitosan-alginate-ethylcellulose microcapsules(CAEMs). The drug efficiency and drug content of clarithromycin in CAEMs were determined to be 72.3%—78.2% and 7.1%—12.7%, respectively. CAEMs showed an obviously sustaining effect for more than 6h in vitro, and more than 70% of CAEMs floated in acetate buffer solution for 8 h in vitro. Furthermore, the in vitro remaining percentage of CAEMs in the stomach 4 h after the administration was 60.5%. The results suggest that floating-bioadhesive microcapsules might be a promising drug delivery system for the treatment of Helicobacter pylori infection.

Key words: Floating-bioadhesive microcapsules, In vitro floating characteristic, Gastric residence characteristic, Helicobacter pylori

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