盐酸环丙沙星胃漂浮缓释片的设计、制备与体外评价

Preparation and in Vitro Evaluation of Ciprofloxacin Hydrochloride Gastro-Retentive Tablets

目的考察聚合物,包括亲水凝胶骨架材料及膨胀剂,对盐酸环丙沙星胃漂浮缓释片漂浮性能和释放行为的影响。方法分别以羟丙甲纤维素(HPMC),羟丙纤维素(HPC)和羟乙基纤维素(HEC)为亲水凝胶骨架材料,以交联聚维酮(PVPP XL,PVPP XL-10)和交联羧甲基纤维素钠(CCS)为膨胀剂,制备盐酸环丙沙星胃漂浮缓释片,以起漂时间,漂浮持续时间和漂浮力为指标评价漂浮性能,以盐酸环丙沙星释放度为指标评价缓释性能。结果羟丙甲纤维素K250与交联聚维酮交联聚维酮XL合用可以获得起漂时间较短,漂浮持续时间较长且药物体外释放较理想的盐酸环丙沙星胃漂浮缓释片。结论聚合物的种类和用量对胃漂浮片的漂浮性能和药物释放特性具有显著影响,羟丙甲纤维素K250和交联聚维酮XL是制备盐酸环丙沙星胃漂浮缓释片的较合适聚合物。

OBJECTIVE To investigate the effect of polymers,including hydrophilic polymers and swelling aids,on floatability and dissolution of ciprofloxacin hydrochloride gastro-retentive tablets. METHODS Hydroxypropyl methyl cellulose（ HPMC）,hydroxyethylcellulose（ HEC） and hydroxypropylcellulose（ HPC） were used as hydrophilic swelling excipients,and disintegrants crospovidone（ PVPP XL and PVPP XL-10） or croscarmellose sodium（ CCS） were used as swelling agents to facilitate the swelling /floating and drug release. Initial floating time and floating duration were tested to evaluate buoyance,and drug dissolution was tested to evaluate the controlled release. RESULTS Using HPMC K250 and PVPP XL as excipients for ciprofloxacin hydrochloride gastro-retentive tablets could obtain products with rapid onset of floating,long floating durion and desirable drug release. CONCLUSION Variety and amount of polymers have dramatic effects on buoyance and drug release of gastro-retentive tablets. HPMC K250 and PVPP XL are suitable excipients for ciprofloxacin hydrochloride gastro-retentive tablets.