水性包衣工艺制备红霉素肠溶微丸的研究

Studies on preparation of erythromycin enteric pellets by aqueous coating process

目的 采用丙烯酸树脂水性包衣工艺制备红霉素肠溶微丸。方法 采用切线喷型流化床包衣设备和肠溶丙烯酸树脂水性包衣材料对红霉素微丸进行包衣 ,考察药物体外释放度和稳定性 ,并进行人体生物利用度研究。结果 包衣微丸具有良好的肠溶效果 ,pH1.2盐酸溶液中释放量小于 10 % ,pH6 .8磷酸盐缓冲液中药物迅速释放完全。微丸体外稳定 ,工艺重现性好。 2 0例健康志愿者体内药动学证明 ,自制肠溶胶囊与进口对照品生物等效 ,相对生物利用度 (10 0 .5 9± 19.47) %。结论 水性包衣方法制备红霉素肠溶微丸工艺可行 ,制剂质量稳定。

OBJECTIVE The aqueous acrylic coating process was adopted to develop the erythromycin enteric pellets.METHOD The erythromycin pellets were developed by layering technique, and were coated by aqueous coating formulation(Eudragit L100 55) in tangential spray fluid bed.The drug release profiles in vitro and stability of coated pellets were studied.The bioavailability of enteric capsules were studied in 20 healthy male volunteers,the imported capsules were used as the reference.RESULTS The acrylic coated pellets showed enteric release profiles in vitro. Less than 10% of the drug was released in pH1.2 HCl solution, while the drug was quickly released in pH6.8 buffer.The coated pellets were stable after storage for 3 months.The pharmacokinetic results showed that the erythromycin enteric capsule was bioequivalent to the imported capsule, and the relative bioavailability was (100.59±19.47)%.CONCLUSION The erythromycin enteric pellets can be developed by the aqueous acrylic coating process with good reproduction and stability.