CN1236792C - 防治脑病和益智的脑活性作用物质及其制备方法 - Google Patents

防治脑病和益智的脑活性作用物质及其制备方法 Download PDF

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CN1236792C
CN1236792C CNB021422583A CN02142258A CN1236792C CN 1236792 C CN1236792 C CN 1236792C CN B021422583 A CNB021422583 A CN B021422583A CN 02142258 A CN02142258 A CN 02142258A CN 1236792 C CN1236792 C CN 1236792C
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Abstract

本发明公开了一种防治脑病和益智的脑活性作用物质，可以制作防治脑老化和脑血管病，增进智力，治疗夜尿，遗尿，失禁和弱智，老年痴呆，帕金森症等由于脑功能不健全或障碍所引起的病症的保健品或药物，并可防止关节炎，血管硬化，血液循环病，风湿病，雷诺氏综合症等，且疗效显著。其特征在于所述脑活性作用物质为文冠果的果壳(包括果柄)的提取物。本发明还公开另一种防治脑病和益智脑活性作用物质，其特征在于所述脑活性作用物质为文冠果的果壳(包括果柄)的粗皂甙提取物。这两种脑活性作用物质可以调解和改善脑神经系统功能；本发明也公开了这两种提取物的制备方法。

Description

防治脑病和益智的脑活性作用物质及其制备方法
技术领域：
本发明涉及两种脑活性作用植物提取物，一种是文冠果果壳的醇提取物，另一种是文冠果果壳的粗皂甙。同时，本发明还涉及该两种物质的制备方法。
背景技术：
文冠果是无患子科(Sapindaceae)文冠果属(Xanthoceras)的植物，拉丁文名Xanthoceras sorbifolia Bunge，俗名又叫文冠花，文光果，文冠树，文官果，崖木瓜和西拉森登等。落叶灌木或小乔木，可达8米高；奇数羽状复叶；总状花序，花白色，杂性；蒴果绿色，果壳厚，木质，成熟黑褐色开裂成三瓣，种子黑褐色，卵球形，多数。仅产于中国，主要分布于中国北部，野生或栽培。种子含油脂可达50％以上，可食用。茎叶可入药，治风湿。种子在民间用于治遗尿症。
本发明的目的在于提供两种从文冠果果壳(包括果柄)提取的脑活性作用物质。
发明内容：
本发明所提供的脑活性作用物质，可以调解和改善脑神经系统功能，对防治脑老化和脑血管病，增进记忆和开发智力，治疗夜尿，遗尿，失禁，尿频和弱智，老年痴呆，帕金森症等由于脑功能不健全或障碍所引起的病症都有显著效果。其特征在于所述脑活性作用物质为文冠果的果壳(包括果柄)的提取物。
其中之一为文冠果的果壳(包括果柄)的醇类等有机溶剂提取物，主要含有皂甙和其它物质，具体含量如下：
皂甙   糖      粗蛋白   水     粗脂肪   其它
30-32  15-25   8-14     7-10   1-4      余
生产依下列步骤进行：
●采收文冠果，清选果壳，干燥；
●粉碎文冠果果壳；
●醇类等有机溶剂浸提文冠果果壳粉；
●回收溶剂，浓缩得流浸膏；
●干燥，灭菌得醇等有机溶剂提取物；
文冠果醇等有机溶剂提取物可制成各种剂型的调解和改善脑神经系统功能的药物。该药物对遗尿症的疗效总有效率高于当前同类药物中任何一种，是目前最有效的首选药物。同时，它还可防治脑老化和脑血管病，增进记忆和开发智力，治疗尿频，遗尿，失禁，痴呆，弱智，帕金森症等由于脑功能不健全或障碍所引起的其它病症和防治关节炎，血管硬化，血液循环病，风湿病，雷諾氏綜合症等。
本发明提供的提取物是文冠果果壳的醇等有机溶剂提取物，和中科药业公司生产的文冠果果仁霜(遗尿停原料药)及其醇提取物都不同。它的文冠果皂甙的含量(30-32％)大大高于文冠果果仁霜(2-4％)，也高于其醇提取物(12-19％，见表一)。因此，用本发明提供的提取物做原料制备的同类药物治疗遗尿症，不仅效果好而且服用量仅是遗尿停的六分之一，即一天三次，一次一粒。方便了病人，减少了病人服药的痛苦，特别是儿童。同时，制备方法也比生产果仁霜的醇提取物工艺简便，仅五步工艺省工省料，而生产果仁霜的醇提取物至少要十步以上：1)采收文冠果，清选种子，干燥；2)剥壳得到种仁；3)轧油得种仁饼；4)干燥，粉碎种仁饼得种仁粉；5)用有机溶剂提取种仁粉进一步去油；6)回收有机溶剂；7)干燥，磨粉得果仁霜；8)溶乙醇提取果仁霜；9)回收乙醇；10)干燥，灭菌得果仁霜的醇提取物。况且，本发明提供的提取物用文冠果果壳为原料，文冠果果壳现在仅被做为燃料烧掉，成本和果仁霜原料的种子相比，减少很多，因此，整个生产成本减少了60％以上。
表1文冠果果壳的提取物和果仁霜及其醇提取物的比较
    皂甙    糖    粗蛋白    水    粗脂肪  其它
A  30-32  15-25   8-14     7-10    1-4     余
B  10-19  20-30   15-20    10-15   1-10    余
C  2-4     -      55-65    7-16    1-10    余
A：果壳的醇提取物；B：果仁霜的醇提取物；C：果仁霜
同时，本发明还提供了另外一种调解和改善脑神经系统功能的脑活性作用物质，其特征在于所述脑活性作用物质为文冠果的果壳(包括果柄)的粗皂甙提取物。
工艺过程如下：
●采收文冠果，清选果壳，干燥；
●粉碎文冠果果壳；
●醇类等有机溶剂浸提文冠果果壳粉，按有机溶剂∶果壳粉2∶1的比例，在室温下，浸提4-5次，每次20-35小时；
●收集浸提液，再回流热提(80℃)2-3次；
●收集合并提取液；
●脱去溶剂，得流浸膏；
●干燥，灭菌，得乙醇提取物，；
●流浸膏再用水溶解，正丁醇萃取；
●正丁醇萃取物经色谱分离得粗皂甙。
所得粗皂甙可制成各种剂型药物和保健品，或与文冠果的醇提物配伍用于调解和改善脑神经系统功能，它还可防治脑老化和脑血管病，增进记忆和开发智力，治疗尿频，遗尿，失禁，和痴呆，弱智，帕金森症等由于脑功能不健全或障碍所引起的其它病症和防治关节炎，血管硬化，血液循环病，风湿病，雷諾氏綜合症等。文冠果果壳粗皂甙是文冠果果壳醇提取物的进一步精制物，含有更多的皂甙(50％以上)，因而在制备药物和应用方面会比醇提取物更为优越。
本发明是以文冠果果壳为原料的植物提取物，是目前最好的治疗夜尿的药物，经毒理，药理试验，无任何毒副作用。制备工艺方便，皂甙收率高，而且成本低。下面通过实施例做进一步说明。
具体实施方式：
实施例1
本实例说明文冠果果壳醇提取物的制备方法：
●采收文冠果，清选果壳，干燥，粉碎，得10kg果壳粉；
●按乙醇∶果壳粉2∶1的比例，用20升乙醇浸提4-5次，每次20-35小时；
●收集浸提液，再回流热提(80℃)2-3次，收集合并提取液；
●脱去溶剂，得流浸膏；
●干燥，灭菌，得乙醇提取物140.5g，组成部分为：
  皂甙    糖     粗蛋白   水     粗脂肪   其它
  31.3    17.2   11.6     9.4    3.9      26.6
实施例2
将实施例1所述乙醇提取物量50g软化，过筛制粒，装2号胶囊250粒，，三十粒一瓶。本胶囊可用于治疗遗尿症和其它由于脑功能不健全或障碍所引起的病症。治疗遗尿症，小儿每日三次，每次一粒，十五日一疗程，一至三疗程。
实施例3
将实施例1所述乙醇提取物量50g，过筛制成粉状，加葡萄糖粉450g混均，制粒，干燥，装2.0g袋250袋，即为一种治疗遗尿症和其它由于脑功能不健全或障碍所引起的病症的颗粒剂。治疗遗尿症，小儿每日三次，每次一袋，十五日一疗程，一至三疗程。
实施例4
将实施例1所述乙醇提取物量40g，过筛制成粉，加0.8g干淀粉，0.4g滑石粉和少许乙醇，混匀，压片，灭菌，制成200g片，即为一种治疗遗尿症和其它由于脑功能不健全或障碍所引起的病症的片剂。治疗遗尿症，小儿每日三次，每次一片，十五日一疗程，一至三疗程。
实施例5
本实例说明文冠果果壳粗皂甙的制备方法：
●采收文冠果，清选果壳，干燥，粉碎，得20kg果壳粉；
●按乙醇∶果壳粉2∶1的比例，用10升乙醇浸提4-5次，每次20-35小时；
●收集浸提液，再回流热提(80℃)2-3次，收集合并提取液；
●脱去溶剂，得流浸膏；
●干燥，灭菌，得乙醇提取物281.5g；
●流浸膏再用水溶解，正丁醇萃取；
●正丁醇萃取物再用水溶解，正丁醇提取，得正丁醇提取物；
●正丁醇提取物经液滴逆流色谱得21.6g粗皂甙。
实施例6
将实施例5所述乙醇提取物量9.0g，加入适量干淀粉，滑石粉和少许乙醇，混匀，压片，灭菌，制成200mg片250g片，即为一种治疗遗尿症和其它由于脑功能不健全或障碍所引起的病症的片剂。治疗遗尿症，小儿每日三次，每次一片，十五日一疗程，一至三疗程。
实施例7
将实施例5所述皂甙9.0g，装2号胶囊250粒，三十粒一瓶。本胶囊可用于治疗遗尿症和其它由于脑功能不健全或障碍所引起的病症。治疗遗尿症，小儿每日三次，每次一粒，十五日一疗程，一至三疗程。
附图说明：
图1为皂甙A、B、C、D结构图
其中R      R1     R2     R3      R4       R5
    H      H       H       乙酰基    当归基    乙酰基    皂甙A
    H      H       H       乙酰基    当归基    当归基    皂甙B
    H      H       乙酰基   H        当归基    乙酰基    皂甙C
    H      H       乙酰基   H        当归基    当归基    皂甙D

Claims (12)

1.一种脑活性作用物质，其特征是，该物质是用文冠果的果壳和/或果柄制备的醇提取物；含有如下物质：
总甙   糖      粗蛋白    水     粗脂肪  其它
30-32  15-25   8-14      7-10   1-4     余
2.一种生产权利要求1的脑活性作用物质的制备方法，其特征是，依下列步骤：
·采集文冠果，清洗果壳，干燥；
·粉碎文冠果果壳；
·醇类有机溶剂浸提文冠果果壳；
·回收溶剂得流浸膏；
·干燥，灭菌得醇有机溶剂提取物；
其中醇类有机溶剂浸提文冠果果壳步骤中，所述醇类有机溶剂是乙醇或甲醇；使用的醇类有机溶剂与果壳粉的重量比为2∶1；浸提次数为4-5次，每次20-35小时；
所述回收溶剂得流浸膏的步骤，包括收集浸提液，80℃下回流热提2-3次，收集合并提取液的步骤。
3.权利要求2的制备方法，其特征是，所述采集文冠果是每年的8-10月间采收。
4.权利要求2的制备方法，其特征是，是在室温下进行。
5.权利要求1所述的物质，其特征是，含有30％以上文冠果皂甙。
6.权利要求1所述的物质，其特征是，是文冠果果壳的醇提取物。
7.权利要求1所述的物质在制备治疗遗尿症和其它由于脑功能不健全或障碍所引起的病症的保健品或药物中的应用。
8.以权利要求1所述的物质为活性成分的药物制剂。
9.一种脑活性作用物质，其特征是，该物质是用文冠果的果壳和/或果柄提取的粗皂甙提取物，含有50％以上的文冠果皂甙。
10.一种权利要求9所述物质的制备方法，其特征是，依下列步骤：
·采改文冠果，清洗果壳，干燥；
·粉碎文冠果果壳；
·用乙醇浸提文冠果果壳粉，按乙醇∶果壳粉2∶1的比例，在室温下，浸提4-5次，每次20-35小时；
·收集浸提液，再回流80℃热提2-3次；
·收集合并提取液；
·脱去溶剂，得流浸膏；
·干燥，灭菌，得醇取物；
·流浸膏再用水溶解，正丁醇萃取；
·正丁醇萃取物经色谱分离得粗皂甙。
11.权利要求9所述的物质在制备治疗遗尿症和其它由于脑功能不健全或障碍所引起的病症的保健品或药物中的应用。
12.以权利要求9所述的物质为活性成分的药物制剂。
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