新型环索奈德胶囊型干粉吸入剂的研制及其质量研究  

Preparation and quality control of a novel capsule type of cyclesonide dry powder inhaler

作　　者：王桂玲[1] 李婷[1] 郑黎 吕万良[1] 张强[1] 

机构地区：[1]北京大学药学院药剂系,北京100083 [2]奥星公司,北京100020

出　　处：《中国新药杂志》2007年第11期872-876,共5页Chinese Journal of New Drugs

摘　　要：目的:研制用于治疗哮喘的环索奈德胶囊型干粉吸入剂,建立其含量测定方法,并对其稳定性进行初步考察。方法:用高效液相色谱-紫外法检测环索奈德干粉吸入剂中主药环索奈德及其有关物质的含量。将主药与辅料混合后,以含量均匀度和肺部沉积率为指标进行处方筛选,考察制剂的有关物质和影响因素,并进行了加速稳定性和长期留样稳定性试验。结果:建立的高效液相色谱法,色谱条件如下:色谱柱为Alltima C18(250 mm×4.6mm,5μm);流动相为乙醇-水(65∶35);流速为1.2 mL.min-1;检测波长为243 nm。最后选择乳糖作为辅料,确定了最佳处方和工艺,获得了较好的含量均匀度和肺部沉积率(约19%)。稳定性结果显示,本制剂应置于阴凉、干燥处保存,在室温下保存至少在1年内稳定,长期放置稳定性在继续考察。结论:建立的高效液相色谱法适合于环索奈德胶囊型干粉吸入剂的日常质量控制,研制的制剂处方稳定。Objective： To optimize the preparation, quantification and stability of a novel capsule type of cyclesonide dry powder inhaler （DPI）. Methods： The cyclesonide and related substances in the cyclesonide DPI was quantified by RP-HPLC consisted of an Alhima C18 column （250 mm × 4.6 mm, 5μm）, an eluate of ethanol and water （65： 35, v/v） with a flow rate of 1.2 mL·min^-1 and a detection wavelength at 243 nm. The formulations were optimized in accordance with the uniformity and pulmonary deposition ratio. The stability tests of the optimal cyclesonide DPI were conducted in accelerated and long-term stabilities settings. Results：The optimal ratio of lactose to cyclesonide was at 16 mg over 160μg, and the optimal pulmonary deposition ratio of the DPI was for 19%. The final cyclesonide DPI was stable for 1 year and up. Conclusion： The quality control of the stable cyclesonide DPI might be performed by the RP-HPLC.

关 键 词：环索奈德 干粉吸入剂 肺部沉积率 高效液相色谱法 

分 类 号：R927.2[医药卫生—药学] R974.3