CN101141954A - 消化道促动力剂 - Google Patents
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Abstract
本发明提供一种促消化道动力作用显著、安全性高的药剂。本发明涉及一种含有氯化甲硫氨基酸的消化道促动力剂。该药剂可以作为具有显著药理作用而且没有副作用的优良的消化道促动力剂使用。
Description
技术领域
本发明涉及一种基于氯化甲硫氨基酸(methylmethionine sulfoniumchloride，MMSC)的新药效的消化道促动力剂。
背景技术
近年来，消化道运动功能下降被逐渐理解为能引起慢性胃炎、反流性食管炎、腹部不适或假性肠梗阻等各种胃肠障碍疾病中的一种。因此认识到含有能够促进消化道运动功能的药物的药剂，可以作为能够解除或缓解上述慢性胃炎等胃肠障碍的药剂即消化道促动力剂使用。
这种消化道促动力剂例如已知有西沙必利(非专利文献1、2)和甲氧氯普胺(非专利文献3、4)等。另外，己知生药成分苍术也具有这种促消化道动力作用(非专利文献5)。
但是，据报道甲氧氯普胺有抗多巴胺作用引起的锥体外系症状副作用、西沙必利有帕金森症状副作用，其它还有心室性脉律不齐、过敏症等副作用也得到确认。另外，苍术作为生药成分显示稳定的疗效，但是很难说其药理作用充分。
非专利文献1·Schuurkes，J.A.J.等，1985年，J.Pharmacol.Exp.Ther.，第234卷，第775页(日文原文：シュ一ルケスら、1985年、J.Pharmacol.Exp.Ther.，第234巻、第775頁)。
非专利文献2：Schuurkes，J.A.J.等，1984年，Gastrointestinal Motility，Roman，C.，第95页，MTP出版社，Lancaster(日文原文：シュ一ルケスら、1984年、Gastrointestinal Motility，Roman，C.、第95頁、MTPプレス、Lancaster)。
非专利文献3：福原武等：日平滑肌志，1966年，第2卷，第1号，第15页，[PP11038](日文原文：福原武ほか：日平滑筋誌、1966年、第2巻、第1号、第15頁、[PP11038])
非专利文献4：熊田重敦等：药学研究，1968年，第39卷、第2号、第44页、[PP11550](日文原文：熊田重敦ほか：薬学研究、1968年、第39巻、第2号、第44頁、[PP11550])
非专利文献5：第14改正日本药局方解说书，2001年，D-674～677页(日文原文：第14改正日本薬局方解説書、2001年、D-674～677頁)
发明内容
本发明的目的在于提供一种具有促消化道动力作用的新的药剂。
本发明人等意外地发现，作为胃粘膜修复剂已知的氯化甲硫氨基酸(MMSC)具有促消化道动力作用，从而完成了本发明。
即：本发明涉及一种含有MMSC的消化道促动力剂。另外，本发明还提供一种用于抑制嗳气、要吐、恶心、呕吐或解除胸闷、积食、消化不良、胃部·腹部胀满或食欲不振的、含有MMSC的消化道促动力剂。
本发明的消化道促动力剂与生药成分苍术相比，其药理作用显著优越。另一方面，没有报道MMSC具有抗多巴胺作用或者西沙必利及甲氧氯普胺出现的锥体外系症状、帕金森症状等中枢神经系统副作用及其它副作用等。因此，含有MMSC的药剂可以作为具有显著药理作用和高安全性的消化道促动力剂使用。
具体实施方式
MMSC是1959年开始上市的药剂，主要用作胃粘膜修复剂或改善慢性肝病的肝功能，但是，MMSC具有促消化道动力作用，因此可作为消化道促动力剂，关于这一点至今没有报道也没有表述。本发明提供MMSC的这种新用途。
本发明中使用的MMSC，例如可以使用米泽浜理药品工业(株式会社)(日文原文：米沢浜理薬品工業(株))的市售品，另外也可以使用根据特公昭36-13209号公报记载的方法合成的MMSC。
另外，本发明的消化道促动力剂，可以以MMSC单一的形式使用，或以含有医药上可接受的载体及其它医药成分、赋形剂、粘合剂、崩解剂、润滑剂、着色剂、矫味剂等的医药组合物的形式使用。
赋形剂例如有乳糖、淀粉类、结晶纤维素、蔗糖、甘露醇、轻质二氧化硅等。粘合剂例如有羟丙基甲基纤维素、羟丙基纤维素、明胶、α化淀粉、聚乙烯吡咯烷酮、聚乙烯醇、普鲁兰多糖等。崩解剂例如有羧甲基纤维素、羧甲基纤维素钙、交联羧甲基纤维素钠、交联聚维酮、玉米淀粉、低取代度羟丙基纤维素等。润滑剂例如有硬脂酸镁、滑石等。着色剂例如有焦油色素、三氧化二铁等。矫味剂例如有甜叶菊、阿斯巴甜、香料等。
本发明的消化道促动力剂，根据目的可以制备成散剂、颗粒剂、片剂、咀嚼片、薄膜包衣片、糖衣片、口服液、软胶囊剂、硬胶囊剂、凝胶剂等剂型使用。特别优选制备成散剂、颗粒剂、片剂、薄膜包衣片的剂型使用。
将MMSC作为消化道促动力剂使用时的给药量，与剂型、疾病程度、患者年龄等因素有依赖关系，通常成人给予MMSC30～3000mg/天，特别优选150～225mg/天。
本发明的消化道促动力剂如下述实施例中所示，具有提高肠道输送率的作用。因此，本发明的消化道促动力剂能够解除因肠内容物滞留引起的慢性胃炎、反流性食管炎、腹部不适或假性肠梗阻等各种症状。另外，本发明通过提高肠道输送率，可以有效抑制或解除因肠内容物滞留引起的嗳气、要吐、恶心、呕吐、胸闷、积食、消化不良、胃部·腹部胀满及食欲不振等症状，特别是由饮酒过量或进食过饱引起的这些症状。而且，通过提高肠道输送率、解除肠内容物滞留也可以促进消化。
下面通过药理试验例、制备例更具体地说明本发明，但是这些例子并不是对本发明的限制。
实施例1
根据下述试验方法，研究了受试物的肠道输送机能的效果。
试验前一天断食的5周龄ddY系雄性小鼠口服0.5％甲基纤维素(以下称MC)中悬浮的氯化甲硫氨基酸(1000mg/kg、3000mg/kg)，15分钟后，口服活性炭末悬浊液。再于30分钟后颈椎脱臼处死动物，摘除幽门部至回盲部的肠管。受试物的肠道输送机能用自幽门部的炭末的移动距离除以肠管全长得到的肠道输送率表示。另外，用苍术干燥浸膏S(300mg/kg、相当于原生药3000mg/kg)进行了同样的试验。试验结果如表1所示。
表1
| 组 | 用量(mg/kg) | 移动率(％) | |
| 平均值±标准误差 | 比率 | ||
| 对照组MMSCMMSC苍术 | 100030003000 | 56.6±2.873.4±4.3*86.6±4.6*53.0±3.1 | 1.0001.2971.5300.936 |
N＝6
*相对于对照组，p＜0.05(Williams多重比较)
由上述可以确认：通过给予MMSC可提高肠道输送率，并具有用量依赖性的促消化道动力作用。
Claims (5)
1.一种含有氯化甲硫氨基酸的消化道促动力剂。
2.如权利要求1所述的消化道促动力剂，其中所述药剂用于抑制嗳气、要吐、恶心、呕吐或解除胸闷、积食、消化不良、胃部·腹部胀满或食欲不振。
3.如权利要求2所述的消化道促动力剂，其中所述的嗳气、要吐、恶心、呕吐、胸闷、积食、消化不良、胃部·腹部胀满及食欲不振由饮酒过量或进食过饱引起。
4.如权利要求1所述的消化道促动力剂，其中所述药剂用于解除腹部不适或假性肠梗阻。
5.如权利要求1所述的消化道促动力剂，其中所述药剂用于促进消化。
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2005127046 | 2005-04-25 | ||
| JP127046/2005 | 2005-04-25 |
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| Publication Number | Publication Date |
|---|---|
| CN101141954A true CN101141954A (zh) | 2008-03-12 |
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| CNA2006800087441A Pending CN101141954A (zh) | 2005-04-25 | 2006-04-24 | 消化道促动力剂 |
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| JP (1) | JPWO2006115238A1 (zh) |
| KR (1) | KR20080003318A (zh) |
| CN (1) | CN101141954A (zh) |
| WO (1) | WO2006115238A1 (zh) |
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| KR101100901B1 (ko) * | 2009-04-09 | 2012-01-02 | 주식회사 씨티네트웍스 | 광섬유의 어댑터 연결부위에서 광신호 유무를 확인하는 센싱 어댑터 |
| JP2015214530A (ja) * | 2013-07-31 | 2015-12-03 | 興和株式会社 | 胃腸薬組成物 |
| US10509185B2 (en) | 2016-04-27 | 2019-12-17 | Huawei Technologies Co., Ltd. | Optical connector with photodetector, adaptor for optical connector, and system |
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| JPH08259445A (ja) * | 1995-01-27 | 1996-10-08 | Takeda Chem Ind Ltd | 胃排出能改善性医薬組成物 |
| JP4627574B2 (ja) * | 1999-05-18 | 2011-02-09 | 進 黒澤 | 消化管運動改善剤 |
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- 2006-04-24 CN CNA2006800087441A patent/CN101141954A/zh active Pending
- 2006-04-24 WO PCT/JP2006/308514 patent/WO2006115238A1/ja active Application Filing
- 2006-04-24 JP JP2007514704A patent/JPWO2006115238A1/ja active Pending
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| Publication number | Publication date |
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| WO2006115238A1 (ja) | 2006-11-02 |
| KR20080003318A (ko) | 2008-01-07 |
| JPWO2006115238A1 (ja) | 2008-12-18 |
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