Objective To prepare Tetracycline Hydrochloride gastric floating microspheres using ionic gelation method,and to improve drug release percentage and therapeutic effect of anti-Helicobacter pylori.Methods Chitosan and alginate were chosen as the carriers,and NaHCO3 was utilized as the foaming agent.The orthogonal experiment was adopted to investigate the weight ration of tetracycline/alginate and alginate/NaHCO3,as well as the concentration of CaCl2 and chitosan.Therefore,the optimum preparation was determined by evaluating floating performances,drug release,encapsulation efficiency and balling index.Results The optimal conditions were as followed:the concentration of chitosan was 8 mg/mL,the weight ration of alginate/tetracycline was 4∶1,the concentration of CaCl2 was 20 mg/mL,and the weight ration of alginate/NaHCO3 was 2∶1.The microcapsules could float in stomach for 24 h with a floating rate of 95％,and the encapsulation efficiency was 79.90％.The in vitro experiments suggested that these floating microspheres had good sustain-release properties.Conclusion According to the results above,tetracycline gastric floating microspheres meet the requirements of gastric retention,which can increase drug absorption and therapeutic effect of antiHelicobacter pylori,reduce dosing frequency,and have more selection of dosage forms.%目的 采用离子胶凝法制备盐酸四环素胃内漂浮微球,改善其胃内释药及抗幽门螺旋杆菌治疗时的疗效.方法 选用壳聚糖及海藻酸钠为载体,以NaHCO3为起泡剂;通过正交试验考察海藻酸钠与药物用量比、壳聚糖浓度、CaCl2浓度、海藻酸钠与NaHCO3用量比等对其体外漂浮性能、体外释放、包封率、成球性的影响,筛选出最佳工艺.结果 最优工艺条件:壳聚糖浓度为8 mg/mL,海藻酸钠与药物比例为4∶1,CaCl2浓度为20 mg/mL,海藻酸钠与NaHCO3比例为2∶1,所制备的盐酸四环素胃内漂浮12h微球漂浮率为95％,包封率为79.90％,形态良好,体外试验具备缓释性.结论 该盐酸四环素胃内漂浮微球达到了胃内滞留要求,可提高吸收及抗幽门螺旋杆菌疗效,减少口服给药次数,可解决现有上市剂型的不足.
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