目的 基于黄连解毒汤（Huanglian Jiedu Decoction，HJD）部分药效和毒副作用评价抑苦掩味伴侣剂［纽甜、单甲氧基聚乙二醇-左旋聚乳酸（mPEG₂₀₀₀-PLLA₂₀₀₀）、γ-环糊精（γ-CD）、HJD药液（以生药量计0.2 g/mL）质量比0.028∶0.15∶1.5∶100］对中药汤剂疗效和安全性的影响。方法 以HJD为例，采用体外抗氧化（1,1-二苯基-2-苦基肼基自由基清除率、超氧阴离子清除率和羟自由基清除率）、抗二甲苯致小鼠耳肿胀和解内毒素致小鼠高热试验研究抑苦掩味伴侣剂对中药汤剂疗效的影响，以小鼠急性毒性试验研究该伴侣剂对汤剂安全性（毒性）的影响，最后采用16S rDNA测序技术探索抑苦掩味伴侣剂对中药汤剂作用（可能的不良反应）的影响。结果 抑苦掩味伴侣剂既不影响HJD体外抗氧化（1,1-二苯基-2-苦基肼基自由基、超氧阴离子和羟自由基清除率）作用，也不影响HJD抗二甲苯致小鼠耳肿胀效果和抗内毒素致热作用。同时，在实验剂量范围内，抑苦掩味伴侣剂和HJD对小鼠均无急性毒性。此外，抑苦掩味伴侣剂对小鼠肠道菌群的干扰与HJD并无显著性差异。结论 抑苦掩味伴侣剂在实验剂量范围内不影响HJD的药效和安全。

Objective To evaluate the effect of the bitter taste-masking companion [with mass ratio of neotame, mPEG₂₀₀₀-PLLA₂₀₀₀, γ-CD and Huanglian Jiedu Decoction (HJD, 黄连解毒汤) of 0.028:0.15:1.5:100] on the efficacy and safety of traditional Chinese medicine decoction, partial efficacy and toxic side effects of HJD were explored. Methods HJD was taken as an example in this study. Antioxidant activity in vitro (1,1-diphenyl-2-picrylhydrazyl radical scavenging rate, hydroxyl radical scavenging rate and superoxide anion radical scavenging rate), inhibition of xylene-induced ear edema and anti-endotoxin-induced fever test in mice were used to study the effect of the companion of bitter taste-masking on decoction. An acute toxicity test in mice was performed to determine the safety of the companion. Finally, the 16S rDNA sequencing technique was used to analyze the effect of companion on decoction (possible side effects) of microflora in the gut tract. Results The companion did not affect the antioxidant effect of HJD in vitro (1,1-diphenyl-2-bitter hydrazine free radical, superoxide anion and hydroxyl radical clearance), it also did not affect the role in the inhibition of xylene-induced ear edema and anti-endotoxin-induced fever effect of HJD in mice. At the same time, within the experimental scope, neither the companion nor HJD was acutely toxic to mice. In addition, the disturbance of the companion agent to the intestinal flora of mice was not significantly different from HJD. Conclusion The companion didn’t affect the efficacy and safety of HJD within the experimental dosage range.

R283.6

国家自然科学基金项目（81803745）；国家博士后科学基金面上项目（2020M683269）