羟丙基甲基纤维素对左金胃漂浮缓释片的漂浮性能和药物释放特征的影响

Effect of HPMC on floatation and release of Zuojin Gastric Floating Sustained-release Tablet

目的:探讨不同品种的羟丙基甲基纤维素(HPMC)对左金胃漂浮缓释片的漂浮和释药特征的影响,并优选最佳品种。方法:以不同厂家生产的7个HPMC品种为主要辅料制备7种左金胃漂浮缓释片,以起漂时间和持续漂浮时间评价制剂的漂浮性能,以小檗碱和巴马汀体外释放度评价制剂的释放特征。结果:HPMCMK-100000和MK-15000制备的片子快速崩解,不具有漂浮和缓释特征;K-100M和MK-4000所制备的片子起漂时间长,药物释放缓慢;60RT-50、K-4M和MK-1500所制备的片子起漂时间短,持续漂浮时间长,药物释放速度适中,均可作为左金胃漂浮缓释片的亲水凝胶骨架材料。结论:HPMC的品种显著影响左金胃漂浮缓释片的漂浮和释药特征,HPMC60RT-50为最佳品种。

AIM： To elucidate the effect of HPMC on the floating and releasing performances of Zuojin Gastric Floating Sustained-Release Tablets（ ZJ -GFST） and to select the optimum matrix adjuvant for ZJ -GFST.METHODS： Seven kinds of ZJ -GFST from pharmaceutical factories as main adjuvant respectively. The floating lag time and the sustained floating time were used to evaluate the floating performance of ZJ - GFST. The accumulative relea- sing rates of berberine and palmatine in vitro were used to evaluate the releasing efficiency of ZJ - GFST. RESULTS ： The tablets prepared with HPMC MK - 100000 and MK-15000 disintegrated quickly when contacting with water, and the tablets prepared with HPMC MK-100M and MK-4000 had too long floating lag time and low release speed. The tablets prepared with HPMC 60RT-50,K-4M and MK-1500 all possessed short floating lag time and long sustained floating time and suitable drug releasing rate. CONCLUSION： The selected HPMC is 60RT-50.