WO2006115238A1 - Gastrointestinal motor activation regulator - Google Patents
Gastrointestinal motor activation regulator Download PDFInfo
- Publication number
- WO2006115238A1 WO2006115238A1 PCT/JP2006/308514 JP2006308514W WO2006115238A1 WO 2006115238 A1 WO2006115238 A1 WO 2006115238A1 JP 2006308514 W JP2006308514 W JP 2006308514W WO 2006115238 A1 WO2006115238 A1 WO 2006115238A1
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- WO
- WIPO (PCT)
- Prior art keywords
- gastrointestinal motility
- regulator
- activation regulator
- activation
- motor activation
- Prior art date
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- 230000004913 activation Effects 0.000 title claims abstract description 22
- 230000002496 gastric effect Effects 0.000 title abstract description 7
- 230000005176 gastrointestinal motility Effects 0.000 claims description 23
- 230000001105 regulatory effect Effects 0.000 claims description 5
- 206010000060 Abdominal distension Diseases 0.000 claims description 4
- 206010015137 Eructation Diseases 0.000 claims description 4
- 206010028813 Nausea Diseases 0.000 claims description 4
- 206010047700 Vomiting Diseases 0.000 claims description 4
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- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims description 3
- YDBYJHTYSHBBAU-YFKPBYRVSA-N S-methyl-L-methioninate Chemical compound C[S+](C)CC[C@H](N)C([O-])=O YDBYJHTYSHBBAU-YFKPBYRVSA-N 0.000 claims description 3
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- 230000000694 effects Effects 0.000 abstract description 7
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- MYGVPKMVGSXPCQ-JEDNCBNOSA-N Methylmethionine sulfonium salt Chemical compound [Cl-].C[S+](C)CC[C@H](N)C(O)=O MYGVPKMVGSXPCQ-JEDNCBNOSA-N 0.000 abstract 1
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- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
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- JEIPFZHSYJVQDO-UHFFFAOYSA-N iron(III) oxide Inorganic materials O=[Fe]O[Fe]=O JEIPFZHSYJVQDO-UHFFFAOYSA-N 0.000 description 1
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- 230000004899 motility Effects 0.000 description 1
- 230000007659 motor function Effects 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
Definitions
- the present invention relates to a gastrointestinal motility activation regulator based on a new medicinal effect of methylmethionine sulfo-um chloride (MMSC).
- MMSC methylmethionine sulfo-um chloride
- a decrease in the motor function of the gastrointestinal tract has been understood and recognized as a type of disease that causes various gastrointestinal disorders such as chronic gastritis, reflux esophagitis, abdominal indefinite complaints or pseudo-intestinal obstruction. It has become. Therefore, a drug containing a drug that can activate the motility function of the gastrointestinal tract can be used as a drug that can eliminate or alleviate the above gastrointestinal disorders such as chronic gastritis, that is, a gastrointestinal motility activation regulator. Has come to be recognized.
- Non-patent Documents 1 and 2 As examples of the gastrointestinal motility activation regulator, cisapride (Non-patent Documents 1 and 2) and Nymetoku Blamide (Non-patent Documents 3 and 4) are known. It is also known that soju ( ⁇ ⁇ ), a kind of herbal medicine component, has this gastrointestinal motility activation regulating effect (Non-patent Document 5).
- Non-patent document 1 Schuurkes, J.A.J., et al., 1985, J. Pharmacol. Exp. T., 234, 775.
- Non-Patent Document 2 Schuurkes, J.A.J., et al., 1984, Gastrointestinal Motility, Roman, C., page 95, MTP press, Lancaster.
- Non-Patent Document 3 Takeshi Fukuhara et al .: Nissho-Musuji, 1966, Vol. 2, No. 1, pp. 15, [PP11 038]
- Non-Patent Document 4 Shigeaki Kumada et al .: Pharmaceutical Research, 1968, No. 39, No. 2, p. 44, [PP115 50]
- Non-Patent Document 5 14th Revised Japanese Pharmacopoeia, 2001, D-674-677
- An object of the present invention is to provide a new medicament having a gastrointestinal motility activation regulating action.
- MMSC methylmethionine sulfo-chloride
- the present invention relates to a gastrointestinal motility activation regulator containing MMSC.
- this invention regulates activation of gastrointestinal motility, including MMSC, to suppress belching, scalding, nausea or vomiting, or to relieve chest grip, leaning, indigestion, stomach / abdominal bloating or loss of appetite Agents are also provided.
- the gastrointestinal motility activation regulator of the present invention has a strong pharmacological action and superior effectiveness compared to the soju that is a crude drug component.
- MMSC has not reported any side effects or other side effects of the central nervous system, such as extrapyramidal symptoms and Parkinson's symptoms, which are observed in anti-dopaminergic cisapride or methucral bramid. Therefore, a medicine containing MMSC can be used as a gastrointestinal motility activation regulator with high pharmacological action and safety.
- MMSC is a drug that was launched in 1959.
- MMSC has been used mainly as a gastric mucosal repair agent or for improving liver function in chronic liver disease. To date, there is no report or suggestion that it has an activity-regulating action and therefore can be a gastrointestinal motility-regulating agent.
- the present invention provides a new application of this MMSC.
- the MMSC used in the present invention is commercially available from, for example, Yonezawa Hamari Chemical Co., Ltd. It may be used according to the method described in Japanese Patent Publication No. 36-13209.
- the gastrointestinal motility activation regulator of the present invention may be a single form of MMSC, or a pharmaceutically acceptable carrier or other pharmaceutical ingredient, excipient, binder, disintegrant, lubricant, It can also be used in the form of a pharmaceutical composition containing a colorant, a corrigent and the like.
- excipients include lactose, starches, crystalline cellulose, sucrose, mannitol, light non-aqueous key acid and the like.
- binder include hydroxypropylmethylcellulose, hydroxypropylcellulose, gelatin, alpha-monoized starch, polybulurpyrrolidone, polybullic alcohol, and pullulan.
- disintegrant include carmellose, carmellose calcium, croscarmellose sodium, crospovidone, corn starch, and low-substituted hydroxypropylcellulose.
- lubricants include magnesium stearate and talc.
- the colorant include tar pigments and iron sesquioxide.
- corrigent include stevia, aspartame, and fragrances.
- the gastrointestinal motility activation regulator of the present invention includes powders, granules, tablets, chewable tablets, film-coated tablets, dragees, drinks, soft capsules, hard capsules, jelly agents and the like depending on the purpose. It can be manufactured and used in a dosage form. In particular, it is preferable to prepare and use powders, granules, tablets, and film-coated tablets.
- MMSC When MMSC is used as a gastrointestinal motility regulator, the dose depends on the dosage form, degree of disease, patient age, etc. MMSC is usually about 30 to 3000 mgZ for adults In particular, it is preferable to administer about 150 to 225 mgZ days.
- the gastrointestinal motility activation regulator of the present invention has an action of improving the intestinal tract transport rate as shown in Examples described later. Therefore, the gastrointestinal motility activation regulator of the present invention can eliminate various symptoms such as chronic gastritis, reflux esophagitis, abdominal indefinite complaints or pseudo-intestinal obstruction caused by retention of intestinal contents. In addition, the present invention improves the intestinal transit rate, thereby causing retention of intestinal contents, burping, scalding, nausea, vomiting, chest gripping, leaning, indigestion, stomach / abdominal bloating and loss of appetite. It is possible to effectively suppress or eliminate symptoms such as those caused by excessive drinking or eating. Furthermore, improve intestinal transport rate and eliminate retention of intestinal contents Can also promote digestion.
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- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nutrition Science (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A highly safe pharmaceutical having an excellent gastrointestinal motor activation-regulating effect is provided. It is a gastrointestinal motor activation regulator comprising methylmethionine sulfonium chloride, which can be used as an excellent gastrointestinal motor activation regulator having a high pharmacological action and no side effects.
Description
明 細 書 Specification
消化管運動賦活調整剤 Gastrointestinal motility regulator
技術分野 Technical field
[0001] 本発明は、メチルメチォニンスルホ -ゥムクロライド (MMSC)の新たな薬効に基づ く消化管運動賦活調整剤に関する。 [0001] The present invention relates to a gastrointestinal motility activation regulator based on a new medicinal effect of methylmethionine sulfo-um chloride (MMSC).
背景技術 Background art
[0002] 近年、消化管の運動機能の低下は、慢性胃炎、逆流性食道炎、腹部不定愁訴ある いは擬性腸閉塞などの種々の胃腸障害をもたらす疾患の一種として理解、認識され るようになってきた。そのため、消化管の運動機能を賦活ィ匕することのできる薬物を含 む医薬は、上記の慢性胃炎等の胃腸障害を解消あるいは緩和することのできる医薬 、すなわち消化管運動賦活調整剤として利用可能であると認識されるようになってき た。 [0002] In recent years, a decrease in the motor function of the gastrointestinal tract has been understood and recognized as a type of disease that causes various gastrointestinal disorders such as chronic gastritis, reflux esophagitis, abdominal indefinite complaints or pseudo-intestinal obstruction. It has become. Therefore, a drug containing a drug that can activate the motility function of the gastrointestinal tract can be used as a drug that can eliminate or alleviate the above gastrointestinal disorders such as chronic gastritis, that is, a gastrointestinal motility activation regulator. Has come to be recognized.
[0003] この消化管運動賦活調整剤の例としては、シサプリド (非特許文献 1、 2)ゃメトク口 ブラミド (非特許文献 3、 4)などが知られている。また、生薬成分の一種であるソウジュ ッ (蒼朮）にも、この消化管運動賦活調整効果があることが知られている (非特許文献 5)。 [0003] As examples of the gastrointestinal motility activation regulator, cisapride (Non-patent Documents 1 and 2) and Nymetoku Blamide (Non-patent Documents 3 and 4) are known. It is also known that soju (ジ ュ), a kind of herbal medicine component, has this gastrointestinal motility activation regulating effect (Non-patent Document 5).
[0004] しかし、メトクロブラミドには抗ドパミン作用による錐体外路症状が、シサプリドにはパ 一キンソン症状が、それぞれ副作用として報告されており、その他にも、心室性不整 脈や過敏症などの副作用も確認されている。また、ソウジュッは生薬成分として穏ゃ かな効き目を示すが、反面、薬理作用として十分であるとは言い難い。 [0004] However, anti-dopaminergic extrapyramidal symptoms have been reported for metocloblamide, and Pakinson's symptoms have been reported for cisapride, and other side effects such as ventricular arrhythmia and hypersensitivity have also been reported. It has been confirmed. Moreover, Soujutsu has a mild effect as a crude drug component, but it is difficult to say that it is sufficient as a pharmacological action.
[0005] 非特許文献 1：シュールケスら（Schuurkes,J.A.J.,et al.)、 1985年、 J. Pharmacol. Exp. T her.,第 234卷、第 775頁。 [0005] Non-patent document 1: Schuurkes, J.A.J., et al., 1985, J. Pharmacol. Exp. T., 234, 775.
非特許文献 2 :シュールケスら（Schuurkes,J.A.J.,et al.)、 1984年、 Gastrointestinal Mo tility,Roman,C.、第 95頁、 MTPプレス、 Lancaster。 Non-Patent Document 2: Schuurkes, J.A.J., et al., 1984, Gastrointestinal Motility, Roman, C., page 95, MTP press, Lancaster.
非特許文献 3 :福原 武ほか：日平滑筋誌、 1966年、第 2卷、第 1号、第 15頁、 [PP11 038] Non-Patent Document 3: Takeshi Fukuhara et al .: Nissho-Musuji, 1966, Vol. 2, No. 1, pp. 15, [PP11 038]
非特許文献 4 :熊田重敦ほか:薬学研究、 1968年、第 39卷、第 2号、第 44頁、 [PP115
50] Non-Patent Document 4: Shigeaki Kumada et al .: Pharmaceutical Research, 1968, No. 39, No. 2, p. 44, [PP115 50]
非特許文献 5 :第 14改正 日本薬局方解説書、 2001年、 D-674〜677頁 Non-Patent Document 5: 14th Revised Japanese Pharmacopoeia, 2001, D-674-677
発明の開示 Disclosure of the invention
発明が解決しょうとする課題 Problems to be solved by the invention
[0006] 本発明の目的は、消化管運動賦活調整作用を有する新たな医薬を提供することに ある。 [0006] An object of the present invention is to provide a new medicament having a gastrointestinal motility activation regulating action.
課題を解決するための手段 Means for solving the problem
[0007] 本発明者らは、意外にも胃粘膜修復剤として知られるメチルメチォニンスルホ -ゥム クロライド (MMSC)が消化管運動賦活調整作用を有していることを見出し、本発明 を完成した。 The present inventors have unexpectedly found that methylmethionine sulfo-chloride (MMSC), which is known as a gastric mucosal repair agent, has a gastrointestinal motility activation regulating action, and has found the present invention. completed.
[0008] すなわち、本発明は、 MMSCを含む消化管運動賦活調整剤に関する。また本発 明は、げっぷ、はきけ、悪心もしくは嘔吐の抑制、又は胸つかえ、もたれ、消化不良、 胃部 ·腹部膨満感もしくは食欲不振の解消のための、 MMSCを含む消化管運動賦 活調整剤も提供する。 That is, the present invention relates to a gastrointestinal motility activation regulator containing MMSC. In addition, this invention regulates activation of gastrointestinal motility, including MMSC, to suppress belching, scalding, nausea or vomiting, or to relieve chest grip, leaning, indigestion, stomach / abdominal bloating or loss of appetite Agents are also provided.
発明の効果 The invention's effect
[0009] 本発明である消化管運動賦活調整剤は、生薬成分であるソウジュッに比べて薬理 作用が強く有効性に優れる。一方、 MMSCには、抗ドパミン作用ゃシサプリドゃメトク 口ブラミドに認められる錐体外路症状やパーキンソン症状などの中枢神経系の副作 用その他の副作用などは報告されていない。従って、 MMSCを含む医薬は、高い薬 理作用と安全性とを備えた消化管運動賦活調整剤として利用することができる。 発明を実施するための最良の形態 [0009] The gastrointestinal motility activation regulator of the present invention has a strong pharmacological action and superior effectiveness compared to the soju that is a crude drug component. On the other hand, MMSC has not reported any side effects or other side effects of the central nervous system, such as extrapyramidal symptoms and Parkinson's symptoms, which are observed in anti-dopaminergic cisapride or methucral bramid. Therefore, a medicine containing MMSC can be used as a gastrointestinal motility activation regulator with high pharmacological action and safety. BEST MODE FOR CARRYING OUT THE INVENTION
[0010] MMSCは、 1959年に販売が開始された医薬であり、主に胃粘膜修復剤として、あ るいは慢性肝疾患における肝機能の改善のために用いられてきた力 MMSCが消 化管運動賦活調整作用を有し、従って消化管運動賦活調整剤となり得ることについ ては、これまでのところ報告も示唆もない。本発明はこの MMSCの新たな用途を提 供するものである。 [0010] MMSC is a drug that was launched in 1959. MMSC has been used mainly as a gastric mucosal repair agent or for improving liver function in chronic liver disease. To date, there is no report or suggestion that it has an activity-regulating action and therefore can be a gastrointestinal motility-regulating agent. The present invention provides a new application of this MMSC.
[0011] 本発明で使用する MMSCは、例えば米沢浜理薬品工業 (株)から市販されている
ものを利用してもよぐまた特公昭 36— 13209号公報に記載された方法に従って合 成し、使用してもよい。 [0011] The MMSC used in the present invention is commercially available from, for example, Yonezawa Hamari Chemical Co., Ltd. It may be used according to the method described in Japanese Patent Publication No. 36-13209.
[0012] また本発明の消化管運動賦活調整剤は、 MMSCの単身の形態でも、あるいは医 薬上許容される担体や他の医薬成分、賦形剤、結合剤、崩壊剤、滑沢剤、着色剤、 矯味剤等を含む医薬組成物の形態としても使用することができる。 [0012] Further, the gastrointestinal motility activation regulator of the present invention may be a single form of MMSC, or a pharmaceutically acceptable carrier or other pharmaceutical ingredient, excipient, binder, disintegrant, lubricant, It can also be used in the form of a pharmaceutical composition containing a colorant, a corrigent and the like.
[0013] 賦形剤としては、乳糖、デンプン類、結晶セルロース、蔗糖、マン-トール、軽質無 水ケィ酸等が挙げられる。結合剤としては、ヒドロキシプロピルメチルセルロース、ヒド ロキシプロピルセルロース、ゼラチン、アルファ一化デンプン、ポリビュルピロリドン、 ポリビュルアルコール、プルラン等が挙げられる。崩壊剤としては、カルメロース、カル メロースカルシウム、クロスカルメロースナトリウム、クロスポビドン、トウモロコシ澱粉、 低置換度ヒドロキシプロピルセルロース等が挙げられる。滑沢剤としては、ステアリン 酸マグネシウム、タルク等が挙げられる。着色剤としては、タール色素、三二酸化鉄 等が挙げられる。矯味剤としてはステビア、アスパルテーム、香料等が挙げられる。 [0013] Examples of excipients include lactose, starches, crystalline cellulose, sucrose, mannitol, light non-aqueous key acid and the like. Examples of the binder include hydroxypropylmethylcellulose, hydroxypropylcellulose, gelatin, alpha-monoized starch, polybulurpyrrolidone, polybullic alcohol, and pullulan. Examples of the disintegrant include carmellose, carmellose calcium, croscarmellose sodium, crospovidone, corn starch, and low-substituted hydroxypropylcellulose. Examples of lubricants include magnesium stearate and talc. Examples of the colorant include tar pigments and iron sesquioxide. Examples of the corrigent include stevia, aspartame, and fragrances.
[0014] 本発明の消化管運動賦活調整剤は、 目的に応じて散剤、顆粒剤、錠剤、チュアブ ル錠、フィルムコーティング錠、糖衣錠、ドリンク剤、軟カプセル剤、硬カプセル剤、ゼ リー剤等の剤型に製造して使用することができる。特に、散剤、顆粒剤、錠剤、フィル ムコーティング錠の剤型に製造して使用することが好ましい。 [0014] The gastrointestinal motility activation regulator of the present invention includes powders, granules, tablets, chewable tablets, film-coated tablets, dragees, drinks, soft capsules, hard capsules, jelly agents and the like depending on the purpose. It can be manufactured and used in a dosage form. In particular, it is preferable to prepare and use powders, granules, tablets, and film-coated tablets.
[0015] MMSCを消化管運動賦活調整剤として使用する場合の投与量は、剤型、疾患の 程度、患者の年齢等の要素に依存する力 通常成人に対して MMSCを 30〜3000 mgZ日程度、特に 150〜225mgZ日程度を投与することが好ましい。 [0015] When MMSC is used as a gastrointestinal motility regulator, the dose depends on the dosage form, degree of disease, patient age, etc. MMSC is usually about 30 to 3000 mgZ for adults In particular, it is preferable to administer about 150 to 225 mgZ days.
[0016] 本発明の消化管運動賦活調整剤は、後述する実施例において示されるように、腸 管輸送率を向上させる作用を有している。従って、本発明の消化管運動賦活調整剤 は、腸管内容物の滞留に起因する慢性胃炎、逆流性食道炎、腹部不定愁訴あるい は擬性腸閉塞などの種々の症状を解消し得る。また、本発明は、腸管輸送率を向上 させることによって、腸管内容物の滞留が原因となるげっぷ、はきけ、悪心、嘔吐、胸 つかえ、もたれ、消化不良、胃部 ·腹部膨満感ならびに食欲不振などの症状、特に飲 み過ぎもしくは食べ過ぎによって生じるこれらの症状を効果的に抑制あるいは解消す ることができる。さらには、腸管輸送率を向上させ、腸管内容物の滞留を解消すること
によって消化促進を促すこともできる。 [0016] The gastrointestinal motility activation regulator of the present invention has an action of improving the intestinal tract transport rate as shown in Examples described later. Therefore, the gastrointestinal motility activation regulator of the present invention can eliminate various symptoms such as chronic gastritis, reflux esophagitis, abdominal indefinite complaints or pseudo-intestinal obstruction caused by retention of intestinal contents. In addition, the present invention improves the intestinal transit rate, thereby causing retention of intestinal contents, burping, scalding, nausea, vomiting, chest gripping, leaning, indigestion, stomach / abdominal bloating and loss of appetite. It is possible to effectively suppress or eliminate symptoms such as those caused by excessive drinking or eating. Furthermore, improve intestinal transport rate and eliminate retention of intestinal contents Can also promote digestion.
[0017] 以下に、薬理試験例、製造例を用いて本発明を具体的に説明するが、本発明はこ れらに限定されるものではない。 [0017] The present invention will be specifically described below using pharmacological test examples and production examples, but the present invention is not limited thereto.
実施例 1 Example 1
[0018] 下記試験方法に従って、腸管輸送能に及ぼす被験物質の効果を検討した。 [0018] According to the following test method, the effect of the test substance on the intestinal transport ability was examined.
[0019] 試験前日に絶食した 5週齢の ddY系雄性マウスに、 0. 5%メチルセルロース（以下 MCという）に懸濁したメチルメチォニンスルホ -ゥムクロライド（1000mgZkg、 3000 mgZkg)を経口投与し、その 15分後に活性炭素末懸濁液を経口投与した。さらにそ の 30分後に動物を頸椎脱臼にてと殺し、幽門部力も回盲部までの腸管を摘出した。 被験物質の腸管輸送能は、幽門部からの炭素末の移動距離を腸管の全長で除し、 腸管輸送率として表した。また、同様の試験をソウジュッ乾燥エキス S (300mgZkg、 原生薬換算量として 3000mgZkg)について行った。試験結果を表 1に示す。 [0019] 5-week-old male ddY mice fasted the day before the study were orally administered methylmethionine sulfo-um chloride (1000 mgZkg, 3000 mgZkg) suspended in 0.5% methylcellulose (hereinafter referred to as MC), After 15 minutes, the activated carbon powder suspension was orally administered. 30 minutes later, the animal was killed by cervical dislocation, and the intestinal tract of the pyloric region up to the ileocecal region was removed. The intestinal transport ability of the test substance was expressed as the intestinal transport rate by dividing the distance of the carbon powder from the pylorus by the total length of the intestinal tract. A similar test was conducted on Sojitsu dried extract S (300 mgZkg, 3000 mgZkg as the amount of drug substance). Table 1 shows the test results.
[0020] [表 1] [0020] [Table 1]
用量 移動率 (50 Dose transfer rate (50
群 Group
(rag/kg) 平均値 土 標準誤差 比率 (rag / kg) Average value Soil Standard error Ratio
iン卜 π—ル 56. 6 ± 2. 8 1. 000 i-n π-l 56. 6 ± 2. 8 1. 000
MM S C 1 0 0 0 73. 4 土 4. 3 1. 297 MM S C 1 0 0 0 73. 4 Sat 4. 3 1. 297
MM S C 3 0 0 0 86. 6 土 4. 6 1. 530 ソウジュッ 3 0 0 0 53. 0 ± 3. 1 0. 936 MM S C 3 0 0 0 86.6 Sat 4. 6 1. 530 Power 3 0 0 0 53. 0 ± 3. 1 0. 936
N=6 N = 6
*:p〈0. 05 vs コントローノレ （Williamsの多重比較） *: p 〈0. 05 vs control line (Williams multiple comparison)
[0021] 以上のように、 MMSCの投与によって腸管輸送率の向上が確認され、用量依存的 な消化管運動賦活調整作用が確認された。
[0021] As described above, it was confirmed that administration of MMSC improved the intestinal transport rate, and a dose-dependent gastrointestinal motility activation regulating action was confirmed.
Claims
[1] メチルメチォニンスルホ -ゥムクロライドを含む消化管運動賦活調整剤。 [1] Gastrointestinal motility regulator containing methyl methionine sulfo-um chloride.
[2] げっぷ、はきけ、悪心もしくは嘔吐の抑制、又は胸つかえ、もたれ、消化不良、胃部- 腹部膨満感もしくは食欲不振の解消のための、請求項 1に記載の消化管運動賦活 調整剤。 [2] Gastrointestinal motility activation regulator according to claim 1, for suppressing belching, scalding, nausea or vomiting, or for eliminating chest grip, leaning, indigestion, stomach-abdominal bloating or loss of appetite .
[3] げっぷ、はきけ、悪心、嘔吐、胸つかえ、もたれ、消化不良、胃部 ·腹部膨満感ならび に食欲不振が飲み過ぎもしくは食べ過ぎによるものである、請求項 2に記載の消化管 運動賦活調整剤。 [3] Gastrointestinal motility according to claim 2, wherein belching, scalding, nausea, vomiting, chest gripping, leaning, indigestion, stomach / abdominal bloating and loss of appetite are due to overdrinking or overeating. Activation regulator.
[4] 腹部不定愁訴あるいは偽性腸閉塞の解消のための、請求項 1に記載の消化管運動 賦活調整剤。 [4] The agent for regulating gastrointestinal motility activation according to claim 1, for eliminating abdominal indefinite complaints or pseudo-intestinal obstruction.
[5] 消化促進のための、請求項 1に記載の消化管運動賦活調整剤。
[5] The gastrointestinal motility activation regulator according to claim 1, for promoting digestion.
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| JP2015214530A (en) * | 2013-07-31 | 2015-12-03 | 興和株式会社 | Gastrointestinal agent composition |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH08259445A (en) * | 1995-01-27 | 1996-10-08 | Takeda Chem Ind Ltd | Medicinal composition for improving gastric emptying performance |
| JP2000327567A (en) * | 1999-05-18 | 2000-11-28 | Susumu Kurosawa | Agent for improving movement of digestive canal |
-
2006
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH08259445A (en) * | 1995-01-27 | 1996-10-08 | Takeda Chem Ind Ltd | Medicinal composition for improving gastric emptying performance |
| JP2000327567A (en) * | 1999-05-18 | 2000-11-28 | Susumu Kurosawa | Agent for improving movement of digestive canal |
Non-Patent Citations (4)
| Title |
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| HARADA N.: "Shokaki Shikkan ni Tomonau Jikaku Shojo ni Taisuru Cabagin-U Kowa San no Yuyosei no Kento", BASIC PHARMACOLOGY & THERAPEUTICS, vol. 9, no. 12, 1981, pages 5211 - 5215, XP003006792 * |
| KABUSHIKI KAISHA YAKUJI NIPPOSHA: "Saikin no Shin'yaku 2002", KABUSHIKI KAISHA YAKUJI NIPPOSHA, 2002, pages 297, XP003006791 * |
| SALIM A.S. ET AL.: "Sulphydryl-containing agents and the prevention of duodenal ulcer relapse", PHARMACOLOGY, vol. 46, no. 5, 1993, pages 281 - 288, XP008009446 * |
| WATANABE T. ET AL.: "Rat Ethanol Kaiyo ni Okeru Inen'eki To Tanpakushitsu no Ryoteki Hendo ni Taisuru Methyl Methionine Sulfonium Chloride (MMSC) Mae Toyo no Koka", BASIC PHARMACOLOGY & THERAPEUTICS, vol. 22, no. 10, 1994, pages 4355 - 4361, XP003006793 * |
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