治疗2型糖尿病的黄连解毒汤制剂改良及药效学评价  

Improvement and pharmacodynamic evaluation of Huang Lian Jie Du Tang for the treatment of type 2 diabetes

作　　者：李驭帅 刘松枝 林耀新 廖苏玲 孙长山[2] LI Yushuai;LIU Songzhi;LIN Yaoxin;LIAO Suling;SUN Changshan(School of Traditional Chinese Materia Medica,Shenyang Pharmaceutical University,Shenyang 110016,China;School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]沈阳药科大学中药学院,辽宁沈阳110016 [2]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《中国药剂学杂志（网络版）》2022年第1期14-32,共19页Chinese Journal of Pharmaceutics：Online Edition

摘　　要：目的将中医传统方剂黄连解毒汤优化改良为无糖颗粒剂,并对其治疗2型糖尿病进行药效学评价。方法通过高效液相色谱法对乙醇浓度单因素考察、采用综合评分及正交实验设计优化,筛选黄连解毒汤最优提取方案;通过稀释剂种类筛选、混合稀释剂比例筛选、稀释剂与提取粉比例筛选和润湿剂乙醇浓度筛选得出黄连解毒无糖颗粒剂的最优制剂处方工艺;以大鼠状态观察、血糖及胰岛素监测、口服糖耐量试验、血脂监测、肝功能指标以及稳态模型胰岛素抵抗指数、胰岛素敏感性指数评价作为药效考察项。结果黄连解毒汤最优提取方案为用体积分数60%的乙醇,提取3次,每次提取时间为2 h,提取溶剂与药材液料比为8:1;黄连解毒无糖颗粒剂最优处方为提取粉:稀释剂总量比例为1:2,稀释剂中糊精:甘露醇比例为1:3比例量,以体积分数80%的乙醇作润湿剂,1430μm孔径筛制粒60℃干燥即得;其药效学研究表明黄连解毒无糖颗粒剂?可改善大鼠精神状态,降低血糖血脂,保护肝功能,改善胰岛素抵抗并增加外周胰岛素敏感性。结论黄连解毒汤可通过现代工艺转变为无糖颗粒剂,解除患者用药限制,对治疗2型糖尿病有良好效果。objective To optimize and improve the traditional Chinese medicine prescription Huang Lian Jie Du Tang into sugar-free granules and make the pharmacodynamic evaluation in the treatment of type 2 diabetes.Methods The optimal extraction scheme of Huang Lian Jie Du Tang was selected through the single factor investigation of ethanol concentration,comprehensive score and orthogonal experimental design optimization by HPLC;The optimal formulation technology of Huang Lian Jie Du granules was obtained by the diluent type selection,the mixture diluent proportion selection,the diluent to extraction powder proportion selection,and the wetting agent ethanol concentration selection;The observation of the state of rats,the monitoring of blood glucose and insulin,the oral glucose tolerance test,the monitoring of blood lipid,the indexes of liver function,homeostasis model assessment for insulin resistance index and insulin sensitivity index were used as the pharmacodynamic items.Results The optimal extraction scheme of Huang Lian Jie Du Tang was ethanol(Φ=60%),3 times of extraction,2 hours of extraction time each time,the ratio of extraction solvent to medicinal materials was 8:1;The optimal prescription of Huang Lian Jie Du sugar-free granules was extraction powder:the ratio of total diluent was1:2,the ratio of diluent dextrin:mannitol was 1:3,ethanol(Φ=80%)was used as wetting agent;The granulating process was carried out by 1430μm sieving and dried at 60℃;Pharmacodynamics results showed that Huang Lian Jie Du Tang can improve the mental state of rats,reduce blood glucose and lipid,protect liver function,improve insulin resistance and increase peripheral insulin sensitivity.Conclusions Huang Lian Jie Du Tang can be transformed into sugar-free granules through modern research.Huang Lian Jie Du granules have good performance and good therapeutic effect on type 2 diabetes.

关 键 词：中药药剂学 无糖颗粒剂 单因素考察 正交实验 黄连解毒汤 2型糖尿病 药效学 

分 类 号：R943[医药卫生—药剂学]