多指标优选银桑降糖颗粒辅料研究(1)
[摘要]该文通过研究各辅料对提取物的吸湿性影响，对制剂内多糖测定的干扰以及对小鼠血糖值的影响筛选了辅料种类，采用单因素试验法，以吸湿性，成型性和流动性为指标，测定了吸湿量，颗粒得率以及休止角，结合物料外观性状，筛选了辅料配比及用量，并测定了颗粒的相对临界湿度。优选的银桑降糖颗粒最佳辅料为桑叶清膏微晶纤维素四角蛤蜊粗多糖10∶9∶167，所得颗粒成型性，流动性好，且不易吸潮液化，其相对临界湿度为73%。经研究优选所得银桑降糖颗粒制剂工艺和处方科学可行，可以明显改善提取物易吸湿液化的性质，提高制剂稳定性，适合工业化生产，并为其他制剂筛选辅料提供借鉴。
[关键词]银桑降糖颗粒； 辅料； 吸湿性； 液化
Optimize excipients for Yinsang hypoglycemic granules by using multiple indexes
DU Junchao1，2， CHENG Jianming1，2， LIU Rui1，2， WANG Xinzhi1，2， ZHANG Qian1，2， ZHANG Wenying1，2， WU Hao1，2*
, 百拇医药
(1Jiangsu Key Laboratory of Research and Development in Marine Bioresoure Pharmaceutics， Nanjing University of
Chinese Medicine， Nanjing 210023， China；
2Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization， Nanjing 210023， China)
[Abstract]Optimal excipients were screened by studying the effect of different excipients on the hygroscopicity of the extract， testing polysaccharide in the preparation and blood glucose value Single factor tests were performed with hygroscopicity， formability and fluidity as the indexes， and the moisture content， granule yield and angle of repose were combined with physical characters of the materials to screen the proportioning and dosage of excipients Then the critical relative humidity of preferred Yinsang granules were measured The optimum excipients for Yinsang hypoglycemic granules were mulberry leaf pastemicrocrystalline cellulosemactra veneriformis crude polysaccharides (10∶9∶167) The obtained granules had good formability and fluidity， which were not easy to absorb moisture for liquefaction， with a critical relative humidity of 73% This formation process was reasonable and feasible， suitable for industrial production， which can significantly improve hygroscopicity and liquefaction properties of extracts， improve stability of Yinsang granules， and provide reference for screening of excipients for other preparations
, 百拇医药
[Key words]Yinsang granules； excipients； hygroscopicity； liquefaction
桑叶做为药食两用品，自古就有治疗糖尿病的记载，如《本草备要》[1]中：桑叶“代茶止消渴”。現代研究表明其降糖活性成分为生物碱类和黄酮类物质[2]。银桑降糖颗粒是基于传统中医药理论，将具有降血糖活性的海洋中药四角蛤蜊粗多糖[3]与桑叶提取物[4]进行配伍，制成用于治疗糖尿病的新药，目标剂型定为颗粒剂，其中间体的制备工艺和配伍比例已经确定，前期考察了不同干燥方式，发现桑叶提取物表面易形成膜化物，遇热即软很难干燥，干燥后提取物容易吸潮发黏液化，不易粉碎，不适用干浸膏粉和辅料混合制粒，故考虑采用清膏加辅料得软材制粒法，由于该制剂是含有多糖用来治疗糖尿病的药物，因此辅料需要满足几个条件：①能防止提取物吸潮液化；②不对血糖值产生影响；③不干扰多糖含量的测定。由于制剂中多糖加入量相对较少，且吸潮液化主要是由于桑叶提取引起，故先通过考察各辅料对桑叶提取物吸湿性影响，以及各辅料对多糖含量测定的干扰筛选出备选辅料，再对其是否影响血糖值进行研究，进一步考察制剂中辅料比例及用量，并对最终所得颗粒的相对临界湿度进行测定以验证制剂工艺。, http://www.100md.com(杜俊潮 程建明 刘睿 王欣之 张倩 张文英 吴皓)
[关键词]银桑降糖颗粒； 辅料； 吸湿性； 液化
Optimize excipients for Yinsang hypoglycemic granules by using multiple indexes
DU Junchao1，2， CHENG Jianming1，2， LIU Rui1，2， WANG Xinzhi1，2， ZHANG Qian1，2， ZHANG Wenying1，2， WU Hao1，2*
, 百拇医药
(1Jiangsu Key Laboratory of Research and Development in Marine Bioresoure Pharmaceutics， Nanjing University of
Chinese Medicine， Nanjing 210023， China；
2Jiangsu Collaborative Innovation Center of Chinese Medicinal Resources Industrialization， Nanjing 210023， China)
[Abstract]Optimal excipients were screened by studying the effect of different excipients on the hygroscopicity of the extract， testing polysaccharide in the preparation and blood glucose value Single factor tests were performed with hygroscopicity， formability and fluidity as the indexes， and the moisture content， granule yield and angle of repose were combined with physical characters of the materials to screen the proportioning and dosage of excipients Then the critical relative humidity of preferred Yinsang granules were measured The optimum excipients for Yinsang hypoglycemic granules were mulberry leaf pastemicrocrystalline cellulosemactra veneriformis crude polysaccharides (10∶9∶167) The obtained granules had good formability and fluidity， which were not easy to absorb moisture for liquefaction， with a critical relative humidity of 73% This formation process was reasonable and feasible， suitable for industrial production， which can significantly improve hygroscopicity and liquefaction properties of extracts， improve stability of Yinsang granules， and provide reference for screening of excipients for other preparations
, 百拇医药
[Key words]Yinsang granules； excipients； hygroscopicity； liquefaction
桑叶做为药食两用品，自古就有治疗糖尿病的记载，如《本草备要》[1]中：桑叶“代茶止消渴”。現代研究表明其降糖活性成分为生物碱类和黄酮类物质[2]。银桑降糖颗粒是基于传统中医药理论，将具有降血糖活性的海洋中药四角蛤蜊粗多糖[3]与桑叶提取物[4]进行配伍，制成用于治疗糖尿病的新药，目标剂型定为颗粒剂，其中间体的制备工艺和配伍比例已经确定，前期考察了不同干燥方式，发现桑叶提取物表面易形成膜化物，遇热即软很难干燥，干燥后提取物容易吸潮发黏液化，不易粉碎，不适用干浸膏粉和辅料混合制粒，故考虑采用清膏加辅料得软材制粒法，由于该制剂是含有多糖用来治疗糖尿病的药物，因此辅料需要满足几个条件：①能防止提取物吸潮液化；②不对血糖值产生影响；③不干扰多糖含量的测定。由于制剂中多糖加入量相对较少，且吸潮液化主要是由于桑叶提取引起，故先通过考察各辅料对桑叶提取物吸湿性影响，以及各辅料对多糖含量测定的干扰筛选出备选辅料，再对其是否影响血糖值进行研究，进一步考察制剂中辅料比例及用量，并对最终所得颗粒的相对临界湿度进行测定以验证制剂工艺。, http://www.100md.com(杜俊潮 程建明 刘睿 王欣之 张倩 张文英 吴皓)