蒲地蓝消炎口服液中黄芩提取工艺优化及其性质、含量及药动学研究  

Properties,content and pharmacokinetics of Scutellariae Radix from Pudilan Xiaoyan Oral Liquid after optimization of extraction process

作　　者：李萱 丁珂 杨挡 姜梦华 李超 朱法根 何丹丹[1,2] 孙娥[1,2] 封亮 贾晓斌 LI Xuan;DING Ke;YANG Dang;JIANG Meng-hua;LI Chao;ZHU Fa-gen;HE Dan-dan;SUN E;FENG Liang;JIA Xiao-bin(Affiliated Hospital of Integrated Traditional Chinese and Western Medicine,Nanjing University of Chinese Medicine,Nanjing 210028,China;Key Laboratory of New Drug Delivery Systems of Chinese Materia Medica,Jiangsu Province Academy of Traditional Chinese Medicine,Nanjing 210028,China;Jiangsu Key Laboratory of Chinese Medicine and Characteristic Preparations for Paediatrics,Jumpcan Pharmaceutical Co.,Ltd.,Taixing 225400,China;School of Traditional Chinese Pharmacy,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]南京中医药大学附属中西医结合医院,江苏南京210028 [2]江苏省中医药研究院国家中医药管理局中药口服释药系统重点研究室,江苏南京210028 [3]济川药业集团有限公司江苏省儿科中药与特色制剂重点实验室,江苏泰兴225400 [4]中国药科大学中药学院,江苏南京211198

出　　处：《中草药》2023年第10期3101-3108,共8页Chinese Traditional and Herbal Drugs

基　　金：国家重点研发计划项目(2018YFC1706902);国家中医药管理局重点研究室能力提升项目(2022GJJZDYJS-01);江苏省儿科中药与特色制剂重点实验室开放课题(BM2019011);江苏省科技成果转化专项资金(BA2020077);江苏省医学创新团队项目(CXTDB2017003);江苏省研究生实践创新计划项目(SJCX21-0716)。

摘　　要：目的优化蒲地蓝消炎口服液(Pudilan Xiaoyan Oral Liquid,PXOL)生产工艺过程中黄芩Scutellariae Radix提取工艺,比较该提取工艺变更前后PXOL的制剂性质、质量标志物含量及其药动学特征。方法以PXOL(原口服液)和黄芩新工艺PXOL(新口服液)的流浸膏物料性质为基础,通过比较两者的制剂性质、质量标志物含量以及体内的药动学特征,评价新口服液的合理性和可行性。结果与原口服液相比,新口服液pH值、浊度和黏度发生了显著性变化,不良口感降低了13%;主要有效成分黄芩苷含量增加了25%;同时通过药动学评价原口服液和新口服液在成年大鼠体内的差异可知,给予新口服液后,黄芩苷、汉黄芩素和腺苷的曲线下面积(area under the curve,AUC)均提高、达峰时间(time of C_(max),T_(max))均提前,4种质量标志物的平均滞留时间(mean residence time,MRT)均延长,表明新口服液在体内吸收快、起效迅速。结论新口服液相较于原口服液,制剂质量和制备效率均提高,降低了安全隐患和环保压力,科学合理。为新口服液的体内药效研究提供了数据支撑,也为其安全、合理用药奠定基础。Objective Optimize the extraction process of Huangqin(Scutellariae Radix)in the production process of Pudilan Xiaoyan Oral Liquid(蒲地蓝消炎口服液,PXOL),compare the preparation properties,quality marker content,and pharmacokinetic characteristics of PXOL before and after the change in the extraction process.Methods Based on the properties of the flow extract materials of Pudilan Xiaoyan Oral Liquid(PXOL,original oral liquid,OOL)and Scutellariae Radix new process PXOL(new oral liquid,NOL),the rationality and feasibility of the NOL were evaluated by comparing the preparation properties,quality marker content and pharmacokinetic characteristics of the two.Results Compared with OOL,the pH,turbidity and viscosity of NOL changed significantly,and the bad taste was reduced by 13%.The main active ingredient baicalin content increased by 25%;At the same time,through pharmacokinetic evaluation of the difference between the OOL and NOL in adult rats,it can be seen that after the administration of NOL,the area under the curve(AUC)of baicalin,wogonin and adenosine were increased,the T_(max) was advanced,and the mean residence time(MRT)of the four quality markers was prolonged,indicating that the NOL was absorbed quickly and had a rapid onset of effect in vivo.Conclusion Compared with OOL,NOL can improve the quality and preparation efficiency of the preparation,reduce the potential safety hazard and environmental protection pressure,which is scientific and reasonable.It provides data support for the study of the efficacy of PXOL,and also lays a foundation for its safe and rational drug use.

关 键 词：蒲地蓝消炎口服液 黄芩 合理性 物料性质 药动学 黄芩苷 汉黄芩素 腺苷 

分 类 号：R283.6[医药卫生—中药学]