复合辅料微晶纤维素-单硬脂酸甘油酯的研究  

Study on co-processd excipient of microcrystalline cellulose and glycerol monostearate

作　　者：严红梅[1,2] 蒋艳荣[1,2] 唐欢[1] 孙娥[1] 贾晓斌[1,2] 张振海[1] 

机构地区：[1]江苏省中医药研究院国家中医药管理局中药释药系统重点研究室,江苏南京210028 [2]南京中医药大学,江苏南京210046

出　　处：《中草药》2014年第9期1245-1251,共7页Chinese Traditional and Herbal Drugs

基　　金：国家"十一五"科技支撑计划(2008BAI51B03);江苏省中医药科技项目(LZ11065)

摘　　要：目的拟制备微晶纤维素(MCC)-单硬脂酸甘油酯(GMS)复合辅料,尝试改善MCC在中药应用中的抗吸湿性,探讨该复合辅料应用于中药片剂制备中的可能性。方法喷雾干燥法制备MCC-GMS复合辅料。以吸湿性、流动性、可压性和崩解度为考察指标,采用均匀设计法优选复合辅料的制备工艺。考察复合辅料的粉体学特征,采用扫描电镜法(SEM)、差示扫描量热法(DSC)、X射线粉末衍射法(XRD)和傅里叶变换红外光谱法(FTIR)等分析复合辅料的微观结构,考察复合辅料对馨月舒、淫羊藿总黄酮和枸杞提取物的喷雾干燥粉体吸湿性影响,并对馨月舒片剂中金丝桃苷和阿魏酸的溶出行为进行研究。结果复合辅料最佳制备工艺是GMS-MCC-水(1∶12∶200)、乳化温度66℃,搅拌时间1 h,此时的综合考察指标最优。复合辅料经喷雾干燥后化学成分没有改变,粒径变小,显示较好的流动性,改善了馨月舒、淫羊藿总黄酮和枸杞提取物喷雾干燥粉体的吸湿性,并且不影响MCC本身的崩解性质。结论所制备的MCC-GMS复合辅料具有抗吸湿作用,是一种有应用前景的复合辅料。Objective The co-processd excipient containing microcrystalline cellulose （MCC） and glycerol monostearate （GMS） was prepared. The humidity resistance of MCC used in Chinese materia medica （CMM） was improved and the possibility of this co-processd excipient used in the preparation of CMM tablet was explored. Methods The co-processd excipient containing MCC and GMS was prepared by applying spray drying method. The moisture absorption, flow ability, compressibility, and disintegration were as the indexes to optimize the best preparation of co-proeessd excipient through uniform design methodology. The powder characteristic of co-processd excipient was investigated and the microstructures were studied by scanning electron microscope （SEM）, differential scanning calorimeter （DSC）, X-ray diffraction （XRD）, and Flourier transform infra-red （FTIR） spectroscopy. The effect of co-processd excipient on the moisture absorption of spray drying power of Xinyueshu, epimedium total flavonoids, and wolfberry extracts was investigated. The in vitro dissolution ofhyperside and ferulic acid in Xinyueshu Tablet was studied. Results The results showed that the optimal conditions of the preparation consisted of 1 portion of GMS, 12 portions of MCC, and 200 portions of water, emulsionzing temperature of 66 ℃, and mixing time of 1 h. It was confirmed that the chemical constituents in co-processd excipient were not changed after spray drying with smaller particle size and better fluidity. The co-processd excipient can improve the moisture absorption of spray drying power of Xinyueshu, epimedium total flavonoids, and wolfberry extracts without affecting the disintegration of MCC. Conclusion The co-processd excipient prepared has good humidity resistance and it is confirmed to have application prospect.

关 键 词：吸湿性 微晶纤维素 单硬脂酸甘油酯 粉体学特征 微观结构 溶出度 

分 类 号：R283.6[医药卫生—中药学]