JPH0374327A - Excitometabolic agent for alcohol - Google Patents
Excitometabolic agent for alcoholInfo
- Publication number
- JPH0374327A JPH0374327A JP1211064A JP21106489A JPH0374327A JP H0374327 A JPH0374327 A JP H0374327A JP 1211064 A JP1211064 A JP 1211064A JP 21106489 A JP21106489 A JP 21106489A JP H0374327 A JPH0374327 A JP H0374327A
- Authority
- JP
- Japan
- Prior art keywords
- cysteine
- alcohol
- administration
- accelerator
- ingestion
- 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.)
- Pending
Links
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 title claims abstract description 34
- XUJNEKJLAYXESH-UWTATZPHSA-N D-Cysteine Chemical compound SC[C@@H](N)C(O)=O XUJNEKJLAYXESH-UWTATZPHSA-N 0.000 claims abstract description 17
- 229930195710 D‐cysteine Natural products 0.000 claims abstract description 17
- 230000004060 metabolic process Effects 0.000 claims abstract description 10
- 229940088594 vitamin Drugs 0.000 claims 1
- 229930003231 vitamin Natural products 0.000 claims 1
- 235000013343 vitamin Nutrition 0.000 claims 1
- 239000011782 vitamin Substances 0.000 claims 1
- 150000003722 vitamin derivatives Chemical class 0.000 claims 1
- 230000000694 effects Effects 0.000 abstract description 6
- 230000037406 food intake Effects 0.000 abstract description 6
- DPJRMOMPQZCRJU-UHFFFAOYSA-M thiamine hydrochloride Chemical compound Cl.[Cl-].CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N DPJRMOMPQZCRJU-UHFFFAOYSA-M 0.000 abstract description 6
- 229930003451 Vitamin B1 Natural products 0.000 abstract description 5
- 229960003495 thiamine Drugs 0.000 abstract description 5
- 239000011691 vitamin B1 Substances 0.000 abstract description 5
- 235000010374 vitamin B1 Nutrition 0.000 abstract description 5
- 150000003839 salts Chemical class 0.000 abstract description 4
- 208000007848 Alcoholism Diseases 0.000 abstract description 3
- 201000007930 alcohol dependence Diseases 0.000 abstract description 3
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 abstract description 3
- 235000018417 cysteine Nutrition 0.000 abstract description 3
- 239000004480 active ingredient Substances 0.000 abstract description 2
- 230000002265 prevention Effects 0.000 abstract description 2
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 description 28
- 239000008280 blood Substances 0.000 description 9
- 210000004369 blood Anatomy 0.000 description 9
- QNAYBMKLOCPYGJ-UHFFFAOYSA-N D-alpha-Ala Natural products CC([NH3+])C([O-])=O QNAYBMKLOCPYGJ-UHFFFAOYSA-N 0.000 description 4
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 4
- QNAYBMKLOCPYGJ-UWTATZPHSA-N L-Alanine Natural products C[C@@H](N)C(O)=O QNAYBMKLOCPYGJ-UWTATZPHSA-N 0.000 description 3
- 241000699670 Mus sp. Species 0.000 description 3
- 229960003767 alanine Drugs 0.000 description 3
- 235000002639 sodium chloride Nutrition 0.000 description 3
- PWKSKIMOESPYIA-UHFFFAOYSA-N 2-acetamido-3-sulfanylpropanoic acid Chemical compound CC(=O)NC(CS)C(O)=O PWKSKIMOESPYIA-UHFFFAOYSA-N 0.000 description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 2
- 229930003270 Vitamin B Natural products 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 235000013334 alcoholic beverage Nutrition 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 231100000419 toxicity Toxicity 0.000 description 2
- 230000001988 toxicity Effects 0.000 description 2
- 235000019156 vitamin B Nutrition 0.000 description 2
- 239000011720 vitamin B Substances 0.000 description 2
- NGNBDVOYPDDBFK-UHFFFAOYSA-N 2-[2,4-di(pentan-2-yl)phenoxy]acetyl chloride Chemical class CCCC(C)C1=CC=C(OCC(Cl)=O)C(C(C)CCC)=C1 NGNBDVOYPDDBFK-UHFFFAOYSA-N 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 206010067125 Liver injury Diseases 0.000 description 1
- 241000699666 Mus <mouse, genus> Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 230000007059 acute toxicity Effects 0.000 description 1
- 231100000403 acute toxicity Toxicity 0.000 description 1
- 229940024606 amino acid Drugs 0.000 description 1
- 235000001014 amino acid Nutrition 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- -1 ampoules Substances 0.000 description 1
- 239000000729 antidote Substances 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 239000003925 fat Substances 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 150000004665 fatty acids Chemical class 0.000 description 1
- 238000004817 gas chromatography Methods 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 231100000234 hepatic damage Toxicity 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 230000008818 liver damage Effects 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 210000003200 peritoneal cavity Anatomy 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 239000007940 sugar coated tablet Substances 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000019190 thiamine hydrochloride Nutrition 0.000 description 1
- 239000011747 thiamine hydrochloride Substances 0.000 description 1
- 229960000344 thiamine hydrochloride Drugs 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
【発明の詳細な説明】
〔産業上の利用分野〕
本発明は、アルコール摂取時のアルコールの代謝を促進
する新規アルコール代謝促進剤に関する。DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to a novel alcohol metabolism promoter that promotes alcohol metabolism during alcohol intake.
アルコール飲料は広く嗜好されているが、その一方で、
アルコールを摂取すると血中アセトアルデヒドが増加し
、急性中毒症状を示したり、長期のアルコール摂取によ
るアルコール症さらには肝障害を引き起こす。このため
、アルコール飲料を健康的に摂取するためには、アルコ
ールおよびその代謝物のアセ１〜アルデヒドが速やかに
代謝されることか望ましい。Alcoholic beverages are widely enjoyed, but on the other hand,
When alcohol is consumed, acetaldehyde increases in the blood, leading to symptoms of acute toxicity, and long-term alcohol consumption can lead to alcoholism and even liver damage. Therefore, in order to consume alcoholic beverages in a healthy manner, it is desirable that alcohol and its metabolites, ace-aldehydes, be metabolized quickly.
Ｄ−ベニシラξンに代表されるＳ Ｈ基を有する化合物
がアルコール代謝に影響を与え、特にアセトアルデヒド
の血中濃度を低下させることが報告されている（Ｈ４ｒ
ａｙａｍａ＋ Ｃｒ、 ｅｔ ａｌ、： Ｂｉｏｃｈ
ｅｍ。It has been reported that compounds with an S H group, represented by D-benicylane, affect alcohol metabolism, and in particular reduce the blood concentration of acetaldehyde (H4r
ayama+ Cr, et al: Bioch
em.
Ｐｈａｒｍａｃｏｌ、、 ３ ２． ３ ２ １
−３ ２ ５ （１９８３） 。Pharmacol, 3 2. 3 2 1
-3 2 5 (1983).
Ｃｅｄｅｒｂａｕｍ Ａ、１． ｅｔ ａｌ：
Ｂｉｏｃｈｅｍ、 Ｐｈａｒ−ｍａｃｏｌ。Cederbaum A, 1. et al:
Biochem, Phar-macol.
２５−２２１７９１１８５（１９８５）参照）。25-221791185 (1985)).
また、Ｌ−システイン、アスコルヒン酸、塩酸チアミン
を含有してなるアセトアルデヒドの解毒剤が開発されて
いる（特開昭６２−２７７３２５号公報参照）。Furthermore, an antidote for acetaldehyde containing L-cysteine, ascorhinic acid, and thiamine hydrochloride has been developed (see Japanese Patent Laid-Open No. 277325/1983).
一方、Ｌ−α−アラニンを有効成分とするアセトアルデ
ヒドの毒性抑制剤についても開発されている（特開昭６
１−１．３４３１３号公報参照）。On the other hand, an acetaldehyde toxicity inhibitor containing L-α-alanine as an active ingredient has also been developed (Japanese Unexamined Patent Publication No. 6
1-1.34313).
本発明は、アルコール代謝を効果的に促進する新規促進
剤を開発することを目的とする。The purpose of the present invention is to develop a new promoter that effectively promotes alcohol metabolism.
本発明者らは、上記課題を解決するために、種種の検討
を行った結果、Ｄ−システインが優れたアルコール代謝
従列効果を有することを見い出し、本発明を完成するに
到った。Ｄ−システインのアルコール代謝促進効果はビ
タミンＢ１を共存せしめることにより相乗的に上昇する
。In order to solve the above problems, the present inventors conducted various studies, and as a result, they discovered that D-cysteine has an excellent alcohol metabolism-enhancing effect, and completed the present invention. The alcohol metabolism promoting effect of D-cysteine is synergistically increased by coexisting with vitamin B1.
本発明の促進剤の投与は、アルコールの摂取前、同時、
摂取後のいずれであってもよいが、とりわけアルコール
の摂取前が好ましい。The enhancer of the present invention can be administered before, simultaneously with, or at the same time as alcohol intake.
It may be done either after ingestion, but it is particularly preferable before ingestion of alcohol.
Ｄ−システインは医薬上許容される塩の形態であっても
よい。D-cysteine may be in the form of a pharmaceutically acceptable salt.
本発明の促進剤は、経口的にまたは非経口的に適用され
得る。経口投与用には例えば、散剤、顆粒、錠剤、糖衣
錠、カプセル、液剤等、非経口投与用には例えば、懸濁
液、液剤、乳剤、アンプル及び注射液等が挙げられ、或
いは、これらを組合わせた形態でも提供できる。組合せ
得る希釈剤としては、固体、半固体及び液体のいずれで
もよく、例えば、水、ゼラチン、Ｗ類、澱粉類、脂肪酸
、その塩、アルコール、油脂、タルク、生理食塩水等ま
たはこれらの２種以上の組合せが挙げられる。The promoters of the invention may be applied orally or parenterally. For oral administration, examples include powders, granules, tablets, sugar-coated tablets, capsules, liquids, etc. For parenteral administration, examples include suspensions, solutions, emulsions, ampoules, injections, etc., or combinations thereof. Can also be provided in a combined format. Diluents that can be combined may be solid, semi-solid, or liquid, such as water, gelatin, Ws, starches, fatty acids, salts thereof, alcohol, fats and oils, talc, physiological saline, etc., or two of these. Combinations of the above may be mentioned.
本発明の促進剤において、Ｄ−システイン及び／または
その塩の総重量が占める比率は一般に０６０１〜１００
重量％である。In the accelerator of the present invention, the ratio of the total weight of D-cysteine and/or its salt is generally from 0.601 to 100.
Weight%.
底入１日当りの投与量は、体重、症状により異なるが、
Ｄ−システインとして２００■を最大限とする。The daily dose for bottoming out varies depending on body weight and symptoms, but
The maximum amount of D-cysteine is 200 μ.
本発明の組成物はアルコール摂取前に投与することによ
り、アルコール代謝を著しく効果的に促進するが、アル
コール症の予防・治療にも使用される。The composition of the present invention, when administered before alcohol intake, significantly and effectively promotes alcohol metabolism, and can also be used for the prevention and treatment of alcoholism.
以下、実施例により、本発明をさらに詳しく説明する。EXAMPLES Hereinafter, the present invention will be explained in more detail with reference to Examples.
実施例１ マウス死亡率に及ぼす影響
ＩＣＲ系雄性マウス（６週令）１０匹を用い、２０時時
間量後、表１に示す被験物質を０．３％カルボキシメチ
ルセルロース（ＣＭＣ）に懸濁して腹腔内投与した。１
時間後にエタノールの代謝物であるアセトアルデヒドＩ
ＯｍｍｏＡ！ ／ ｋｇを腹腔内に投与し、投与後２
４時間の生存マウス数を調べた。結果を表１に合わせて
示した。Example 1 Effect on mouse mortality rate Using 10 male ICR mice (6 weeks old), after 20 hours, the test substance shown in Table 1 was suspended in 0.3% carboxymethyl cellulose (CMC) and injected into the peritoneal cavity. Administered intravenously. 1
Acetaldehyde I, a metabolite of ethanol, after hours
OmmoA! / kg intraperitoneally, 2 days after administration.
The number of surviving mice for 4 hours was determined. The results are shown in Table 1.
対照群の０．３％ＣＭＣのみを投与した群では、アセト
アルデヒド投与後３０分以内にｌＯ例中９例が死亡し、
２４時間以内に金側死亡した。これに対し、Ｄ−システ
イン投与群またはＤ−システインおよびビタミンＢ１投
与群の生存率は著しく増加しており、アセトアルデヒド
の毒性を軽減する作用があることを示している。In the control group, in which only 0.3% CMC was administered, 9 out of 10 cases died within 30 minutes after acetaldehyde administration;
Kim died within 24 hours. On the other hand, the survival rate of the D-cysteine administration group or the D-cysteine and vitamin B1 administration group was significantly increased, indicating that there is an effect of reducing the toxicity of acetaldehyde.
実施例２ 血中アルコール、アセトアルデヒド濃度に及
ぼず影響
ＩＣＲ系雄性マウス（１０週令）６匹を用い、ア多ノ酸
（Ｌ−アラニン、■、−システイン、Ｄシスティン）を
各々２０１■窒素／ ｋｇとなるように腹腔内投与した
。アミノ酸投与１時間後にエタノール（２０ｗ／ｖ％？
容液）を２ｇ／ｋｇとなるように経口投与した。エタノ
ール投与１時間後に血中アルコールおよびアセトアルデ
ヒド濃度を測定した。測定は、ｒＰｅｒｋｉｎ−Ｅｌｍ
ｅｒ Ｆ ４５ Ｊガスクロマトグラフィーにて行った
。結果を表２に示した。Example 2 No effect on blood alcohol and acetaldehyde concentrations Using 6 male ICR mice (10 weeks old), apolino acids (L-alanine, ■, -cysteine, and D-cysteine) were each administered at 201■ nitrogen/ kg was administered intraperitoneally. One hour after amino acid administration, ethanol (20w/v%?
The solution was orally administered at a dose of 2 g/kg. Blood alcohol and acetaldehyde concentrations were measured 1 hour after ethanol administration. Measurements were made using rPerkin-Elm
er F45J gas chromatography. The results are shown in Table 2.
Ｌ−アラニン、Ｌ−アラニンおよびビタミンＢ１投与群
では、血中エタノール、血中アセトアルデヒド濃度共に
対照群に比し差が認められなかった。In the L-alanine, L-alanine, and vitamin B1 administration groups, no difference was observed in blood ethanol and blood acetaldehyde concentrations compared to the control group.
Ｌ−システイン、Ｉ５−システインおよびビタミンＢ１
投与群では血中エタノール、血中アセトアルデヒド濃度
共に対照群に比し低下した。L-cysteine, I5-cysteine and vitamin B1
In the treated group, blood ethanol and blood acetaldehyde concentrations were both lower than in the control group.
一方、Ｄ−システイン、Ｄ−システインおよびビタミン
Ｂ＋投与群においても血中エタノール濃度は対照群に比
し低下したが、この低下度は■、システィンより大きく
、Ｄ−システインおよびビタミンＢ、投与群では、対照
群の約１／２の値を示した。アセトアルデヒド濃度は対
照群に比し、むしろ高値であったが、実施例１の結果と
合わせて考えると、Ｄ−システインの投与により、より
多くの結合型アセトアルデヒドが増加しており、これを
観察していると考えられ、このことは、■〕システィン
ばアセトアルデヒドに対しより大きな親和性を示し、結
合体を生成することにより体内への吸収をブロフクし、
代謝を促進していることを示唆している。On the other hand, the blood ethanol concentration in the D-cysteine, D-cysteine, and vitamin B + administration group also decreased compared to the control group, but the degree of decrease was greater than in the D-cysteine, vitamin B, and cysteine administration group. , the value was about 1/2 that of the control group. The acetaldehyde concentration was rather high compared to the control group, but when considered together with the results of Example 1, more bound acetaldehyde increased with the administration of D-cysteine, which was observed. This means that ■] cysteine has a greater affinity for acetaldehyde and blocks its absorption into the body by forming a conjugate;
This suggests that it promotes metabolism.
以上のように、本発明の促進剤はアルコール代謝を効果
的に促進することができ、医薬上、有用である。As described above, the promoter of the present invention can effectively promote alcohol metabolism and is pharmaceutically useful.
Claims (2)
コール代謝促進剤。(1) An alcohol metabolism promoter characterized by containing D-cysteine.
ことを特徴とする請求項１記載の促進剤。(2) The promoter according to claim 1, which contains D-cysteine and vitamin B_1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1211064A JPH0374327A (en) | 1989-08-16 | 1989-08-16 | Excitometabolic agent for alcohol |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP1211064A JPH0374327A (en) | 1989-08-16 | 1989-08-16 | Excitometabolic agent for alcohol |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JPH0374327A true JPH0374327A (en) | 1991-03-28 |
Family
ID=16599803
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP1211064A Pending JPH0374327A (en) | 1989-08-16 | 1989-08-16 | Excitometabolic agent for alcohol |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH0374327A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002036098A1 (en) * | 2000-10-30 | 2002-05-10 | Licentia Ltd | Method and preparation for binding acetaldehyde in saliva, stomach and large intestine |
| US8227513B2 (en) | 2005-04-01 | 2012-07-24 | Biohit Oyj | Food composition for binding acetaldehyde in mouth and in digestive track, and method for the preparation of the composition |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS62277325A (en) * | 1986-02-18 | 1987-12-02 | Takeda Chem Ind Ltd | Antidote for acetaldehyde |
-
1989
- 1989-08-16 JP JP1211064A patent/JPH0374327A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS62277325A (en) * | 1986-02-18 | 1987-12-02 | Takeda Chem Ind Ltd | Antidote for acetaldehyde |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002036098A1 (en) * | 2000-10-30 | 2002-05-10 | Licentia Ltd | Method and preparation for binding acetaldehyde in saliva, stomach and large intestine |
| JP2004512353A (en) * | 2000-10-30 | 2004-04-22 | ライセンティア・リミテッド | Methods and formulations for binding acetaldehyde in saliva, stomach, colon |
| US9474733B2 (en) | 2000-10-30 | 2016-10-25 | Biohit Oyj | Method and preparation for binding acetaldehyde in saliva, stomach and large intestine |
| US8227513B2 (en) | 2005-04-01 | 2012-07-24 | Biohit Oyj | Food composition for binding acetaldehyde in mouth and in digestive track, and method for the preparation of the composition |
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