中药复杂提取物无定形态转晶现象及其对溶出行为的影响研究——以葛根总黄酮为例  

Crystallization transformation of amorphous extracts of traditional Chinese medicine and its effect on dissolution behavior——Taking total flavonoids from Pueraria lobata as an example

作　　者：赵乙力 梁霖霖 何小双 衡伟利 庞遵霆 钱帅[1] 高缘[1] 张建军[2] 魏元锋[1] ZHAO Yili;LIANG Linlin;HE Xiaoshuang;HENG Weili;PANG Zunting;QIAN Shuai;GAO Yuan;ZHANG Jianjun;WEI Yuanfeng(School of Traditional Chinese Pharmacy,China Pharmaceutical University,Nanjing 211198;School of Pharmacy,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]中国药科大学中药学院,南京211198 [2]中国药科大学药学院,南京211198

出　　处：《中国药科大学学报》2023年第1期68-76,共9页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.81873012,No.82074029,No.82104401,No.82274217,No.82204636);中国博士后基金资助项目(No.2021M693517);中央高校基本科研业务费重点项目(No.2632021ZD15);江苏省博士后科研资助项目。

摘　　要：为保障中药产品质量,研究了中药复杂提取物的转晶现象及固态形式对理化性质的影响。以葛根总黄酮提取物为模型药物,通过不同条件下放样使其转晶,并进行特性溶出试验。发现环境应力条件下湿度是诱导葛根总黄酮转晶的关键因素,湿度越高,转晶越快;转晶后,葛根总黄酮溶出速率最高下降了96.51%。进一步模拟葛根总黄酮的制剂工艺后发现,引入了水分后的湿法制粒过程也将导致转晶行为并降低溶出速率。转晶样品的溶出速率与转晶量之间存在反比例关系。中药提取物在储存和制剂过程中均存在转晶风险,其转晶行为会对溶出速率产生显著影响,进而影响中药产品质量。本研究发现了无定形态中药复杂提取物的转晶现象,并系统研究了转晶现象对溶出行为的影响,为保障中药产品质量、促进中药制剂水平的提高提供了新的研究思路。In order to guarantee the quality of traditional Chinese medicines(TCMs),the crystallization transformation of complex extracts of TCMs and the influence of solid form on their physicochemical properties were studied.The extract of total flavonoids from Pueraria lobata was taken as a model.Crystallization transformation happened when lofting under different conditions,and the intrinsic dissolution tests were carried out.It was found that humidity was the key factor to induce crystallization of total flavonoids from Pueraria lobata.The greater the wettability was,the more the crystallization was.The dissolution rate of total flavonoids from Pueraria lobata with the most crystallization amount significantly decreased by 96.51% compared to the sample without crystallization.After further simulating the preparation process of total flavonoids from Pueraria lobata,it was found that the wet granulation process with introduced water would also lead to crystallization and reduced dissolution rate.As for all crystallization samples,there was an inversely proportional relationship between the dissolution rates and the amount of crystallization.The risk of crystallization existed both in the storage and preparation process of TCM extracts.Crystallization would significantly affect the dissolution rate,and thus the quality of TCM products.In this study,the crystallization transformation of amorphous complex TCM extracts was discovered,and the effect of the crystallization transformation on its dissolution behavior was systematically studied,which provides a new research idea for assuring the quality of TCM products and promoting the improvement of TCM preparation level.

关 键 词：中药提取物 无定形态 转晶 葛根总黄酮 溶出速率 

分 类 号：R913[医药卫生—药学]