溶剂蒸发-沉积法制备溴吡斯的明掩味固体分散体  

Preparation of taste masking of pyridostigmine bromide solid dispersion by solvent evaporation-deposition method

作　　者：张梨[1] 谭群友[2] 邓波[2] 程训官[3] 刘碧林[1] 张景勍[1] 

机构地区：[1]重庆医科大学药物高校工程研究中心和生物化学与分子药理学重点实验室,重庆400016 [2]第三军医大学大坪医院野战外科研究所胸外科,重庆400042 [3]重庆医科大学药物化学与生物材料研究室,重庆400016

出　　处：《中国医院药学杂志》2011年第21期1773-1777,共5页Chinese Journal of Hospital Pharmacy

基　　金：教育部博士点基金资助项目(编号:20095503120008);重庆市教育委员会资助项目(首批高等学校优秀人才资助;编号:KJ090308)

摘　　要：目的:研制溴吡斯的明掩味固体分散体,并对其进行初步稳定性考察。方法:通过正交试验设计,以综合评分为指标优化处方和制备工艺,通过红外分光光度法(IR)和差示扫描量热法(DSC)对药物可能存在状态进行判断。加速实验条件下考察固体分散体的初步稳定性。结果:掩味固体分散体的最优处方是以甘露醇作为不溶性载体、药物与EUDRAGITEPO质量比为1∶3,分散颗粒黏度为150～180μm。IR和DSC表明,药物可能以无定形状态分散于载体中。加速实验条件6个月,固体分散体的外观、含量和2 min累积溶出率无显著性变化。结论:采用溶剂蒸发-沉积法可成功制备溴吡斯的明的掩味固体分散体,其初步稳定性较好。OBJECTIVE To prepare taste masking of pyridostigmine bromide sohd dtsperston and to mvesttgate prenmmary stability. METHODS The optimum preparation condition was studied by orthogonal test with composite score as the index of evaluation. The solid dispersion was identified by infrared spectra （IR） methods and differentials scanning calorimetry （DSC）. Stability was investigated in accelerated test. RESULTS The optimum formulation technology factors were as follows： insoluble carrier was mannitol, the ratio of pyridostigmine bromide to EUDRAGIT EPO = 1：3 （quality ratio） and the size of particle was 150- 180μm. IR and DSC tests showed presence of pyridostigmine bromide in carriers maybe in the form of amorphous. There were no significant differences in characters, content and cumulative drug dissolution rate in 6 months. CONCLUSION Preparation of solid dispersion using solvent evaporation-deposition method covered the bitterness of pyridostigmine bromide effectively and was stable in accelerated test.

关 键 词：溴吡斯的明 掩味 固体分散体 溶剂蒸发-沉积法 

分 类 号：R943[医药卫生—药剂学]