摘 要 I 复黄片的研究 摘 要 复黄片的研究 摘 要 痔疮是临床常见病和多发病，有“十人九痔”之说。中医药具有辨证施治、综合疗效好、毒副作用小等特点，在治疗痔疮方面发挥着重要作用。中药复方是中医治疗疾病的主要形式，其核心是通过药物间配伍达到减毒增效的目的。复黄片处方源于临床，是上海中医药大学附属龙华医院的协定处方。由该处方制成的医院制剂疗效确切，十多年的应用未见不良反应。为扩大应用范围、服务于广大患者，十分有必要进一步开发成新药，更好地满足临床需要。 本文是在安全有效的临床协定处方的基础上， 在中医药理论指导下，按照中药 6 类新药的要求进行临床前研究，主要内容包括制备工艺、质量标准、稳定性等药学研究和初步药效学研究。 本文采用药理、化学等指标研究了制备工艺，确定的制备工艺路线和条件如下：取四味药材，加水浸泡 0.5 小时，煎煮二次，每次 1小时，分别加水 12 倍量、10 倍量，煎液滤过，滤液合并，浓缩至相对密度为 1.051.10(5060)，加乙醇至含醇量为 70，冷藏过夜，取上清液减压回收乙醇至相对密度为 1.351.40(5060)，加入淀粉混匀，60以下真空干燥，粉碎成细粉，加适量 80%乙醇润湿，过 16 目筛制粒，80以下干燥，整粒，加入硬脂酸镁，混匀，压片，包薄膜衣，分装，即得。中试结果表明，该制备工艺合理、可行。 摘 要 II 根据复黄片的剂型特点及相关要求，进行了质量标准研究和制定。包括性状，香蒲新苷、槐角苷和大黄的鉴别，片重差异、崩解时限和微生物限度检查，香蒲新苷和槐角苷的含量测定。 采用加速实验和长期实验考察了复黄片的稳定性， 结果表明在考察期内样品各项质量检查指标均符合规定， 包装材料对样品亦无不良影响。 初步药效学试验结果表明， 研制的复黄片具有明显的抗炎作用和止血作用，对金黄色葡萄球菌、枯草芽孢杆菌、白色念珠菌、霉菌有较强的抑菌作用。 关键词：关键词：复黄片，痔疮，制备工艺，质量标准，稳定性，初步药效学 Abstract III STUDY ON FUHUANG TABLET ABSTRACT Hemorrhoid is the common and frequently-occurring disease in clinic. Traditional Chinese medicine (TCM) plays an important role in treating hemmorhoid with the characteristics of treating disease on the basis of symptom, good efficacy of long treatment and little toxicity. TCM compound recipe is the main form for the treatment of disease of Chinese Medicine. The key is to obtain the object of lowering toxicity and enhance efficacy through the drug compatibility. The prescription of Fuhuang Tablet is the concerted recipe of Longhua Hospital affiliated to Shanghai University of TCM and comes from clinic. Fuhuang Tablet is effective and no side effect was found in clinic for more than ten years. In order to enlarge the application scope and serve more people, it is necessary to further develop and satisfy the need of clinic better. In this dissertation, the preclinical research was performed on the basis of the safe and effective concerted prescription in clinic, under the guidance of TCM theory and the requirement of No.6 new drugs. This study mainly includes preparation techniques, quality standard, and stability, and primary pharmacodynamic research. In this dissertation, the preparation technique was studied with index of pharmacology and chemistry and the optimal routie and optimal conditions are as follows: Dried medicinal materials were ground into powder accurately weighed and dipped in 12 times of water for 30 min Abstract IV and then decocted for 1 h. The extraction was repeated in 10 times water. The extracted solution was combined and then concentrated by evaporation till the relative density was about 1.05-1.10 (50-60), then ethanol was added till the concentration of ethanol was 70%, laying aside and precipitation was appeared. The upper liquid was taken out and evaporated till the relative density was 1.35-1.40(50-60), then 0.1 times of the weight of the dry extract of starch was added and mixed uniformly, dried under vacuum, ground, screened, add magnesium stearate, mixed uniformly, pressed and coated. The results of the three batches of pilot study indicated the procedure is reasonable and applicable. The study and establishment of the quality standard was performed according to the characteristics and relative requirements of the preparation type of fuhuang tablet. The content of typhaneoside and sophoricoside was determined and the character, the weight diversity and other quality control criteria were also investigated. The stability of Fuhuang Tablet was investigated by acceleration and long term experiment. The results showed that all quality indexes are accorded with regulation and the package material has no side effect on samples. Primary pharmacological experiment showed that the Fuhuang Tablet prepared with the established method has distinct effects of anti- inflammation and hemostasis and it is also has the antibacterial effect of 治痔疮的药http:/www.315bed.com/痔疮药Abstract V staphylococcus aureus, bacillus subtilis, candida albicans and mildew. Keywords: Hemorrhoid, Fuhuang Tablet, preparation technique, quality standard, stability, preliminary pharmacology 治痔疮的药http:/www.315bed.com/痔疮药第一章 前言 1 一、 前 言 一、 前 言 肛肠痔瘘病俗称痔疮，是人类特有的常见病、多发病。痔疮(Hemorrhoid)是指由于各种因素导致的肛管直肠下段血管性衬垫组织的病理性增生或扩张1，它的主要症状是出血、脱出、疼痛、痉痒、嵌顿2。有关资料表明3，人群中包括有症状和无症状的痔的发生率高达 86%，男女皆可得病，任何年龄都可发病，其中 20-40 岁的人较为多见，并可随着年龄的增加而逐渐加重，故有“十人九痔”之说4-5。近年来,由于饮食结构及饮食习惯的改变，高热、辛辣、多油成为大部分国人的日常饮食口味，导致痔疮的发病率明显上升6-7。在第十届全国中医药肛肠学术会议上，有专家指出，我国肛肠疾病的发生率每年大约以 16%的速度上升8。普查资料显示，个别省的肛肠疾病病人己高达人群总数的 80%以上9。 现代医学将痔疮分为内痔、外痔和混合痔三种: (1)内痔。分三期：第期：无明显自觉症状，仅于排便时出现带血、滴血或喷血现象。肛门镜检查，在齿状线上可见粘膜呈结节状突起，第期：排便时间歇性带血、滴血或喷血，内痔脱出，便后可自行还纳。第期：大便时内痔脱出，或在劳累较甚、步行过久、咳嗽时脱出，内痔脱出后不能自行还纳，必需用手托入，或卧床休息后方可还纳。 (2)外痔。分四类：血栓性外痔：因肛门静脉丛发炎或排便时用力过猛，而致肛门静脉丛内有血栓形成，有皮下隆起疼痛者。静脉曲张性外痔：久蹲或作内痔吸引时，肛缘皮下肿胀，可见曲张的静脉团，不能立即消散者。结缔组织性外痔：因慢性炎症刺激，反复发作致肛缘局部皮肤纤维化，结缔组织增生形成皮垂者，也称赘皮外痔。炎性外痔：肛缘皮肤操作或感染后，形成肛门皮肤皱襞突起，呈红肿疼痛的炎性现象者。 (3)混合痔。由齿状线上下同一方位的直肠和肛门静脉丛扩张屈曲，相互吻合，括约肌间沟消失，使上下形成一整体者。 我国目前多数医家认为，痔的发生原因，有以下几个方面： (1)解剖学原因：人在站立或坐位时，肛门直肠位于下部，由于重力和脏器的压迫， 静脉向上回流颇受障碍。 直肠静脉及其分枝缺乏静脉瓣， 血液不易回流，治痔疮的药http:/www.315bed.com/痔疮药第一章