黄芩苷口崩片的制备及质量标准研究

The Preparation and quality standard of orally disintegrating tablets of balcalin

目的筛选黄芩苷和β-环糊精包合物的最佳比例,解决黄芩苷溶出度低的难题,提高黄芩苷的临床应用。方法用喷雾干燥的方法,制备了黄芩苷-β环糊精1∶1、1∶2、1∶3、2∶1的包合物。用紫外分光光度法测定其含量,用智能溶出仪测定其溶出度,以累积溶出率与包合物的包载量等因素为指标,对各比例的包合物进行筛选。以崩解时间为指标,采用Lg(34)正交设计法优选口崩片处方,通过对口崩片中主要有效成分黄芩苷的含量测定,确定制剂的质量标准。以外观,含量,崩解时限和溶出参数为考察指标进行质量检查。结果 1.黄芩苷-β-环糊精包合物在溶出介质蒸馏水中有较高的溶出度,与黄芩苷原料药比较,各比例包合物在15min内溶出度已达90%以上,溶出速率快,溶出更完全。2.黄芩苷-环糊精口崩片在45min内溶出度达到85%以上,溶出度比单纯黄芩苷的溶出度高。3.最优崩解剂为交联聚维酮(PVPP),用量6%,采用内外加法。黏合剂为PVP,用量1%,硬度控制在4.0kg,矫味剂甘露醇和阿斯巴甜比例为1∶1。结论用本法制备黄芩苷口崩片可操作性强,制备工艺稳定可行且黄芩苷释放度良好,口感不错,具有良好的应用前景。

Objective We screen the optimal proportion of baicalin andβ-cyclodextrin inclusion complexes proportion,in order to solve the problem of low dissolution and improve the clinical application of baicalin.Methods In this paper,we use the spray drying method to prepare the baicalinβ-cyclodextrin with a ratio of 1∶1,1∶2,1∶3,2∶1,inclusion complex,its content was determined by ultraviolet spectrophotometry,its dissolution was determined by smart dissolution test,load factors as an indicator of cumulative dissolution rate of inclusion complex package,filter the proportion inclusion.Using disintegration time as indicators and Lg（34）Orthogonal Design to choose orally disintegrating tablets prescription;through counterpart collapse film the main active ingredient of baicalin content determination,through the appearance,content,disintegration time and dissolution parameters as examining index for quality check.Results 1.Baicalin-βentrapped cyclodextrin complex possess higher dissolution in the dissolution medium,compared with baicalin bulk pharmaceutical chemicals,the proportion of clathrate dissolved in 15 min has a percentage of more than 90%,the dissolution rate is fast and dissolution is more completely.2.The dissolution rate of Baicalin cyclodextrin orally disintegrating tablets within 45 min is more than85%,the dissolution of baicalin is higher than baicalin.3.The optimal disintegrant is cross-linked povidone（PVPP）with amount of 6%,using internal and external adder;adhesives is PVP with the amount of 1%;hardness control in the proportion of 4.0kg,the ratio of mannitol and taste masking agent aspartame is 1∶1.ConclusionBaicalin orally disintegrating tablets has a good operability prepared through this method,the preparation process is stable and the releasing rate of baicalin is good,it also tastes good,and may have a good application prospects.