盐酸环丙沙星泡片.docVIP

摘要　目的:制备盐酸环丙沙星阴道泡腾片并建立该制剂的质量控制标准。方法:采用正交设计对处方辅料进行筛选，考察制剂的稳定性及体外释药性能，以紫外分光光度法测定盐酸环丙沙星的含量。结果:制备工艺可行，制剂体外释药性能优于普通片剂、栓剂，对光、热稳定，对湿度不稳定。结论:该制剂为一新型局部外用制剂，质量控制方法准确可靠。关键词　盐酸环丙沙星；阴道泡腾片；质量控制中图分类号：R944.4　　文献标识码：A　　文章编号：1001-5213(2000)04-0205-03 Preparation and quality control of ciprofloxacin hydrochloride vaginal effervescent tablet Liu Hui,Yang Ginxiang,Tang Ren(Wuhan General Hospital of Guangzhou Command PLA,Hubei Wuhan 430070) ABSTRACT　OBJECTIVE：To prepare ciprofloxacin hydrochloride vaginal effervescent tablets and establish quality control standard.METHODS：The formulational excipients were selected by means of orthogonal design method. Both the stability and the drug release property of the effervescent tablet were studied.A spectrophotometric method for determination of this preparation was established.RESULTS：The preparing method was practical.The drug release property of this preparation was better than general tablet and suppository.The preparation was stable to light and heat,but was unstable to humidity.CONCLUSIONS：ciprofloxacin hydrochloride is a new preparation for topical use.KEY WORDS　ciprofloxacin hydrochloride;vaginal effervescent tablet;quality control 　　盐酸环丙沙星(ciprofloxacin hydrochloride)是第三代喹诺酮类广谱抗菌药，对由绿脓杆菌、革兰阳性菌和阴性菌等引起的妇科感染疗效显著［1］。现有环丙沙星片剂和注射剂可供使用。为了增强其局部治疗效果，根据环丙沙星的药理作用特点，制备CIP*HCL阴道泡腾片，使药物在阴道内经由片剂泡腾崩解后，均匀持久的分布于阴道内壁和宫颈粘膜，增加药物与组织的接触面积，产生良好的阴道局部治疗作用，现报道如下。 1　仪器与试药 1.1　仪器　UV-260紫外分光光度计(Shimadzu)；pHS-2型酸度计(江苏金坛电子仪器厂)。1.2　试药　盐酸环丙沙星(浙江新昌制药厂，批号961226)；十二烷基硫酸钠(上海大众制药厂)；海藻酸钠(温州东升化学试剂厂)；鲸蜡醇(北京化工厂)；PEG-1000(广州化学试剂批发部)；吐温-80，司盘-80(广东顺德风化二厂)；酒石酸、酒石酸氢钾、碳酸氢钠、硼酸、硬脂酸镁、羧甲基纤维素钠(CMC-Na)、淀粉均为药用辅料。 2　处方与制剂工艺 2.1　处方确定　泡腾制剂的主要赋形剂为酸源、碱源构成的泡腾剂及表面活性剂组成的稳泡剂。以酸度和浊度为指标，设计L9(34)正交试验，因素和水平见表1。经方差分析，最佳泡腾剂处方为A3B3C2D1。以泡沫高度、维持时间、细度和吸附程度为指标，设计L9(34)正交试验，因素和水平见表2。经综合平衡法分析，最佳稳泡剂处方为A2B2C3D1。故确定盐酸环丙沙星阴道泡腾片处方为(每100片)：盐酸环丙沙星25g，酒石酸10g，酒石酸氢钾10g，碳酸氢钠12g，硼酸6g，十二烷基硫酸钠1g，海藻酸钠0.01g，鲸蜡醇1g，淀粉45g，CMC-Na1g，加硬脂酸镁适量。 　　　表1　泡腾剂因素水平表 水平 因　　　　　　素 A(酒石酸)g B(酒石酸氢钾)g C(碳酸氢钠)g D(硼酸)g 1 0.08 0.06 0.20 0.06