目的 设计包含腰痛宁胶囊全方10味中药在内的13个有效部位单方或组合共计10个样品，评价各样品的体内外抗炎镇痛活性，寻找以中药有效部位组合为基础的风湿骨病候选组方。方法 采用液闪发光分析仪测量计数，以同位素³H的量为评价指标，分别检测各样品抑制³H-缓激肽与其受体结合的能力及与³H-纳洛酮竞争结合阿片受体的能力，以评价各组方的体外抗炎、镇痛活性。对体外实验筛选出的组方，采用二甲苯致小鼠耳肿胀实验、热刺激痛阈实验及醋酸致扭体实验进一步评价样品的体内抗炎及镇痛活性。结果 腰痛宁胶囊全方具有较好的体外及体内抗炎、镇痛作用；由腰痛宁组方生物碱+黄酮+皂苷有效部位组合的拆方减少90%马钱子生物碱的量所得的腰痛宁减毒拆方（样品Ⅷ）以及由麻黄生物碱+甘草皂苷+红花黄酮等质量比混合的样品Ⅵ的体外抗炎、镇痛效果优于腰痛宁全方；但样品Ⅵ小鼠体内镇痛活性不明显，样品Ⅷ小鼠体内抗炎、镇痛效果显著优于腰痛宁全方，且其对小鼠醋酸致扭体反应实验中的镇痛活性显著优于对照药阿司匹林。结论 腰痛宁减毒拆方可作为风湿骨病新药候选药物；减少腰痛宁处方药材及有效部位种类以及马钱子生物碱的量可提高腰痛宁胶囊的抗炎镇痛活性、药物安全性及质量可控性。

Objective According to the results of preliminary cellular pharmacological experiments,13 active fractions,including Yaotongning Capsule(YTNC) whole formula,were designed to evaluate their in vitro and in vivo anti-inflammatory and analgesic activities to look for candidate prescriptions for rheumatism treatment.Methods The in vitro anti-inflammatory and analgesic effects of the prescriptions were estimated by detecting their ability to inhibit ³H-bradykinin binding to its receptor and ability to inhibit ³H-naloxone binding to opioid receptors,respectively.And the tests were conducted by a liquid scintillation counter to check the content of the isotope ³H as evaluating indicator.Ear edema model in mice induced by dimethylbenzene test,hot plate test,and acetic acid writhing test in mice were conducted to evaluate the in vivo anti-inflammatory and analgesic activities of the prescriptions.Results YTNC whole formula had good in vitro and in vivo anti-inflammatory and analgesic effects.However,the prescription containing equal amount of Ephedra sinica alkaloids,Glycyrrhiza uralensis aponins,and Carthamus tinctorius flavones(Sample Ⅵ) as well as the optimized and decomposed formula of YTNC(Sample Ⅷ),which was designed by reducing 90% of Strychnos nux-vomica alkaloids from YTNC's decomposed formula composed by alkaloids,flavonoids,and saponins in YTNC,performed more excellent in vitro anti-inflammatory and analgesic effects than whole formula of YTNC.However,Sample Ⅵ did not exhibit obvious in vivo analgesic effect,but the in vivo anti-inflammatory and analgesic activities of the optimized and decomposed formula of YTNC(Sample Ⅷ) were more significantly better than those of YTNC whole formula.It also had significantly better analgesic effect than aspirin(the positive control drug) in acetic acid writhing test.Conclusion The optimized and decomposed formula of YTNC could be a candidate drug for rheumatism treatment.The anti-inflammatory and analgesic effects,safety,and quality control ability of YTNC could be improved by reducing the varieties of material medicines and active fractions and the content of S.nux-vomica alkaloids in YTNC.

上海市科学技术委员会支撑项目（13401901100）