【作者】 靳文仙；

【导师】 赵广荣； 王春龙；

【作者基本信息】 天津大学 ， 制药工程， 2007， 硕士

【摘要】 外阴瘙痒是一种非常常见的妇科疾病,发病率较高。目前国内治疗该类药物主要是中成药,起效慢。而西药也只有单方制剂,不能同时起到止痒、消炎、杀菌、保护皮肤的作用。本文根据国内外用药情况,以利多卡因、盐酸苯海拉明,EX和麝香草酚为模型药物,研制了阴道用复方软膏剂,具有起效全面快速,使用方便等优势。通过乳化剂的考察和基质用量的正交试验,确定了复方软膏剂的最佳处方。即以平平加O为乳化剂,以白凡士林、液体石蜡、山嵛醇、单硬脂酸甘油酯为油相,甘油为水相,肉豆蔻酸异丙酯为透皮吸收促进剂。单因素考察了制备工艺参数,最终确定其理想工艺过程为:乳化温度80℃,将油相缓缓加入水相中,保温搅拌5min,再以1500rpm的速度搅拌至冷。建立了HPLC法同时测定利多卡因,盐酸苯海拉明和麝香草酚三组分含量的方法。采用C18色谱柱(46×250mm,5μm),以甲醇-pH8.0磷酸盐缓冲液-乙腈(60:25:15)为流动相,流速1.0ml/min,柱温35℃,255nm检测。经过方法学验证,该方法简便快速,结果准确可靠。同时还建立并方法学验证了HPLC法测定EX含量及利多卡因和盐酸苯海拉明的有关物质。对复方软膏的理化性质及稳定性进行了考察。结果本软膏外观,pH值,熔点,稠度均符合药典规定,通过染色法验证了本软膏为o/w型乳膏。影响因素和留样实验表明本软膏中EX及麝香草酚均对光和热敏感,应室温避光保存。更多还原

【Abstract】 Pruritus vulvae with a high attack rate is most common Gynecological disease. There are many medicine to treat this disease internal at present,most of which are chinese traditional medicine.Western medicine is only single preparation,which do not have the function of curing itch,dephlogistication and bacteriostasis simultaneously.On the basis of the requirement,lidocaine,benadryl hydrochloride, EX and thymol are taken as the model drugs to prepare the compound ointment which has rapid curative effect.After the investigation of emulsifier and basis material,we selected and optimized the formula by orthogonal design.The compound ointment was composed of peregal, liquid paraffin, docosyl alcohol, glyceryl monostearate, glycerin, isopropyl myristate and water.The study also includes praeparatum technology of the formula.An HPLC method was established to determine three constituent content in the same chromatographic condition. The drugs were eluted with the mobile phase of methanol-buffer phosphate（pH8.0）-acetonitrile（60:25:15） at the flow rate of 1.0mL·min^-1 on a C18 column at 35℃. The drugs were detected at the wavelength of 255nm. After validating,the method is convenient,rapid,accurate and reliable.We also established HPLC methods to determine the content of vitamin E and related substances of lidocaine and benadryl hydrochloride respectively.The physicochemical properties and stability of compound ointment were studied.The appearance,pH value, fusing point and consistance of the ointment all conformed to the pharmacopoeia stipulation. The ointment style was qualified by staining method as oil-in-water .From influential factors experiments, accelerated tests and room temperature trials, it could be concluded that EX and thymol were unstable,so the ointment should be preserved away from light in room temperature.更多还原