CN104257704B - 东革阿里提取物的新用途 - Google Patents
东革阿里提取物的新用途 Download PDFInfo
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- CN104257704B CN104257704B CN201410475535.4A CN201410475535A CN104257704B CN 104257704 B CN104257704 B CN 104257704B CN 201410475535 A CN201410475535 A CN 201410475535A CN 104257704 B CN104257704 B CN 104257704B
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Abstract
本发明涉及医药化学领域，具体地，涉及东革阿里提取物在治疗咳嗽方面的用途。
Description
技术领域
本发明涉及医药化学领域，具体地，涉及东革阿里提取物在治疗咳嗽方面的用途。
背景技术
东革阿里是生长在东南亚靠近赤道的原始热带雨林中潮湿砂质土壤里的一种野生灌木植物，为苦木科Eurycoma属直属，主要分布在马来西亚、泰国等国家。成熟期一般为5年以上。树高4-6米，最高可达12米，树干直径8-10厘米，最粗可达15厘米。东革阿里的根部有多种功效，与燕窝、锡器一起并称为马来西亚三大国宝。研究显示，东革阿里根部(特别是芯)包含许多植物化学药物，它能增进睾酮的产量，睾酮是男性性功能所需的荷尔蒙，也是生殖器官和脑部发育所需的激素。
目前对东革阿里已开展了多方面的研究，研究结果显示东革阿里对于保健肾脏、增强免疫力、促进生育、治疗前列腺炎、抗疟疾等具有良好的效果。
英国日刊体育医学报告说，tongkatali(东革阿里)精华的作用在五个星期内提高了5％的肌肉质量，这个结果是从一个双盲对照科学试验治疗组上得出的，而且在对照组中没有发现任何明显的副作用。
从动物试验看，也证实了东革阿里可有效地促进睾酮的产生，增幅最高可达440％。人体试验表明，DHEA(一种雄性激素)水平从服用一周后的26％增长到服用三周后的47％，而SHBG(性激素结合球蛋白)水平在服用一周后下降36％，三周后下降66％。结果是，当SHBG下降时，绝大部分试验者的“游离睾酮指数”上升。“游离睾酮指数”的上升意味着它对睾酮的产生具有生物促进(非药物促进)的作用。
研究发现，阿里能改善精子的质量，提高精子数量、大小和移动速度。在实验室的白鼠试验中，服用的雌鼠产的小崽的体积比不服用的雌鼠产的小崽体积增加了一倍。研究人员推测这可能是雌鼠卵子分裂、双生和多次排卵引起的。他们从实验中得出的结论是更强的生育能力完全是精子数量和质量提高的结果。另外，阿里对提高生殖力的效果也非常明显，在动物实验中，雄性后代比雌性后代的提高了3倍。
由马来西亚政府资助的一个研究机构和美国麻省理工学院联合进行的研究发现，阿里含有强效抗癌和抗HⅣ(艾滋病)的成分。根据马来西亚森林研究所所长AbdulRazakMohdAli所说，它中的化学成分比现有的抗癌药更为有效。此外，其它实验还证明它所含的Auassinoid化学成分可以抗肿瘤和抗发热。
在本发明之前，现有技术中关于东革阿里的研究都集中在上述诸多方面，从未有研究关注东革阿里对于治疗咳嗽的效果。
肺系疾患的主要证候之一就是咳嗽。纵观历史，历代医家对于咳嗽都有不同见解。《黄帝内经》提出“五脏六腑皆令人咳，非独肺也”的论证。《景岳全书》又论“咳嗽一证，窃见诸家立论大繁，皆不得其要，多致后人临证莫知所从，所以治难得效”。张景岳将咳嗽证由分为外感、内伤两类。《河间六书》中又提及“寒暑燥湿风火六气，皆令人咳”。咳嗽既是病又是证候，任何年龄均可发病，冬春季节多见。咳嗽的病因有外感、内伤之别，风、寒、暑、湿、燥、火六淫之邪侵袭肺系引起的咳嗽，为外感咳嗽，外邪中又以风、寒、热咳嗽居多，并常以风为先号，挟寒或挟热、挟燥犯肺，发生风寒或风热、风燥等咳嗽；由于肺脏亏虚与其他脏腑功能失调影响到肺而引起的咳嗽，为内伤咳嗽。临床上常内伤、外感咳嗽互见并互为因果。正如《医学心语·咳嗽》所说：“肺体属金，譬若钟然，钟非叩不鸣，风寒暑湿燥火六淫之邪自外击之则鸣，劳欲情志，饮食炙煿之火自内攻之则亦鸣”。
咳嗽以八纲辨证为纲，首辨外感与内伤，以外感咳嗽多见，以宣发肺气为基本原则。汪受传将小儿外感咳嗽分为风寒和风热两大证型，韩新民将其分为风寒、风热和风燥三大证型，其中风寒咳嗽以疏风散寒、宣肺止咳为治法，以金沸草散加减；风热咳嗽以疏散风热、宣肺止咳为治法，以桑菊饮加减；风燥咳嗽以疏风清肺、润肺止咳为治法，以清燥救肺汤加减。钟华等则依据小儿体质辨治外感咳嗽，将其分为四型即正常质儿、痰湿质儿、气虚质儿和阴虚质儿，正常质儿以疏散外邪、宣肺止咳为治法，以杏苏散、桑菊饮及麻杏石膏汤等为主方；痰湿质儿以健脾燥湿、化痰止咳为治法，以麻杏二陈汤为主方；气虚质儿以疏风宣肺、化痰止咳、佐以健脾益气为治法，在风寒或风热基本方上酌情加用白术、黄芪等益气药，或六君子汤加射干、鱼腥草、连翘、桔梗等。
CN102078558A公开了一种治疗咳嗽的药物组合物，其中原料药的重量配比如下：钩藤30份，天竺黄40份，桔梗10份，砂仁50份，陈皮50份，茯苓10份，薄荷50份，甘草20份，牛黄7份。
发明概述
本申请发明人长期从事对东革阿里提取物药理活性方面的研究，出人意料地发现，东革阿里提取物对于治疗咳嗽具有良好效果。在本发明之前，从未有文献报道过东革阿里这方面的用途。
东革阿里中的化学成分有多种，根据《东革阿里化学成分的分离与鉴定》(张毅等，沈阳药科大学学报，第31卷第1其，2014年1月，第9-12页)记载，可以从东革阿里中分离多种化学成分，包括东莨菪素、9-甲氧基-铁屎米-6-酮、eurylene等。该文献在此全文引入作为说明书的一部分。
本发明的一个方面，提供了一种药物，其中包括东革阿里提取物。
本发明的另一个方面，提供了一种药物，其中东革阿里提取物包括东莨菪素、9-甲氧基-铁屎米-6-酮、eurylene等。
本发明的另一个方面，提供了一种药物，其中东革阿里提取物是东莨菪素。
本发明的另一个方面，提供了东革阿里提取物在制备治疗咳嗽的药物中的用途。
本发明的另一个方面，提供了东莨菪素在制备治疗咳嗽的药物中的用途。
本发明的另一个方面，提供了9-甲氧基-铁屎米-6-酮在制备治疗咳嗽的药物中的用途。
本发明的另一个方面，提供了eurylene在制备治疗咳嗽的药物中的用途。
本发明的另一个方面，提供了东革阿里提取物的制备方法，包括如下步骤：将东革阿里的根洗净、晾干、切碎，放入容器中，加冷水漫过药面，浸泡15～20分钟，再加水没过药面约8厘米，进行煎煮。未沸前采用武火煎煮，沸后用文火煎煮20～30分钟；第二次煎煮，水沸后文火煎煮15～20分钟。两次煎煮去渣取汁，合并。
本发明的另一个方面，上述容器包括但不限于铝锅、陶器、砂锅、玻璃器皿等。
本发明的另一个方面，接受治疗的患者包括哺乳动物和鸟类。
本发明的另一个方面，接受治疗的患者是人。
本发明的另一个方面，东革阿里提取物、东莨菪素、9-甲氧基-铁屎米-6-酮、eurylene在治疗咳嗽时对接受治疗的患者的给药量受多种条件限制，包括但不限于患者的年龄、性别、体重、疾病类型、疾病严重程度等。具体给药量是本领域技术人员根据其专业知识可以确定的。
本发明所述药物可以是本领域已知的任何药剂形式，包括但不限于片剂、胶囊、滴丸、注射液、冻干粉针、汤剂、缓释制剂、散剂、颗粒剂、栓剂、气雾剂等。
本发明制备药物制剂采用本领域已知的药物辅料，包括粘合剂、填充剂、润滑剂、稀释剂、溶剂、缓释材料等。包括但不限于淀粉、糊精、乳糖、甘露醇、微晶纤维素、羟丙甲纤维素、聚维酮、交联羧甲基纤维素钠、滑石粉、硬脂酸、泊洛沙姆、乙基纤维素、丙烯酸树脂等。
具体实施方式
实施例1
东革阿里提取物的制备
将东革阿里的根洗净、晾干、切碎，取100g放入容器中，加冷水漫过药面，浸泡15～20分钟，再加水没过药面约8厘米，进行煎煮。未沸前采用武火煎煮，沸后用文火煎煮20～30分钟；第二次煎煮，水沸后文火煎煮15～20分钟。两次煎煮去渣取汁，合并。
实施例2
东莨菪素片剂处方
实施例3
eurylene颗粒处方
实施例4
对二氧化硫烟雾致小鼠咳嗽模型的镇咳作用
将18-22g的小鼠随机分为5组，每组15只。模型对照组给予灌胃生理盐水，受试组给予灌胃样品1-3，阳性对照组给予右美沙芬，连续给药7天。于末次给药后30分钟，将小鼠置密闭玻璃箱内，定量喷入硫磺燃烧生成的烟雾诱导致咳，记录小鼠咳嗽潜伏期和3分钟内咳嗽次数。实验结果如表1所示。
样品1：实施例1东革阿里提取物
样品2：东莨菪素
样品3：eurylene
表1本发明药物样品对二氧化硫烟雾致小鼠咳嗽的镇咳作用(n＝15)
结果表明本发明药物有明显镇咳作用。
实施例3临床治疗效果：
疗效标准：疗效判断主要依据为咳嗽症状是否消失。用药15天为1个疗程。具体疗效分以下三级：
治愈——咳嗽症状全部消失，计算为治愈率；
好转——咳嗽症状明显减轻，计算为有效率；
无效——用药1个疗程后，咳嗽症状毫无消失，计算为无效率。
效果：用本发明药物和空白对照治疗咳嗽患者200例，分为4组，每组50例。治疗1个疗程，具体结果如下表2。
咳嗽模型组空白给药，受试组给予样品1-3
样品1：实施例1东革阿里提取物，给药量1.0g/kg
样品2：东莨菪素，给药量0.2mg/kg
样品3：eurylene，给药量0.2mg/kg
表2.
典型病例：
刘某，女，60岁，农民。2011年4月就诊。患者自述，犯咳嗽病已有十日有余。症状咳嗽气短，咯痰粘黄，咽痛，微恶风寒。苔薄白，舌尖红，脉浮数。采用本发明实施例1药物，先服10天，症状明显好转，后续服5天，痊愈。2个月追访，未见复发。
张某，男，47岁，公务员。2011年10月就诊，慢性咽炎引发咳嗽。采用本发明实施例2药物，2天症状明显好转，后续用药3天，痊愈。
Claims (2)
1.eurylene在制备治疗咳嗽的药物中的用途。
2.如权利要求1所述的用途，其中药物的药剂形式包括片剂、胶囊、滴丸、注射液、冻干粉针、汤剂、缓释制剂、散剂、颗粒剂、栓剂、气雾剂。
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| CN105557952A (zh) * | 2016-01-26 | 2016-05-11 | 廖丽萍 | 一种东革阿里保健饼干及其制备方法 |
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