【作者】 吴凌；

【导师】 滕利荣； 逯家辉；

【作者基本信息】 吉林大学 ， 微生物与生化药学， 2011， 硕士

【摘要】 疼痛是临床常见病症,如何更好地控制疼痛,始终是医学界面临的一项重要课题。临床上常用的阿片类镇痛药虽然镇痛效果好,但具有依赖性。因此人们致力于寻找无成瘾性的镇痛良药。鼠妇和徐长卿作为我国传统中药,其镇痛作用早已被许多文献报导过,民间也多有用水煎剂治疗疼痛的先例。为了充分利用我国宝贵中药资源,将传统中医药资源与现代化生产工艺充分结合,本文在总结现有临床研究及民间用药研究的基础上,对鼠妇、徐长卿的提取工艺、药效学、安全性、制剂工艺、质量标准和稳定性进行了研究。本实验运用中心组合实验及响应面法对鼠妇和徐长卿中镇痛活性成分的提取工艺进行了优化；确定了复方鼠妇镇痛片剂的处方和制备工艺并建立了质量标准；通过对小鼠最大给药量试验和长期毒性试验对镇痛片剂的安全性了进行探索；利用小鼠扭体试验、热板试验和甩尾试验对镇痛片剂的药效学作用进行了考察；通过长期稳定性试验、加速试验和影响因素试验对片剂的稳定性进行了研究,为以后的临床用药和生产提供了依据。更多还原

【Abstract】 Pain and inflammation are associated with concomitant symptom of many diseases, which bother countless patients in the world every year. At present, there are two major categories of analgesic widely used in clinic. One is nervous analgesic, which easily leads to addiction after a long-term continuous application. The other is a antalgic, antipyretic, and anti-inflammatory non-steroidal drug. Long-term use of this analgesic could easily causes adverse reactions to digestive and cardiovascular systems. Therefore, if we can develop a curative effect, less toxic side effects of analgesic drug for the treatment of pain will have a profound impact.To take full advantage of our precious traditional Chinese medicine resources, in the premise of assurancing Chinese medical scientific theories and characteristics, features and advantages of clinical application, we should inherit and carry forward. In this paper, based on summary of the previous theoretical and experimental researches, and by using the advanced modern pharmaceutical science and technology, the extraction process of Armadillidiam Vulgare and Paniculate Swallowwort root, pharmacodynamics and preparation process were studied.Choose water as the extraction solvent with the mouse acetic acid writhing test. According to the central composite experimental design theory, response surface method on Armadillidiam Vulgare and Paniculate Swallowwort root dose were optimized to determine the optimal analgesic effect. Under these conditions, analgesia rate of extracts was 52.6 percent. The model is very nicety.Using response surface analysis Armadillidiam Vulgare and Paniculate Swallowwort root extraction of active ingredients conditions were optimized. Set three single factors:extraction temperature, extraction time and ratio of water to sample. with the mouse acetic acid writhing test the analgesic effect of the extract. According to single factor test results. According to Box-Benhnken the central composite experimental design theory, response surface method in the three factors and three levels on Armadillidiam Vulgare and Paniculate Swallowwort root extraction conditions were optimized to determine the optimal extraction conditions: extraction temperature 100℃, extraction time 45min, ratio of water to sample (g/ml) 10:1. Under these conditions, analgesia rate of extracts was 55.1 percent.Filler and adhesive were screened with tablet appearance, tablet weight variation, hardness and disintegration time are evaluated. Ultimately determine the prescription. Every 3000 tablets, Armadillidiam Vulgare 7000g, Paniculate Swallowwort root 5400g, starch 1240g, magnesium stearate 2.5g, talcum powder 2.5g, adhesive 80% ethanol. Each of the tablets is 0.5g.The establishments of quality standards were established, including tablet character, tablet weight variation, hardness and disintegration time. Using colorimetric and HPLC to obtained the total sterol and paeonolum content of the tablets. The methodological study was also investigated, including method linearity, precision, reproducibility, and recovery. The results showed that this method is accurate, effective, and can be applied to the preparation of quality control.Pharmacodynamics and toxicity of the tablets were studied. The result of pharmacodynamics showed that the analgesia effect of the tablets is very good. In acetic acid writhing in mice, mouse hot plate and thermal stimulation in mice flick method, the analgesia effect of the tablets is better than yuanhu analgesia tablets in high and middle dose. In maximum amount toxicity test and long-term toxicity test, the animals didn’t show any toxic reaction or abnormal, indicating the toxicity of the analgesia tablets is small, and safe to use.Useing room temperature test, accelerated test and influencing factor test to study items of character, weight difference, hardness, disintegration time, content and microbial limit. The result showed the tablets had good stability.更多还原