对香豆酸壳聚糖生物黏附微球的制备与体内外评价  

Preparation and in vitro/in vivo Evaluation of p-Coumaric Acid Chitosan Microspheres

作　　者：吕琳[1] 何晓明[2] 赵婷[2] 贾炯[2] 党云洁[2] 

机构地区：[1]天津泰达国际心血管病医院药剂科,天津300270 [2]河北医科大学药学院

出　　处：《中国药师》2016年第12期2218-2222,共5页China Pharmacist

基　　金：河北省自然科学基金青年基金项目(编号:H2016206584);河北省高等学校科学技术研究项目(编号:QN20131011)

摘　　要：目的:以壳聚糖为生物黏附材料制备对香豆酸微球,延长药物在体内吸收时间并提高其口服生物利用度。方法:采用喷雾干燥技术制备对香豆酸壳聚糖生物黏附微球,采用激光粒度仪和扫描电镜考察微球的粒径及外观形态,并考察其体外释放度;以大鼠为动物模型进行生物利用度评价。结果:所制备的黏附微球粒径在4μm左右,形态圆整,90 min内释放完全;在体内显示出较好的缓释和促吸收效果,大鼠口服后,相对生物利用度为222%。结论:制备的对香豆酸生物黏附微球具有较好的体内缓释效果,并显著提高了口服生物利用度,可为对香豆酸的制剂开发提供参考依据。Objective： To prepare p-coumaric acid microspheres with chitosan as the bioadhesive material to prolong the drug absorption time and improve the oral bioavailability. Methods ： Spray drying technology was used to prepare p-coumaric acid ehitosan bioadhesive microspheres. The particle size and morphology was evaluated respectively by a laser particle analyzer and a scanning electron microscope （SEM）, and the in vitro release was detected as well. SD rats were used as the animat model to study the bioavailability of the microspheres. Results： The particle size of microspheres was about 4 μm, and the shape was round, p-Coumaric acid was released completely from tile mierospheres in 90 rain in the simulated gastric juice. The relative bioavailabJity was 222% after oral administration when compared with free p-coumaric acid. Conclusion： The bioadhesive microspheres have good sustained release and significantly improved oral bioavailability, which provide important reference for the development of p-coumaric acid.

关 键 词：对香豆酸 壳聚糖 生物黏附微球 制备工艺 生物利用度 

分 类 号：R944.9[医药卫生—药剂学] R945[医药卫生—药学]