中药一致性评价关键技术——中药溶出-系统指纹定量法评价溶出曲线相似性  

Dissolution-systematically quantified fingerprint method for evaluating the similarity in traditional Chinese medicine dissolution curves

作　　者：张凡[1] 杨婷 兰丽丽 张沁怡 迟晗笑 孙万阳 孙国祥[1,2] ZHANG Fan;YANG Ting;LAN Li-li;ZHANG Qin-yi;CHI Han-xiao;SUN Wan-yang;SUN Guo-xiang(College of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016;Medicinal Capital(Benxi)Consistency Science and Technology Ltd.,Company,Benxi Liaoning 117004;College of Pharmacy,Jinan University,Guangzhou 510632)

机构地区：[1]沈阳药科大学药学院,沈阳110016 [2]药都(本溪)一致科技有限公司,辽宁本溪117004 [3]暨南大学药学院,广州510632

出　　处：《中南药学》2021年第11期2245-2252,共8页Central South Pharmacy

摘　　要：目的建立中药溶出-系统指纹定量法,以复方甘草片为模型药物使用溶出-宏定性相似度(S_(m))和溶出-宏定量相似度(P_(m))评价供试制剂与参比制剂溶出曲线一致性。方法以复方甘草片为例,在水和pH 1.0盐酸溶出介质中,用紫外全指纹溶出度测定法测定样品累积溶出度和溶出曲线,用S_(m)、P_(m)及f_(2)评价溶出曲线相似性,并研究f_(2)与P_(m)间的关系。结果用中药溶出-系统指纹定量法的S_(m)、P_(m)评价溶出曲线相似性,在选择不同溶出介质和不同参照标准时,评价结果显著不同。当溶出曲线满足①S_(m)≥0.9和②90%≤P_(m)≤110%时f_(2)基本大于50。结论本方法从定性和定量两个方面对复方甘草片溶出曲线进行评价,可揭示不同厂家产品质量的差异性。中药制剂溶出曲线可定在DG3(85%≤P_(m)≤115%)。特殊情况,考虑中药多成分复杂性可定在DG5(①S_(m)≥0.9和②70%≤P_(m)≤130%)。中药制剂溶出曲线相似性标准要根据制剂工艺复杂程度和制剂稳定性情况来确定。Objective To establish traditional Chinese medicine(TCM)dissolution-systematically quantified fingerprint method(DSQFM)to evaluate the consistency of dissolution curves between the test preparation and the reference preparation of TCM solid formulations was evaluated by the dissolution-macro qualitative similarity(S_(m))and the dissolution-macro quantitative similarity(P_(m)).Methods Compound liquorice tablets(CLTs)was used as the model medicine.The cumulative dissolution of CLTs samples was measured by the overall UV fingerprint dissolution assay in water and pH 1.0 hydrochloric acid dissolution media.The experiment results were evaluated by S_(m),P_(m) and f_(2) to determine the corelation between f_(2) and P_(m).Results With S_(m) and P_(m) of DSQFM to evaluate the dissolution curves of CLTs,the evaluation results varied significantly with different dissolution media and reference preparations.It clearly reflected the in vitro dissolution difference among CLTs produced by different manufacturers.When the dissolution curve profile met the following requirements①S_(m)≥0.9 and②90%≤P_(m)≤110%,the f_(2) was greater than 50.Conclusion The method can evaluate the dissolution process of CLTs both qualitatively and quantitatively,revealing the difference in products quality consistency by different manufacturers.The dissolution profile of TCM formulations can be set at dissolution grade 3(85%≤P_(m)≤115%).It also can be set as dissolution grade 5(①S_(m)≥0.9 and②70%≤P_(m)≤130%)in some occasions due to the complex conponents of TCM.Dissolution similarity criteria for TCM formulations should be established according to the complexity of the formulation and stability.

关 键 词：中药溶出-系统指纹定量法 溶出曲线相似性评价 溶出-宏定性相似度 溶出-宏定量相似度 复方甘草片 

分 类 号：R917[医药卫生—药物分析学] R284[医药卫生—药学]