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›› 2005, Vol. 5 ›› Issue (5): 558-562.

• 生化工程专栏 • 上一篇    下一篇

生物粘附性微球的制备及其评价-I. 离子交联法制备生物粘附性微球及其粒径预测

仰振球,宋宝珍,李巧霞,樊红雷   

  1. 中国科学院过程工程研究所
  • 出版日期:2005-10-20 发布日期:2005-10-20

Preparation and Evaluation of Bioadhesive Microspheres Drug Delivery System- I. Preparation of Bioadhesive Microspheres by Ionic Crosslinking and Prediction of Their Diameter

YANG Zhen-qiu,SONG Bao-zhen,LI Qiao-xia,FAN Hong-lei   

  1. Institute of Process Engineering, CAS
  • Online:2005-10-20 Published:2005-10-20

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摘要： 以硫酸为离子交联剂，制备了几丁聚糖生物粘附性微球. 与硫酸盐作为离子交联剂相比，本方法制备的微球交联程度高，呈较规则的球形，表面致密，机械强度高，在人工模拟肠液中可以保存24 h以上. 微球的粒径是影响药物释放动力学的重要因素. 运用四因素二次正交回归组合设计方法考察了几丁聚糖浓度、交联剂浓度、交联时间和转速对微球粒径的影响，得出了制备几丁聚糖微球粒径的回归模型方程. 统计检验表明，其中几丁聚糖浓度和搅拌转速对微球粒径的影响最为显著.

关键词: 生物粘附性给药系统, 几丁聚糖, 离子交联, 微球, 实验设计

Abstract: Interest in drug delivery to the gastrointestinal tract by means of chitosan has been increasing. In this study, with the sulfuric acid solution as the crosslinker, chitosan bioadhesive microspheres were prepared via ionic crosslinking. The microspheres with spherical shape could be kept in the artificial simulated intestinal juice for more than 24 h, and also had high mechanical strength and more compact surface, compared with the microspheres crosslinked by sulfate. The diameter of the microsphere is the principal factor influencing the kinetic parameters of drug delivery. With the experimental design, four-factor second order orthogonal regression composite design, the influences of the factors of chitosan concentration, crosslinker concentration, crosslinking time and agitation speed were investigated, the regression equation with high reliability was obtained.

Key words: bioadhesive drug delivery system, chitosan, ionic crosslinking, microsphere, experimental design