小檗碱生物黏附缓释片的制备及体外评价

摘要

Objective To prepare berberine bioadhesive sustained-release tablets,to study its release in vitro and to measure its adhe-sion with gastric tissue of rats.Methods HPMC and carbopol were used as the bioadhesive material of bioadhesive sustained release tablets,and dosage of excipients had gone through orthogonal design optimization in formulation.Release rate of bioadhesive sustained release tablets was measured with artificial gastric juice(pH =1.2)as the dissolution medium.Homemade adhesion measuring instru-ment was used in measuring and comparing the adhesion to rat gastric tissue between that of berberine bioadhesive sustained release tablets and of berberine hydrochloride tablets.Results In each piece of bioadhesive sustained release tablet 974P/971P was 1 /3,the amount of carbopol was 20 mg,and HPMC was 15 mg.Release in vitro of bioadhesive release tablets was in line with sustained-release formulation of claim,and the rat gastric tissue adhesion was significantly greater than the conventional tablets.Conclusion Prescription and process of berberine bioadhesive sustained release tablets can meet the design requirements.%目的：测定小檗碱生物黏附缓释片和大鼠离体胃组织的黏附力，探究其体外释药作用，制备小檗碱生物黏附缓释片。方法以羟丙基甲基纤维素（HPMC）和卡波姆（carbopol，CP）为生物黏附材料，通过正交试验对辅料用量进行优化。测定生物黏附缓释片的释放度，溶出介质为人工胃液（pH ＝1．2）。通过自制黏附力测定装置测定、比较小檗碱生物黏附缓释片和盐酸小檗碱片对大鼠离体胃组织的黏附力。结果每片生物黏附缓释片中974P／971P 为1／3，卡波姆用量为20 mg，羟丙基甲基纤维素为15 mg。生物黏附缓释片的体外释放达到缓释制剂要求，与普通片剂相比其对大鼠离体胃组织的黏附力更大。结论小檗碱生物黏附缓释片的处方和工艺能够达到设计要求。