【作者】 全大勇；

【导师】 彭智聪；

【作者基本信息】 湖北中医学院 ， 中药学， 2004， 硕士

【摘要】 “回归平衡胶囊”是治疗儿童性早熟的中药复方制剂，本课题包括该药物的制剂工艺学研究、质量标准研究、稳定性研究、药效学研究、免疫学研究、毒理学研究。 在制剂学研究中，以制剂的口感、气味、外观、药效、毒性及稳定性作为评价指标，对其处方、剂型(设计了口服液与胶囊剂两个剂型)、日服剂量进行了实验筛选研究。我们就上述因素设计了若干方案，制备了大量样品，从中取得大量数据，然后约请院内同行帮助分析，比较。结果：口服液与胶囊剂疗效相近，但由于回归平衡胶囊处方中多为大苦之药，口服液很难为儿童所接受，最后选定胶囊剂。并用正交设计等统计学方法对煎煮提取过程中药材浸泡时间、煎煮时间、用水量、煎煮次数进行了优化选择。 一．质量标准研究 (1)鉴别 通过泡沫反应、显色反应，对处方中药物所含生物碱、皂苷，环烯醚萜苷等类成分进行鉴别；用薄层层析法对有关中药进行鉴别。 (2)浸出物测定 由于黄柏、龙胆两味药的主要有效成分明确，高效液相色谱中峰较易分离，阴性干扰小，故可以用本品中的小檗碱、龙胆苦苷含量来控制质量，本品中的小檗碱转化为盐酸小檗碱每粒含量不得少于4.20mg，龙胆苦苷每粒含量不得少于1.88mg。 二．稳定性试验 按《新药审批办法》的有关规定，对本品进行了三个月的连续考察，结果稳定性良好；用加速试验对药品进行稳定性试验，估算药品的有效期。 三．主要药效学试验结果 该制剂能显著降低白兔因性早熟引起的激素E2、PROG、TESTO、LH、FSH含量偏高，使其接近正常水平。 四．毒理学研究 (1)急性毒性试验 以儿童日服剂量的200倍量24h分次给小鼠灌胃，不引起死亡。 (2)长期毒性试验 以儿童日服剂量的100、50、10倍量分别给大鼠连续给药90天，其血象、肝功能、肾功能未发现有毒性作用，且未发现心、肝、肾、脑等生命器官有毒性损害，故示本品安全，可以长期服用。 总之，通过以上试验研究，使回归平衡胶囊的制备工艺、质量标准、稳定性、毒性等得以确定。同时将该药成研制为一种疗效可靠的、安全的、方便的治疗性早熟的中成药，填补此类药品的空白，从而发展成为一种新的中成药品种，造福社会，造福人类，发挥更好社会效益和经济效益。更多还原

【Abstract】 Huigui pingheng capsule is a compound preparation which can treat children sexual precocity .The main research contents on HuiGui Pingheng Capsule include technology of preparation, criteria of quality, the stability of the pharmaceuticals, the effect of medicine , the pharmacody and the toxicology.During the research of the technology of preparation the optimum prescribe, dosage and the dose of the preparation were studied by its taste, appearance, pharmacody , and stability(by comparing oral liquid with Capsules). We practiced several projects designed as the above factors and manufactured lots of samples, by which we got a great deal of data. In the same time specialist in our hospital were invited to help analysis and compare the drugs. The results showed that the effect of the oral liquid and capsule were almost no difference, but the oral liquid was so bitter that it was difficult to be accepted by children. At last we chose Capsules as the dosage .we selected total quantity of dry ointment and gentiopicrin as marker .utilizing L9(34) orthogonal test optimize the process of water-extraction and determined as following :decocted twice ,first ten times volume 2.5hr,then eight times volume 2hr ,combing and concentrated to 1.15g/ml .We chose spray-drying method to desiccate this ointment ,air-inlet temperature at 125℃, air-outlet temperature at 90 ℃ and pressure 0.7Mpa in drying tower.During the quality research preceedings , we identified Anemarrhena asphodeloides Bge and Eclipta prostrata L. by TCL(Thin Layer Chromatogragh )method ,which was special and accurate .The contents of berberine and gentiopicrin were determined by HPLC (High Performance Liquid Chromatograg) after the methodology was completed . The HPLC showed that the rate of recovery was up to standard and its precision, stability and reappearance were good. For the sake of inspecting primary stability of huigui pingheng capsule, the room-temperature and accelerating test were carried into execution, from which the results showed every index marker was normal .It indicated the quality of huigui pingheng capsule was steady and controllable.We carried out main Pharmacodynamical experiment ,in which special rabbits were used .The experiment shows that the preparation can reduce the rabbit levels of hormone E2. PROG, TESTO, LH, FSH and lead them to normal levels.To find out the toxicity of the drug we carried out the research of the toxicology which included the acute and chronic toxicity experiments. The result declared that the drug had little toxic reaction and could be taken for a long time.In a word, according to the above experiments, we made an acknowledge of the technology of preparation, criterion of quality, stability, pharmacodynamic and toxicity. Moreover, we succeeded in researching the effective safe and convenient patent drug, which would be a first new patent drug for sexual precocity in China. We rest assured that the drug would no only benefit our society and human being but also would have a good effect on the value of society and economic.更多还原