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喷雾干燥法制备神经毒素壳聚糖鼻腔给药微球的研究

Preparation of Chitosan Microspheres Loaded with Neurotoxin-Ⅰ for Nasal Delivery by Spray Drying Technique

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【作者】 蔡鑫君夏爱晓柴国宝魏颖慧冯健李范珠

【Author】 CAI Xin-jun,XIA Ai-xiao,CHAI Guo-bao,WEI Ying-hui,Fen Jian,LI Fan-zhu*(College of Pharmaceutical Science,Zhejiang Chinese Medical University,Hangzhou 310053)

【机构】 浙江中医药大学药学院

【摘要】 目的制备神经毒素壳聚糖微球,并对其体外释药模式进行研究。方法采用喷雾干燥法制备神经毒素壳聚糖微球,以包封产率为指标,考察了处方与工艺因素对壳聚糖微球的影响,并采用正交设计L9(3)4对处方和工艺进行了优化。结果最优处方为壳聚糖浓度为0.75%,壳聚糖-TPP重量比为10∶1,进口温度105℃,空气流速550L/h。优化处方制备的神经毒素壳聚糖微球表面圆整,载药量为(19.23±0.42)%,包封产率为(92.10±2.1)%,平均粒径为(6.86±0.76)μm。体外释药数据用Higuchi模型拟合得方程Q=11.42t1/2-5.89(r=0.9920),表明该微球具有缓释作用。结论采用喷雾干燥法制备微球,具有工艺稳定、可连续操作等优点,制备的神经毒素壳聚糖微球具有较好的缓释特性,

【Abstract】 OBJECTIVE To prepare the preparation of neurotoxin-Ⅰloaded chitosan microspheres and to investigate the drug release behavior in vitro.Methods Microspheres were prepared using the spray drying method,the encapsulation efficiency was used to evaluate the influence of different formulation and preparation factors,the formulation was optimized by orthogonal design L9(3)4.Results The optimal formulation was as follows:chitosan concentration(0.75%),ratio of chitosan to TPP(10:1),inlet temperature(105℃),air flow rate(550L/h).The optimized microspheres had a spherical shape,the drug loading was(19.23±0.42)%,encapsulation efficiency was(92.10±2.1)%,average diameter was(6.86±0.76)μm.The drug release profile in vitro could be described by Higuchi equation Q=11.42t1/2-5.89(r=0.9920),the results showed the microspheres prepared obviously sustained release effect..Conclusion Preparation of sustained-release microcapsule by spray drying is a simple method,the process is stable.

【基金】 国家自然科学基金资助项目(30371781);国家自然科学基金资助项目(30772793)
  • 【会议录名称】 2008年中国药学会学术年会暨第八届中国药师周论文集
  • 【会议名称】2008年中国药学会学术年会暨第八届中国药师周
  • 【会议时间】2008-10
  • 【会议地点】中国河北石家庄
  • 【分类号】R94
  • 【主办单位】中国药学会、河北省人民政府
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