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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 To design a total of 10 samples including 13 effective parts of Yaotangning capsule, including 10 herbs, and evaluate the anti-inflammatory and analgesic activity of each sample in vitro and in vivo. To find rheumatoid osteoporosis Candidate group side. Methods The liquid ice-flash luminometer was used to measure the amount of 3H-bradykinin, the amount of isotope 3H was used as the evaluation index, the ability of each sample to inhibit the binding of 3H-bradykinin to its receptor and the ability to compete with 3H- To evaluate each group of anti-inflammatory and analgesic activity in vitro. The in vitro experiments were conducted to determine the anti-inflammatory and analgesic activities of the samples in vitro. The experiments were conducted using xylene-induced mouse ear swelling test, heat stimulation pain threshold test and acetic acid writhing test. Results All of Yaotongning Capsule had good anti-inflammatory and analgesic effects in vitro and in vivo. Low back pain was obtained by reducing the amount of alkaloids of Strychnos nux-vomica by combining the effective fractions of the alkaloids + flavonoids + saponins of Yaotongning. The antiinflammatory and analgesic effects of Ning attenuated demolition prescription (sample VIII) and the mixed sample of ephedrine alkaloids + glycyrrhizin + safflower flavonoids were superior to those of Yaotong Ning in vitro. However, The pain activity was not obvious. The anti-inflammatory and analgesic effects of the sample VIII mice were significantly better than those of Yaotongning, and the analgesic activities of the mice in the sample induced by acetic acid were better than aspirin. Conclusion Yaotongning decoction can be used as a new drug candidate for rheumatoid bone disease. To reduce the content of Prescriptions, effective components and the amount of Strychnos alkaloids in Yaotongning can improve the anti-inflammatory and analgesic activity, the safety and quality Controllability.