JP2003321371A - Diuretic - Google Patents
DiureticInfo
- Publication number
- JP2003321371A JP2003321371A JP2002126021A JP2002126021A JP2003321371A JP 2003321371 A JP2003321371 A JP 2003321371A JP 2002126021 A JP2002126021 A JP 2002126021A JP 2002126021 A JP2002126021 A JP 2002126021A JP 2003321371 A JP2003321371 A JP 2003321371A
- Authority
- JP
- Japan
- Prior art keywords
- diuretic
- composition
- diuretic effect
- effect
- mineral
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Abstract
Description
【0001】[0001]
【発明が属する技術分野】本発明は、ダイフラクトース
アンハイドライド(DFA)を経口又は非経口で摂取す
ることにより利尿効果を高める組成物に関するものであ
る。TECHNICAL FIELD The present invention relates to a composition which enhances a diuretic effect by ingesting difructose anhydride (DFA) orally or parenterally.
【0002】[0002]
【従来の技術】利尿効果はヒトの健康維持、疾病の緩和
に重要なものである。現在は、様々な原因でおこりえる
浮腫の治療で重要な要因となっている。浮腫は、様々な
要因で、水分が体にたまり、「むくみ」を生じるもの
で、足、顔のむくみ、腹部に水がたまる「腹水」、肺に
水がたまる「肺水腫」などがある。「腹水」は、肝硬変
など重篤な肝臓疾患で発生することが多い。「肺水腫」
は、心不全などで、心臓の動きが低下し血液循環が悪化
すると発生することが多く、呼吸難を伴うことが多い。
また、腎臓疾患においては、ネフローゼによる、顔、ま
ぶたのむくみ、腫れ、といった症状として現れる場合が
多い。これらの症状を緩和するために多用される治療薬
は、「ループ利尿剤」、「チアジド系降圧利尿剤」、
「カリウム保持性利尿剤」があげられる。2. Description of the Related Art The diuretic effect is important for maintaining human health and alleviating diseases. Currently, it is an important factor in the treatment of edema that can occur due to various causes. Edema causes "swelling" due to water accumulation in the body due to various factors, and includes swelling of the legs and face, "ascites" in which water is accumulated in the abdomen, and "pulmonary edema" in which water is accumulated in the lungs. "Ascites" often occurs in serious liver diseases such as cirrhosis. "Pulmonary edema"
Often occurs when heart movement slows and blood circulation deteriorates due to heart failure and the like, and is often accompanied by dyspnea.
Moreover, in renal diseases, it often occurs as symptoms such as swelling of the face and eyelids and swelling due to nephrosis. Therapeutic agents often used to relieve these symptoms are "loop diuretics", "thiazide antihypertensive diuretics",
An example is a “potassium-retaining diuretic”.
【0003】「ループ利尿剤」は、プロセミドに代表さ
れるもので、尿細管の塩分と水分の再吸収を抑えること
により、尿量を増加させるものである。「チアジド系降
圧利尿剤」も、同様の作用であるが、利尿効果を高める
ことによる血圧降下剤としても多用されている。「カリ
ウム保持性利尿剤」は、カリウム濃度を保持したまま、
利尿効果を発揮するもので、低カリウム血症」を抑制す
る機能も期待される。このうち、スピロノラクトンは、
抗利尿ホルモンのアルドステロンの働きを抑制する機能
をもち、利尿効果は強くないが、肝硬変、ネフローゼ、
心不全などに伴う、二次性アルドステロン症による浮腫
改善に使用される。The "loop diuretic" is typified by prosemide, which increases the amount of urine by suppressing reabsorption of salt and water in the renal tubule. The "thiazide antihypertensive diuretic agent" has a similar action, but is also widely used as a blood pressure lowering agent by enhancing the diuretic effect. "Potassium-retaining diuretics" are, while maintaining the potassium concentration,
It has a diuretic effect and is expected to have a function of suppressing "hypokalemia". Of these, spironolactone is
It has a function to suppress the action of the antidiuretic hormone aldosterone, and although it does not have a strong diuretic effect, it has cirrhosis, nephrosis,
It is used to improve edema due to secondary aldosteronism associated with heart failure.
【0004】[0004]
【発明が解決しようとする課題】しかしながら、利尿剤
の一般的な副作用として、「電解質異常」が指摘されて
いる。「ループ利尿剤」や「チアジド系降圧剤」は低カ
リウム血症が問題となる。また、逆に「カリウム保持性
利尿剤」の場合は、高カリウム血症の問題がある。この
ようにミネラルバランスの均衡が崩壊することは、利尿
剤の宿命とされている。低ミネラル状態の場合、倦怠
感、筋力低下、便秘、不整脈などの症状がおこる。高ミ
ネラル状態の場合、倦怠感、不整脈、動悸、息切れ、手
足のしびれ、不安感、異常言動などといった症状が現れ
る場合がある。本発明は、このように利尿剤においてみ
られるミネラルバランスを崩壊させることなく、利尿効
果を持つ組成物を見出すことを課題とした。However, "abnormal electrolyte" has been pointed out as a general side effect of diuretics. "Loop diuretics" and "thiazide antihypertensive agents" cause hypokalemia. On the contrary, in the case of "potassium-retaining diuretics", there is a problem of hyperkalemia. This disruption of the mineral balance is the fate of diuretics. In the case of low mineral state, symptoms such as malaise, weakness, constipation and arrhythmia occur. High-mineral status may cause symptoms such as malaise, arrhythmia, palpitation, shortness of breath, numbness of limbs, anxiety, and abnormal behavior. An object of the present invention is to find a composition having a diuretic effect without degrading the mineral balance found in the diuretic agent.
【0005】[0005]
【課題を解決するための手段】本発明らは、ダイフラク
トースアンハイドライド(DFA)が利尿効果を有する
ことを見出した。すなわち、本発明は、ダイフラクトー
スアンハイドライドを含有することを特徴とする、利尿
効果を有する経口用組成物及び利尿剤に関する。DISCLOSURE OF THE INVENTION The present inventors have found that difructose anhydride (DFA) has a diuretic effect. That is, the present invention relates to an oral composition and a diuretic having a diuretic effect, which is characterized by containing difructose anhydride.
【0006】[0006]
【発明の実施の形態】ダイフラクトースアンハイドライ
ドは、2個のフラクトースの還元末端が、互いに、他の
フラクトースの還元末端以外の水酸基に結合した環状二
糖類である。その結合様式は4つあり、それぞれ、DF
AI、DFAII、DFAIII、DFAIVと称されてい
る。これらDFAは、カラメルなど、糖加工食品に含有
されているが、工業的な生産も可能になっている。一例
をあげると、主にチコリに含まれるイヌリンから、イヌ
ラーゼにより生産されるもので、たとえば、Arthobacte
rsp.H65-7 株を使用した発酵法により本菌株が生産する
イヌラーゼIIによるイヌリンの分解により生産される。
ただし、この製法は一例であって、本発明を制限するも
のではない。BEST MODE FOR CARRYING OUT THE INVENTION Difructose hydride is a cyclic disaccharide in which the reducing ends of two fructose groups are bound to each other by hydroxyl groups other than the reducing ends of other fructose. There are four binding modes, and each is DF
They are called AI, DFAII, DFAIII and DFAIV. Although these DFAs are contained in sugar-processed foods such as caramel, industrial production is also possible. To give an example, inulin produced mainly from inulin contained in chicory. For example, Arthobacte
It is produced by degrading inulin by inulase II produced by this strain by a fermentation method using rsp.H65-7 strain.
However, this manufacturing method is an example and does not limit the present invention.
【0007】本発明では、4種類のDFAの内、好まし
くは、DFAIIIを使用する。DFAI、DFAII、D
FAIVは、二糖類として安定性に欠ける事があり、吸湿
・潮解により変質する可能性があり、実用化に際し、ハ
ンドリング性能に問題が生じる可能性があるからであ
る。しかしながら、本発明でいう利尿効果においては、
問題なく使用可能である。In the present invention, of the four types of DFA, DFA III is preferably used. DFAI, DFAII, D
This is because FAIV may lack stability as a disaccharide, may change in quality due to moisture absorption and deliquescent, and may have a problem in handling performance in practical use. However, in the diuretic effect according to the present invention,
It can be used without problems.
【0008】これらDFAは食品として使用することが
できる二糖類であるが、現段階で知られている最大の特
徴は、ミネラル吸収機能を持つ事である。DFAは、カ
ルシウム、カリウムなどに対し、吸収促進効果をもつ。
また、その吸収促進効果は、通常の糖類の場合、腸内細
菌を活性化させ、腸内のpHを低下させることによりミ
ネラルを溶解させて、吸収しやすくする作用機作である
が、DFAは、そのような作用機作以外に、腸管のタイ
トジャンクションを経由して体内にミネラルを取り込む
ことが報告されている。また、この働きは、ミネラルが
欠乏している状態のとき、より吸収機能をたかめ、さら
にミネラルが、過剰のときは、吸収機能が抑制されると
いう特徴をもつ。すなわち、本発明者は、このようなミ
ネラル吸収機能をもつDFAに、利尿効果をもつことを
見出し、本発明を完成させた。[0008] These DFAs are disaccharides that can be used as foods, and the most known feature at this stage is that they have a mineral absorption function. DFA has an absorption promoting effect on calcium, potassium and the like.
In addition, its absorption promoting effect, in the case of ordinary saccharides, is a mechanism of action that activates intestinal bacteria and lowers intestinal pH to dissolve minerals and facilitates absorption. In addition to such a mechanism of action, it has been reported that minerals are taken into the body via a tight junction of the intestinal tract. In addition, this function is characterized in that the absorption function is enhanced when the mineral is deficient, and the absorption function is suppressed when the mineral is excessive. That is, the present inventor has found that DFA having such a mineral absorption function has a diuretic effect, and completed the present invention.
【0009】本発明による組成物は、上記した理由によ
り既存の利尿剤が持つ、低ミネラル状態、または、高ミ
ネラル状態を誘起することなく、利尿効果を高めること
ができる。本発明においては、DFAを含有する組成物
を製造し、利尿効果を期待するヒトに経口又は非経口で
摂取させる。本発明の組成物は、経口又は非経口で摂取
できるものであれば、最終形態の制限はない。The composition according to the present invention can enhance the diuretic effect without inducing the low-mineral state or the high-mineral state that existing diuretics have for the reasons described above. In the present invention, a composition containing DFA is produced and orally or parenterally ingested by a human who expects a diuretic effect. The composition of the present invention is not limited in its final form as long as it can be taken orally or parenterally.
【0010】経口用としては、粉剤、固形、錠剤、飲料
など様々な形態が可能であり、食品としても製造するこ
とが可能である。その場合の賦形剤、香料、滑沢剤、酸
味料など、普通に使用されている原材料の添加は制限な
く実施可能である。また、加工にあたって、加熱、溶
解、圧縮、攪拌など物理的な影響についても、通常の加
工レベルであれば一切、問題なく実施可能である。DF
Aの適性摂取量は、概ね、一日あたり、1g以上10g
以下である。1g以下であると、効果がみられず10g
以上であると、軟便化などの兆候が見られる場合があ
る。For oral use, various forms such as powders, solids, tablets and beverages are possible, and they can be manufactured as foods. In that case, commonly used raw materials such as excipients, flavors, lubricants, acidulants, etc. can be added without limitation. Further, in processing, physical influences such as heating, melting, compression and stirring can be carried out without any problem at a normal processing level. DF
The appropriate intake of A is about 1g to 10g per day.
It is the following. If it is less than 1g, the effect is not seen and 10g
If it is above, signs such as loose stool may be seen.
【0011】ただし、軟便化は、ヒトにより、体質的な
影響、普段の食生活などの影響もあるので、必ずしも、
10g以上の摂取が厳禁ではなく、そのヒトの状況を見
つつ加減することが必要である。いずれにしても、DF
Aは、安全な糖質食品であることから、毒性に関する問
題はないし、一般に使用されている利尿剤のような、ア
ナフィラキシー、アレルギー、意識障害、再生不良性貧
血、皮下出血、などの重篤な副作用、および、肝障害、
発疹などの注意を要する副作用なども発生することはな
く安全に利尿効果を期待できる。非経口用としても、通
常の製剤化技術を適用することができる。[0011] However, since soft stools may affect the constitution of humans and the usual dietary habits depending on humans,
It is not strictly prohibited to take more than 10 g, and it is necessary to adjust the amount while watching the human situation. In any case, DF
Since A is a safe sugar food, there is no problem regarding toxicity, and there are serious diuretics such as anaphylaxis, allergies, consciousness disorders, aplastic anemia, and subcutaneous bleeding that are commonly used. Side effects and liver damage,
No side effects such as a rash that require caution can be expected and a diuretic effect can be expected safely. Even for parenteral use, ordinary formulation techniques can be applied.
【0012】[0012]
【実施例】実施例1
〔DFAIIIを用いた利尿試験〕DFAIIIを造粒し、散
剤食品とした。賦形剤なしで造粒可能であったので、D
FA純度は100%の粉状食品である。健常人男性6名
に、試験第1期として、この散剤食品を1g/1日、水
と一緒に摂取させることを1週間継続した。ついで、1
週間のウオッシュアウト期間を設けた後、試験第2期と
して、同一の健常人6名に、砂糖を1g/1日、水と一
緒に1週間継続して摂取させた。試験期間中は、全員、
同一環境で、生活させ運動強度を同じくし、かつ同一の
食事、飲水量とした。試験期間中の排尿を全量回収し、
その量を測定して一日あたりの排尿量の平均を求め、両
試験期間で比較した。その結果を表1に示す。Examples Example 1 [Diuretic test using DFA III] DFA III was granulated to prepare a powdered food. Since it was possible to granulate without excipients, D
FA purity is 100% powdery food. As a first phase of the test, 6 healthy men were allowed to continue to take this powdered food with water at 1 g / day for 1 week. Then 1
After providing a weekly washout period, as the second stage of the test, 6 healthy subjects were allowed to continuously ingest 1 g / day of sugar together with water for 1 week. During the exam period, everyone,
They were allowed to live in the same environment, had the same exercise intensity, and had the same amount of food and water. Collect all urine during the test period,
The amount was measured to obtain the average urine output per day, and the results were compared in both test periods. The results are shown in Table 1.
【0013】[0013]
【表1】 [Table 1]
【0014】以上のごとく、本発明による組成物を摂取
した試験第1期の尿量/日の平均値は、砂糖を摂取した
試験第2期の尿量/日の平均値よりも同一被験者間で、
明らかな増加傾向を示した。また、あわせておこなっ
た、血液生化学的検査結果、すなわち、肝機能検査値、
腎機能検査値、血圧値、血球数値、総Chol(コレステロ
ール値)、TG(トリグリセリド値)は、試験第1期、第
2期とも、変動はなく、自覚所見においてもなんら異常
は報告されなかった。As described above, the average value of urine volume / day in the first test period ingesting the composition according to the present invention was higher than that in the same test subject in the second period test in which sugar was ingested. so,
It showed a clear increasing trend. In addition, the blood biochemical test results, that is, the liver function test values,
There were no changes in renal function test values, blood pressure values, blood cell counts, total Chol (cholesterol level), TG (triglyceride level) in the first and second phase of the study, and no abnormal findings were reported in the subjective findings. .
【0015】[0015]
【発明の効果】本発明により、安全で副作用がない利尿
効果を有する組成物が提供される。INDUSTRIAL APPLICABILITY The present invention provides a composition which is safe and has a diuretic effect without side effects.
───────────────────────────────────────────────────── フロントページの続き (51)Int.Cl.7 識別記号 FI テーマコート゛(参考) A61P 9/00 A61P 9/00 11/00 11/00 13/12 13/12 C07H 3/04 C07H 3/04 (72)発明者 塩見 卓也 神奈川県横浜市戸塚区上品濃12番13号 株 式会社ファンケル中央研究所内 (72)発明者 田村 亜紀子 神奈川県横浜市戸塚区上品濃12番13号 株 式会社ファンケル中央研究所内 (72)発明者 重松 典宏 神奈川県横浜市戸塚区上品濃12番13号 株 式会社ファンケル中央研究所内 (72)発明者 有塚 勉 東京都中央区京橋2丁目3番13号 日本甜 菜製糖株式会社内 (72)発明者 菊地 裕人 北海道帯広市稲田町南9線西13番地 日本 甜菜製糖株式会社総合研究所内 Fターム(参考) 4C057 BB01 BB03 4C086 AA01 AA02 EA01 MA01 MA04 NA06 NA14 ZA36 ZA59 ZA75 ZA83 ZC21 ─────────────────────────────────────────────────── ─── Continued Front Page (51) Int.Cl. 7 Identification Code FI Theme Coat (Reference) A61P 9/00 A61P 9/00 11/00 11/00 13/12 13/12 C07H 3/04 C07H 3 / 04 (72) Inventor Takuya Shiomi 12-13 Kamishinano, Totsuka-ku, Yokohama, Kanagawa Prefecture FANCL Central Research Institute (72) Inventor Akiko Tamura 12-13 Kamishinano, Totsuka-ku, Yokohama, Kanagawa Central Research Laboratory (72) Inventor Norihiro Shigematsu 12-13 Kamishinano, Totsuka-ku, Yokohama, Kanagawa Stock company FANCL Central Research Laboratory (72) Inventor Tsutomu Arizuka 2-33-1 Kyobashi, Chuo-ku, Tokyo Inside the Sugar Sugar Co., Ltd. (72) Yuto Kikuchi, No. 9 West 9th Line, Inada-cho, Obihiro City, Hokkaido Japan F-Term (Reference) 4C057 BB01 BB03 4C086 inside the Research Center for Sugar Sugar Co. AA01 AA02 EA01 MA01 MA04 NA06 NA14 ZA36 ZA59 ZA75 ZA83 ZC21
Claims (2)
有することを特徴とする利尿効果を有する経口用組成
物。1. An oral composition having a diuretic effect, which comprises difructose anhydride.
有することを特徴とする利尿剤。2. A diuretic characterized by containing difructose anhydride.
Priority Applications (15)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2002126021A JP4183060B2 (en) | 2002-04-26 | 2002-04-26 | Diuretic |
US10/512,212 US7754701B2 (en) | 2002-04-26 | 2003-04-24 | Difructose anhydride-containing composition and use thereof |
PCT/JP2003/005245 WO2003090759A1 (en) | 2002-04-26 | 2003-04-24 | Difructose anhydride-containing composition and use thereof |
EP03725659.1A EP1504761B1 (en) | 2002-04-26 | 2003-04-24 | Difructose anhydride-containing composition and use thereof |
KR1020107009449A KR100993963B1 (en) | 2002-04-26 | 2003-04-24 | A composition for inhibiting the dental caries |
KR1020107009447A KR100993978B1 (en) | 2002-04-26 | 2003-04-24 | A composition for improving bowel movement |
KR1020047016983A KR100994032B1 (en) | 2002-04-26 | 2003-04-24 | Accelerator for absorption of Mg, Zn, Cu |
AU2003231486A AU2003231486A1 (en) | 2002-04-26 | 2003-04-24 | Difructose anhydride-containing composition and use thereof |
CN2008101828362A CN101468029B (en) | 2002-04-26 | 2003-04-24 | Difructose anhydride-containing composition and use thereof |
EP11191344A EP2450044A1 (en) | 2002-04-26 | 2003-04-24 | Difructose anhydride-containing composition for use in inhibiting dental caries |
EP11191343A EP2446889A1 (en) | 2002-04-26 | 2003-04-24 | Difructose anhydride-containing composition for use in improving bowel movement |
CNA2006101093244A CN1923210A (en) | 2002-04-26 | 2003-04-24 | Diructose anhydride-containing composition and use thereof |
CNB038094134A CN100534438C (en) | 2002-04-26 | 2003-04-24 | Difructose anhydride-containing composition and use thereof |
US12/788,159 US7964581B2 (en) | 2002-04-26 | 2010-05-26 | Use of difructose anhydride-containing composition |
US12/788,209 US8492363B2 (en) | 2002-04-26 | 2010-05-26 | Use of difructose anhydride-containing composition |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2002126021A JP4183060B2 (en) | 2002-04-26 | 2002-04-26 | Diuretic |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2003321371A true JP2003321371A (en) | 2003-11-11 |
JP4183060B2 JP4183060B2 (en) | 2008-11-19 |
Family
ID=29540567
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2002126021A Expired - Fee Related JP4183060B2 (en) | 2002-04-26 | 2002-04-26 | Diuretic |
Country Status (2)
Country | Link |
---|---|
JP (1) | JP4183060B2 (en) |
CN (2) | CN101468029B (en) |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2005170855A (en) * | 2003-12-11 | 2005-06-30 | Nippon Beet Sugar Mfg Co Ltd | Crystal or crystal powder difructose anhydride iii |
JP2006083141A (en) * | 2004-09-17 | 2006-03-30 | Fancl Corp | Rapidly disintegrative solid preparation |
WO2006038613A1 (en) * | 2004-10-04 | 2006-04-13 | Fancl Corporation | Oral composition containing difructose anhydride |
JPWO2006016424A1 (en) * | 2004-08-13 | 2008-05-01 | 日本甜菜製糖株式会社 | Calcium deficiency preventive and / or therapeutic agent |
US8530446B2 (en) | 2004-11-17 | 2013-09-10 | Fancl Corporation | Oral composition containing difructose anhydride |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH01225492A (en) * | 1988-03-07 | 1989-09-08 | Mitsubishi Kasei Corp | Production of difructose dianhydride iii |
-
2002
- 2002-04-26 JP JP2002126021A patent/JP4183060B2/en not_active Expired - Fee Related
-
2003
- 2003-04-24 CN CN2008101828362A patent/CN101468029B/en not_active Expired - Fee Related
- 2003-04-24 CN CNA2006101093244A patent/CN1923210A/en active Pending
Cited By (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2005170855A (en) * | 2003-12-11 | 2005-06-30 | Nippon Beet Sugar Mfg Co Ltd | Crystal or crystal powder difructose anhydride iii |
JPWO2006016424A1 (en) * | 2004-08-13 | 2008-05-01 | 日本甜菜製糖株式会社 | Calcium deficiency preventive and / or therapeutic agent |
JP4693777B2 (en) * | 2004-08-13 | 2011-06-01 | 日本甜菜製糖株式会社 | Calcium deficiency preventive and / or therapeutic agent |
US8048866B2 (en) | 2004-08-13 | 2011-11-01 | Nippon Beet Sugar Mfg., Co., Ltd. | Preventive and/or therapeutic agent for calcipenia |
JP2006083141A (en) * | 2004-09-17 | 2006-03-30 | Fancl Corp | Rapidly disintegrative solid preparation |
JP4630614B2 (en) * | 2004-09-17 | 2011-02-09 | 株式会社ファンケル | Fast disintegrating solid preparation |
WO2006038613A1 (en) * | 2004-10-04 | 2006-04-13 | Fancl Corporation | Oral composition containing difructose anhydride |
JP2006104103A (en) * | 2004-10-04 | 2006-04-20 | Fancl Corp | Oral composition comprising difructose anhydride |
JP4721684B2 (en) * | 2004-10-04 | 2011-07-13 | 株式会社ファンケル | Oral composition containing difructose anhydride |
US8530446B2 (en) | 2004-11-17 | 2013-09-10 | Fancl Corporation | Oral composition containing difructose anhydride |
Also Published As
Publication number | Publication date |
---|---|
JP4183060B2 (en) | 2008-11-19 |
CN1923210A (en) | 2007-03-07 |
CN101468029B (en) | 2011-02-02 |
CN101468029A (en) | 2009-07-01 |
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