超临界流体制备BSA包衣微丸及释药特性

Preparation of BSA pellets by supercritical carbon dioxide fluid and in vitro evaluation

目的采用自行设计的CO2超临界流体(supercritical carbon dioxide,ScCO2)包衣设备研究肠溶包衣参数,为开发蛋白质及多肽的口服制剂提供工艺基础。方法以载牛血清白蛋白(bovine serumalbumin,BSA)颗粒为微丸核心,以EUDRAGIT L100-55作为pH敏感的肠溶包衣材料,采用正交表研究压力、温度、增塑剂和包衣持续时间等不同的工艺参数组合,并考察肠溶包衣微丸的形态学和体外释放特性,以选择最优的二氧化碳超临界流体包衣工艺。结果压力为20MPa、温度为35℃、使用40%增塑剂的条件下包衣30min,所得BSA微丸在模拟胃液中释放量小于5%,在模拟肠液中迅速释放,符合肠溶包衣的要求。结论得到了通过ScCO2制备肠溶微丸的最优参数组合,为二氧化碳超临界流体包衣的进一步研究提供了基础。

Objective To prepare enteric-coated BSA pellets by supercritical carbon dioxide （ScCO2） and to screen an optimum coating art by ScCO2. Methods An L9 （34 ） orthogonal table was designed to select an optimum coating art by ScCO2, BSA pellets were characterized by morphology and in vitro release profile. Results In vitro evaluation of BSA pellets coated by parameters of 20 MPa, 35℃, 40% plasticizer for 30 min showed that the cumulative release percentage of BSA in 0. 1 mol/L HC1 was less than 5%. Conclusions An optimum coating art by ScCO2 has been successfully screened and enteric-coated BSA pellets are successfully produced.