JPH03264534A - Agent for suppressing absorption of alcohol - Google Patents
Agent for suppressing absorption of alcoholInfo
- Publication number
- JPH03264534A JPH03264534A JP2065056A JP6505690A JPH03264534A JP H03264534 A JPH03264534 A JP H03264534A JP 2065056 A JP2065056 A JP 2065056A JP 6505690 A JP6505690 A JP 6505690A JP H03264534 A JPH03264534 A JP H03264534A
- Authority
- JP
- Japan
- Prior art keywords
- alcohol
- powder
- extract
- agent
- blood
- 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
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 title claims abstract description 93
- 238000010521 absorption reaction Methods 0.000 title claims abstract description 21
- 239000000843 powder Substances 0.000 claims abstract description 24
- 239000000284 extract Substances 0.000 claims abstract description 20
- 244000068988 Glycine max Species 0.000 claims abstract description 12
- 235000010469 Glycine max Nutrition 0.000 claims abstract description 12
- 239000001397 quillaja saponaria molina bark Substances 0.000 claims abstract description 11
- 229930182490 saponin Natural products 0.000 claims abstract description 11
- 150000007949 saponins Chemical class 0.000 claims abstract description 11
- 235000015468 Lycium chinense Nutrition 0.000 claims abstract description 8
- PHIQHXFUZVPYII-UHFFFAOYSA-N carnitine Chemical compound C[N+](C)(C)CC(O)CC([O-])=O PHIQHXFUZVPYII-UHFFFAOYSA-N 0.000 claims description 30
- 229960000678 carnitine chloride Drugs 0.000 claims description 30
- 235000008434 ginseng Nutrition 0.000 claims description 19
- 235000005035 Panax pseudoginseng ssp. pseudoginseng Nutrition 0.000 claims description 16
- 235000003140 Panax quinquefolius Nutrition 0.000 claims description 16
- 241000411851 herbal medicine Species 0.000 claims description 10
- 241000332371 Abutilon x hybridum Species 0.000 claims description 8
- 235000015459 Lycium barbarum Nutrition 0.000 claims description 7
- 239000003112 inhibitor Substances 0.000 claims description 5
- 239000004480 active ingredient Substances 0.000 claims description 4
- 244000241838 Lycium barbarum Species 0.000 claims 1
- 244000131316 Panax pseudoginseng Species 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 15
- 229940079593 drug Drugs 0.000 abstract description 14
- 239000003795 chemical substances by application Substances 0.000 abstract description 13
- 230000000694 effects Effects 0.000 abstract description 12
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 abstract description 9
- 244000241872 Lycium chinense Species 0.000 abstract description 8
- 230000003247 decreasing effect Effects 0.000 abstract description 7
- 210000001035 gastrointestinal tract Anatomy 0.000 abstract description 7
- PHIQHXFUZVPYII-ZCFIWIBFSA-N (R)-carnitine Chemical compound C[N+](C)(C)C[C@H](O)CC([O-])=O PHIQHXFUZVPYII-ZCFIWIBFSA-N 0.000 abstract description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 abstract description 4
- 235000001014 amino acid Nutrition 0.000 abstract description 3
- 150000001413 amino acids Chemical class 0.000 abstract description 3
- 235000002639 sodium chloride Nutrition 0.000 abstract description 3
- 235000013343 vitamin Nutrition 0.000 abstract description 3
- 239000011782 vitamin Substances 0.000 abstract description 3
- 229940088594 vitamin Drugs 0.000 abstract description 3
- 229930003231 vitamin Natural products 0.000 abstract description 3
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 abstract description 2
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 abstract description 2
- 229960004203 carnitine Drugs 0.000 abstract description 2
- 239000001630 malic acid Substances 0.000 abstract description 2
- 235000011090 malic acid Nutrition 0.000 abstract description 2
- 239000011780 sodium chloride Substances 0.000 abstract description 2
- 235000013399 edible fruits Nutrition 0.000 abstract 2
- 208000007848 Alcoholism Diseases 0.000 abstract 1
- 235000003174 Panax japonicus Nutrition 0.000 abstract 1
- 241000168720 Panax japonicus Species 0.000 abstract 1
- 244000274050 Platycodon grandiflorum Species 0.000 abstract 1
- 235000006753 Platycodon grandiflorum Nutrition 0.000 abstract 1
- 241001078983 Tetradium ruticarpum Species 0.000 abstract 1
- 201000007930 alcohol dependence Diseases 0.000 abstract 1
- 235000015165 citric acid Nutrition 0.000 abstract 1
- 235000019441 ethanol Nutrition 0.000 description 82
- 239000008280 blood Substances 0.000 description 35
- 210000004369 blood Anatomy 0.000 description 35
- 240000004371 Panax ginseng Species 0.000 description 18
- 239000000203 mixture Substances 0.000 description 13
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 13
- 238000002474 experimental method Methods 0.000 description 11
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 9
- 241000700159 Rattus Species 0.000 description 9
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 9
- 239000007864 aqueous solution Substances 0.000 description 8
- 230000002401 inhibitory effect Effects 0.000 description 8
- 239000012153 distilled water Substances 0.000 description 6
- 239000004615 ingredient Substances 0.000 description 6
- 206010019133 Hangover Diseases 0.000 description 5
- 239000002775 capsule Substances 0.000 description 5
- 238000009472 formulation Methods 0.000 description 5
- 230000007661 gastrointestinal function Effects 0.000 description 5
- 210000002784 stomach Anatomy 0.000 description 5
- 230000001988 toxicity Effects 0.000 description 5
- 231100000419 toxicity Toxicity 0.000 description 5
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 description 4
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 4
- 231100000673 dose–response relationship Toxicity 0.000 description 4
- 235000020710 ginseng extract Nutrition 0.000 description 4
- 230000005764 inhibitory process Effects 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 230000004060 metabolic process Effects 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- 235000002789 Panax ginseng Nutrition 0.000 description 3
- IKHGUXGNUITLKF-XPULMUKRSA-N acetaldehyde Chemical compound [14CH]([14CH3])=O IKHGUXGNUITLKF-XPULMUKRSA-N 0.000 description 3
- 238000010171 animal model Methods 0.000 description 3
- 239000008187 granular material Substances 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 239000002207 metabolite Substances 0.000 description 3
- 230000002829 reductive effect Effects 0.000 description 3
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- 239000004471 Glycine Substances 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 2
- 229930006000 Sucrose Natural products 0.000 description 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 2
- 206010000059 abdominal discomfort Diseases 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 235000013334 alcoholic beverage Nutrition 0.000 description 2
- 230000001476 alcoholic effect Effects 0.000 description 2
- 150000001412 amines Chemical class 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- 230000037406 food intake Effects 0.000 description 2
- 239000003205 fragrance Substances 0.000 description 2
- 230000006870 function Effects 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 229960002449 glycine Drugs 0.000 description 2
- PCHJSUWPFVWCPO-UHFFFAOYSA-N gold Chemical compound [Au] PCHJSUWPFVWCPO-UHFFFAOYSA-N 0.000 description 2
- 239000010931 gold Substances 0.000 description 2
- 229910052737 gold Inorganic materials 0.000 description 2
- 230000009931 harmful effect Effects 0.000 description 2
- 230000002440 hepatic effect Effects 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 210000004185 liver Anatomy 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 235000015097 nutrients Nutrition 0.000 description 2
- 235000016709 nutrition Nutrition 0.000 description 2
- VLTRZXGMWDSKGL-UHFFFAOYSA-N perchloric acid Chemical compound OCl(=O)(=O)=O VLTRZXGMWDSKGL-UHFFFAOYSA-N 0.000 description 2
- 230000001629 suppression Effects 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- LKAPTZKZHMOIRE-KVTDHHQDSA-N (2s,3s,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolane-2-carbaldehyde Chemical compound OC[C@H]1O[C@H](C=O)[C@@H](O)[C@@H]1O LKAPTZKZHMOIRE-KVTDHHQDSA-N 0.000 description 1
- 206010002091 Anaesthesia Diseases 0.000 description 1
- 208000000412 Avitaminosis Diseases 0.000 description 1
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical class [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 1
- 206010014418 Electrolyte imbalance Diseases 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 1
- 241000272168 Laridae Species 0.000 description 1
- 241001106041 Lycium Species 0.000 description 1
- 206010025476 Malabsorption Diseases 0.000 description 1
- 208000004155 Malabsorption Syndromes Diseases 0.000 description 1
- 240000000249 Morus alba Species 0.000 description 1
- 235000008708 Morus alba Nutrition 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 206010047627 Vitamin deficiencies Diseases 0.000 description 1
- 230000003187 abdominal effect Effects 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 235000004279 alanine Nutrition 0.000 description 1
- 230000037005 anaesthesia Effects 0.000 description 1
- 229940069428 antacid Drugs 0.000 description 1
- 239000003159 antacid agent Substances 0.000 description 1
- 230000001458 anti-acid effect Effects 0.000 description 1
- 230000001142 anti-diarrhea Effects 0.000 description 1
- 230000004596 appetite loss Effects 0.000 description 1
- 239000006286 aqueous extract Substances 0.000 description 1
- 230000000035 biogenic effect Effects 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 238000009395 breeding Methods 0.000 description 1
- 230000001488 breeding effect Effects 0.000 description 1
- 239000001569 carbon dioxide Substances 0.000 description 1
- 229910002092 carbon dioxide Inorganic materials 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- LKAPTZKZHMOIRE-UHFFFAOYSA-N chitose Natural products OCC1OC(C=O)C(O)C1O LKAPTZKZHMOIRE-UHFFFAOYSA-N 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 235000020931 dietary conditions Nutrition 0.000 description 1
- 235000018823 dietary intake Nutrition 0.000 description 1
- JXSJBGJIGXNWCI-UHFFFAOYSA-N diethyl 2-[(dimethoxyphosphorothioyl)thio]succinate Chemical compound CCOC(=O)CC(SP(=S)(OC)OC)C(=O)OCC JXSJBGJIGXNWCI-UHFFFAOYSA-N 0.000 description 1
- 230000029087 digestion Effects 0.000 description 1
- 230000001079 digestive effect Effects 0.000 description 1
- 231100000676 disease causative agent Toxicity 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 208000035475 disorder Diseases 0.000 description 1
- 238000001647 drug administration Methods 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 210000001198 duodenum Anatomy 0.000 description 1
- 238000006911 enzymatic reaction Methods 0.000 description 1
- 239000010419 fine particle Substances 0.000 description 1
- 235000012631 food intake Nutrition 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- ZFGMDIBRIDKWMY-PASTXAENSA-N heparin Chemical compound CC(O)=N[C@@H]1[C@@H](O)[C@H](O)[C@@H](COS(O)(=O)=O)O[C@@H]1O[C@@H]1[C@@H](C(O)=O)O[C@@H](O[C@H]2[C@@H]([C@@H](OS(O)(=O)=O)[C@@H](O[C@@H]3[C@@H](OC(O)[C@H](OS(O)(=O)=O)[C@H]3O)C(O)=O)O[C@@H]2O)CS(O)(=O)=O)[C@H](O)[C@H]1O ZFGMDIBRIDKWMY-PASTXAENSA-N 0.000 description 1
- 229920000669 heparin Polymers 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 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
- 230000000968 intestinal effect Effects 0.000 description 1
- 230000001788 irregular Effects 0.000 description 1
- 238000002350 laparotomy Methods 0.000 description 1
- 238000012417 linear regression Methods 0.000 description 1
- 235000021266 loss of appetite Nutrition 0.000 description 1
- 208000019017 loss of appetite Diseases 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 235000012054 meals Nutrition 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000035764 nutrition Effects 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- 239000003646 toxicity reducer Substances 0.000 description 1
- 210000002438 upper gastrointestinal tract Anatomy 0.000 description 1
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
Description
【発明の詳細な説明】
（産業上の利用分野）
本発明はチクセツニンジン、ゴシュユ、キキョウおよび
クコシからなる群から選ばれる生薬粉末またはエキス、
ダイズサポニンおよび塩化カルニチンのいずれか１種ま
たは２種以上を有効成分とするアルコール吸収抑制剤に
関する。DETAILED DESCRIPTION OF THE INVENTION (Industrial Application Field) The present invention provides herbal medicine powders or extracts selected from the group consisting of ginseng, goshuyu, bellflower, and wolfberry;
The present invention relates to an alcohol absorption inhibitor containing one or more of soybean saponin and carnitine chloride as active ingredients.
本発明者らは、チクセツニンジン並びにゴシュユの生薬
粉末またはエキス、および塩化カルニチンから選ばれる
健胃剤に、アルコール吸収抑制効果のあることを見い出
し、次いで、健胃剤ではないが、キキョウ並びにクコシ
の生薬粉末またはエキス、およびダイズサポニンにも同
様の作用がみられることを見い出した。以下、健胃剤と
して有用なチクセツニンジン、ゴシュユ、および塩化カ
ルニチンについてまず説明し、最後にキキョウ、クコシ
およびダイズサポニンについて説明する。The present inventors discovered that a stomachic agent selected from ginseng and goshuyu crude drug powder or extract, and carnitine chloride has an alcohol absorption suppressing effect. It was found that similar effects were found in extracts and soybean saponin. Hereinafter, ginseng, goshuyu, and carnitine chloride, which are useful as stomachic agents, will be explained first, and finally, bellflower, wolfberry, and soybean saponin will be explained.
チクセツニンジン、ゴシュユまたは塩化カルニチンを含
有する本発明に係る製剤は、胃腸機能改善作用に加えて
、アルコールの消化管吸収を抑制することにより血中の
アルコール濃度の上昇を防ぎ、飲酒による弊害から生体
を防御するものである。The preparation according to the present invention containing ginseng, goshuyu or carnitine chloride not only improves gastrointestinal function, but also suppresses the absorption of alcohol in the gastrointestinal tract, thereby preventing an increase in blood alcohol concentration and preventing the harmful effects of drinking alcohol. It protects the living body.
（従来の技術）
アルコール飲料として経口的に摂取されたエタノールは
、胃、十二指腸、小腸を主体とする消化管を通して吸収
された後、血液を通じ全身へ運搬される。吸収されたア
ルコールは９０％が肝臓で酵素反応により酸化され、ま
ずアセトアルデヒドに、次に酢酸へと代謝され、最終的
には水と炭酸ガスになる。いわゆる酩酊の発現にはアル
コールの直接作用の他、その代謝産物であるアセトアル
デヒドや電解質のアンバランス、生体アミン等が複雑に
関係しているものと考えられている。(Prior Art) Ethanol ingested orally as an alcoholic beverage is absorbed through the gastrointestinal tract, which mainly consists of the stomach, duodenum, and small intestine, and then is transported throughout the body through the blood. 90% of the absorbed alcohol is oxidized by enzymatic reactions in the liver, first metabolized to acetaldehyde, then to acetic acid, and finally to water and carbon dioxide. In addition to the direct effects of alcohol, the onset of so-called drunkenness is thought to be complicatedly related to its metabolite acetaldehyde, electrolyte imbalance, biogenic amines, etc.
中でも薬理作用の強いアセトアルデヒドは悪酔いの原因
物質と言われており、アセトアルデヒドのトラップ剤や
毒性軽減剤あるいは代謝促進剤などが種々報告されてい
る。また、悪酔いや二日酔いによる胃腸の不快症状の改
善には従来から種々の健胃剤の複合剤か用いられている
。Among them, acetaldehyde, which has a strong pharmacological effect, is said to be a causative agent of drunkenness, and various acetaldehyde trapping agents, toxicity reducers, and metabolism promoters have been reported. In addition, a combination of various stomach-promoting agents has been used to improve gastrointestinal discomfort caused by a hangover or a hangover.
（発明が解決しようとする課題）
本発明者は、アルコール飲料を健康的に飲むためにはア
ルコール自体とその代謝産物であるアセトアルデヒドの
毒性による生体への不都合な作用をいずれも低下もしく
は中和させることが望ましいと考え、そのためには消化
管からのアルコール吸収を阻害することにより、血中ア
ルコール濃度の上昇を抑制する薬剤が効果的であると考
えた。(Problems to be Solved by the Invention) The present inventors believe that in order to drink alcoholic beverages in a healthy manner, it is necessary to reduce or neutralize the harmful effects on living organisms caused by the toxicity of alcohol itself and its metabolite, acetaldehyde. To this end, they believed that a drug that suppresses the increase in blood alcohol concentration by inhibiting alcohol absorption from the gastrointestinal tract would be effective.
また、アルコール及びアルコールの代謝か肝臓における
各種栄養素やビタミンの代謝に悪影響を及ぼすことはよ
く知られている（本明細書の末尾に列挙した文献４．５
．６）が、実際のところ、栄養条件の悪化には食事条件
の変動も大きな要因となり得る（文献７）。すなわち、
アルコールの過剰摂取は食事摂取を不規則にし、食欲の
減退、食事摂取量の減少を引き起こし、さらにアルコー
ルによる上部消化管障害により消化吸収不良が起こり、
栄養素やビタミンの不足を招くと考えられている。従っ
て、健胃剤をアルコール摂取後に服用して胃腸の不快症
状を改善するのも有効であるか、アルコール摂取前に服
用して栄養摂取条件を良好にすることも非常に有効であ
る。In addition, it is well known that alcohol and its metabolism have an adverse effect on the metabolism of various nutrients and vitamins in the liver (References 4 and 5 listed at the end of this specification).
．． 6) However, in reality, fluctuations in dietary conditions can also be a major factor in the deterioration of nutritional conditions (Reference 7). That is,
Excessive consumption of alcohol causes irregular meal intake, resulting in loss of appetite and decreased food intake.Also, alcohol-induced upper gastrointestinal tract disorders cause digestive malabsorption.
It is believed that this can lead to nutrient and vitamin deficiencies. Therefore, it is also effective to take a stomachic agent after ingesting alcohol to improve gastrointestinal discomfort symptoms, or it is very effective to take it before ingesting alcohol to improve nutritional intake conditions.
しかし、健胃剤によってはアルコール摂取前に投与して
もアルコール吸収に何等影響を及ぼさないもの、また逆
にアルコール吸収を促進してアルコールの毒性を強める
ものも有り得ることから、むやみに健胃剤を服用しても
アルコールの毒性防御に有効であるとは言い難い。本発
明者はその点に着目し、消化管機能とアルコール毒性の
両面から生体を防御し得る薬剤を得る目的で、健胃剤成
分の中で血中アルコール濃度の上昇を抑制し得る成分を
種々検索した。However, some stomach medicines have no effect on alcohol absorption even if administered before alcohol intake, while others may promote alcohol absorption and make alcohol more toxic. However, it is difficult to say that it is effective in protecting against alcohol toxicity. The present inventor focused on this point, and conducted a search for various ingredients that can suppress the increase in blood alcohol concentration among the ingredients of stomach-promoting medicines, with the aim of obtaining a drug that can protect the living body from both gastrointestinal function and alcohol toxicity. .
（課題を解決するための手段）
その結果、健胃剤成分のうち、チクセツニンジン及びゴ
シーユの生薬粉末またはエキス、および塩化カルニチン
に、アルコール摂取後の血中アルコール濃度の上昇を抑
制する作用のあること、すなわち消化管からのアルコー
ル吸収を抑制することにより血中へのアルコール移行量
を減少させることが明らかとなった。従ってこれらの健
胃剤成分を投与すれば、健胃作用による消化管機能の調
節と同時にアルコール及びその代謝物の毒性から生体を
極めて有効に防御し得ると考えられる。(Means for solving the problem) As a result, it was found that among the ingredients of the stomach medicine, the herbal medicine powders or extracts of ginseng and gosille, and carnitine chloride have the effect of suppressing the increase in blood alcohol concentration after alcohol intake. In other words, it has been revealed that by suppressing alcohol absorption from the gastrointestinal tract, the amount of alcohol transferred into the bloodstream is reduced. Therefore, it is considered that by administering these ingredients, it is possible to regulate the functions of the gastrointestinal tract through the stomachic effect, and at the same time, to extremely effectively protect the living body from the toxicity of alcohol and its metabolites.
本明細書において、「生薬粉末またはエキス」なる用語
は、生薬を本来の目的に使用する場合の通常の型態を意
味し、従って、字句通りの特定の型態を指すものとして
理解されてはならない。即ち、生薬粉末は、例えば微粒
状、顆粒状に加工されたもの、あるいは、いわゆる「生
のもの」および「刻み」なども包含し、又、エキスは、
水性エキス、流エキス、チンキなども包含するが、これ
らに限定されるものではない。As used herein, the term "herbal medicine powder or extract" refers to the usual form in which the herbal medicine is used for its intended purpose, and therefore should not be understood literally as referring to a specific form. No. That is, herbal medicine powder includes, for example, those processed into fine particles or granules, or so-called "raw" and "chopped" powders, and extracts include:
It also includes, but is not limited to, aqueous extracts, liquid extracts, tinctures, and the like.
本発明の有効成分である塩化カルニチンは市販薬品から
容易に得ることができ、チクセツニンジンとゴシュユは
生薬材料として粉末あるいはエキスのいずれでも入手で
きる。塩化カルニチンは胃腸機能調整剤、チクセツニン
ジンとゴシュユは健胃生薬であるが、いずれも胃腸機能
改善作用を有し、制酸、健胃、消化、整腸、止瀉などの
種々の目的を持つ胃腸薬に配合される成分である。本発
明の製剤にはグリシン、アラニンなどのアミノ酸類、ク
エン酸、リンゴ酸などの有機酸、塩化ナトリウム、塩化
カリウムなどの無機塩類、ビタミン類、他の生薬粉末及
び抽出物、香料などを配合することができる。Carnitine chloride, which is the active ingredient of the present invention, can be easily obtained from commercially available drugs, and ginseng and goshuyu can be obtained as crude drug materials in either powder or extract form. Carnitine chloride is a gastrointestinal function regulating agent, and ginseng and goshuyu are gastrointestinal herbal medicines, both of which have the effect of improving gastrointestinal function, and are used for various purposes such as antacid, healthy stomach, digestion, intestinal regulation, and antidiarrheal function. It is an ingredient added to gastrointestinal medicines. The formulation of the present invention contains amino acids such as glycine and alanine, organic acids such as citric acid and malic acid, inorganic salts such as sodium chloride and potassium chloride, vitamins, other herbal medicine powders and extracts, fragrances, etc. be able to.
またその摂取形態として、液剤の他、粉末剤、顆粒剤、
錠剤、カプセル剤など全ての経口投与剤型が利用できる
。In addition to the liquid form, the ingestion forms include powder, granules,
All oral dosage forms such as tablets and capsules are available.
アルコールを同量飲んでもその吸収代謝速度は体重、体
質などの違いにより非常に個人差が大きく、本発明の有
効成分の有効量を明確に規定することはてきないが、上
記生薬の本来の使用目的に用いる場合の有効用量範囲で
十分なアルコール吸収抑制作用が期待できる。すなわち
、１種のみて用いる場合は、望ましくは１日服用量が塩
化カルニチンは６〜６００ ｍｙ、チクセツニンジンは
エキスの場合は０．６〜６ｇ、粉末の場合は０．３〜３
ｇ、またコシーユはエキスの場合は０．３〜３ｇ、粉末
の場合は０．１−１９を目安とし、２種以上を組み合わ
せる場合は適宜減量して用いる。また、服用時期につい
ては、アルコール摂取前または摂取と同時に服用して悪
酔いや二日酔いの予防に用いると効果的であるが、アル
コール摂取後に服用して悪酔いや二日酔いの軽減に使う
ことも可能である。Even if you drink the same amount of alcohol, the rate of absorption and metabolism varies greatly from person to person due to differences in body weight, constitution, etc., and it is not possible to clearly define the effective amount of the active ingredient of the present invention. A sufficient alcohol absorption inhibitory effect can be expected within the effective dose range when used for the intended purpose. That is, when using only one species, the daily dose is preferably 6 to 600 my for carnitine chloride, 0.6 to 6 g for ginseng extract, and 0.3 to 3 for powder.
For cosille, the amount is 0.3 to 3 g in the case of extract, and 0.1 to 19 g in the case of powder, and when two or more types are combined, the amount is reduced as appropriate. Regarding when to take it, it is effective to take it before or at the same time as alcohol intake to prevent a hangover or hangover, but it can also be taken after alcohol intake to reduce the symptoms of a hangover.
既述した通り、本発明者らは、健胃剤ではないがキキョ
ウおよびクコシの生薬粉末およびダイズサポニンにも、
同様にアルコール吸収抑制作用があることを見い出した
。これらは、いずれも市販されており、その１日服用量
は、いずれも０．３〜５ｇの範囲内である。As mentioned above, the present inventors have also used bellflower and wolfberry herbal medicine powders and soybean saponin, although they are not stomachic agents.
It was also found that it has a similar effect of inhibiting alcohol absorption. All of these are commercially available, and the daily dose for each is within the range of 0.3 to 5 g.
以下に実施例及び製剤例をあげて本発明をより詳細に説
明する。The present invention will be explained in more detail with reference to Examples and Formulation Examples below.
実験例１
（１）実験動物
Ｗｉｓｔａｒ系雄性ラットをう週間の予備飼育後、体重
１５０〜１８０ｇで使用した。実験前−晩絶食し、実験
中は絶食、細氷とした。Experimental Example 1 (1) Experimental Animals Wistar male rats were used at a weight of 150 to 180 g after preliminary breeding for one week. The subjects were fasted the night before the experiment, and were kept on ice during the experiment.
（２）実験方法
ラットをアルコール単独（蒸留水）投与群（対照群１）
、アルコール単独（１ｗ／ｖ％ＣＭＣ）投与群（対照群
２）、塩化カルニチン投与群、チクセツニンジン投与群
、ゴシーユ投与群の５群に分け、原則として■群２５例
とした。(2) Experimental method Rats were given alcohol alone (distilled water) (control group 1)
The animals were divided into 5 groups: , alcohol alone (1 w/v% CMC) administration group (control group 2), carnitine chloride administration group, ginseng administration group, and Gosille administration group, with 25 cases in principle in group Ⅰ.
アルコールはエチルアルコールヲ蒸留水で２０ｖ／ｖ％
に希釈した液を、金側に１０ ｒｔｔ（１／ ｋｇの容
量で経口投与し、被験薬はアルコール投与１時間前に以
下の通り経口投与した。すなわち、塩化カルニチンは２
０ｗ／ｖ％溶液を蒸留水にて調製し、チクセツニンジン
エキス末は２５ｗ／ｖ％、ゴシュユ末は５ｗ／ｖ％溶〆
夜を１％ＣＭＣ（カルボキシメチルセルローステ１〜リ
ウム）水溶液にて調製したものを１０ｍ（１／に９の容
量で投与した。対照群１には被験薬の代わりに蒸留水を
、また対照群２には１％ＣＭＣ水溶岐を’ｒｏｘｇ／ｋ
ｙの容量で投与した。Alcohol is 20v/v% ethyl alcohol and distilled water.
The test drug was orally administered 1 hour before alcohol administration as follows: carnitine chloride was
Prepare a 0 w/v% solution with distilled water, dissolve 25 w/v% of ginseng extract powder, and 5 w/v% of goshuyu powder. Prepare the solution with 1% CMC (carboxymethylcellulose terium-trium) aqueous solution. The mixture was administered at a volume of 10 m (1/9). Control group 1 received distilled water instead of the test drug, and control group 2 received 1% CMC water at
It was administered in a volume of y.
アルコール投与後、０．５．１．２．３．４時間目に各
群５例ずつエーテル麻酔下にて開腹し、腹部大静脈より
ヘパリンナトリウムコートの真空採血管に採血した。次
に採血した血液０．５ｍＱを、予め０．３３Ｎ過塩素酸
溶？（１，４ｍ（ｌを入れて水冷しておいた遠沈管に加
えて激しく撹拌し、４°Ｃ下で３００Ｏｒｐｍ、５分間
遠心分離し、その上清を採取した。血中アルコール濃度
はこの上清を用い、酵素法（文献８）に基つく血中アル
コールＵＶテストｒＢＭｊｊ（ヘーリンガーマンハイム
山之内）により測定した。At 0.5, 1, 2, 3, and 4 hours after the alcohol administration, 5 animals in each group underwent laparotomy under ether anesthesia, and blood was collected from the abdominal vena cava into a vacuum blood collection tube coated with sodium heparin. Next, 0.5mQ of the collected blood was pre-dissolved in 0.33N perchloric acid. (1.4 ml) was added to a water-cooled centrifuge tube, stirred vigorously, and centrifuged at 4°C for 5 minutes at 300 rpm, and the supernatant was collected. It was measured using the blood alcohol UV test rBMjj (Heringer Mannheim Yamanouchi) based on the enzyme method (Reference 8).
（３）実験結果
対照群１及び塩化カルニチン投与群の血中アルコール濃
度の時間的推移を第１図に示した。すなわち、対照群１
ではアルコール投与１時間目に血中濃度は１．５ｚ９／
ｍ＆で最高値を示し、以後漸次低下して４時間目にはほ
ぼ消失していた。一方、塩化カルニチン投与群では対照
群１のような」二昇ピークは見られず、血中濃度０．２
〜０．４ｍｇ／＋１２て殆ど横ばいの推移を示した。特
に投与２時間目までは８０％以上の有意な抑制効果（Ｐ
＜０．００１）を示し、投与３時間目においても４０％
の有意な抑制効果（ｐ＜０．０５）を示した。また比較
上、台形則をもとにしてＡＵＧ（０−４）（０〜４時間
目までの血中濃度曲線平面積）をそれぞれ計算すると、
対照群１では３．４１ ｙｎ９ ・ｈ／ｍ（！、塩化カ
ルニチン投与群では０．９９ｚ９・ｈ／ｍＱとなり、対
照群１に対する抑制率は７１％となった。従って、塩化
カルニチンの投与によりアルコールの吸収が阻害されて
血中への移行量が減少し、血中アルコール濃度が低レベ
ルに抑えられていることが示された。(3) Experimental Results Figure 1 shows the time course of blood alcohol concentration in control group 1 and carnitine chloride administration group. That is, control group 1
Then, the blood concentration was 1.5z9/1 hour after alcohol administration.
It showed the highest value at m&, then gradually decreased and almost disappeared by the 4th hour. On the other hand, in the carnitine chloride-administered group, the "two-rise peak" like that in control group 1 was not observed, and the blood concentration was 0.2.
~0.4mg/+12, showing almost a flat trend. In particular, up to the second hour of administration, there was a significant inhibitory effect of more than 80% (P
<0.001) and 40% even at 3 hours after administration.
showed a significant suppressive effect (p<0.05). For comparison, if AUG(0-4) (plane area of blood concentration curve from 0 to 4 hours) is calculated based on the trapezoidal rule,
In control group 1, it was 3.41 yn9 h/m (!, in the carnitine chloride administration group it was 0.99 yn9 h/mQ, and the inhibition rate against control group 1 was 71%. Therefore, by administering carnitine chloride, alcohol It was shown that the absorption of alcohol was inhibited and the amount transferred into the bloodstream was reduced, thereby suppressing the blood alcohol concentration to a low level.
対照群２、チクセツニンジン投与群及びコシユニ投与群
の血中アルコール濃度の時間的推移を第２図に示した。Figure 2 shows the time course of blood alcohol concentration in control group 2, the ginseng administration group, and the Koshiuni administration group.
まず、対照群２ではアルコール投与後１時間目に血中濃
度は１．２ｍｙ／ｍ（ｌて最高値を示し、以後漸次低下
して４時間目にはほぼ消失した。チクセツニンジン投与
群でも対照群２と同しような推移を示したが、投与後２
時間目までは対照群２より低い濃度て推移した。すなわ
ち０５５時間目は４２％（Ｐ＜０． ｌ Ｏ）、ピーク
の１時間目では１３％の抑制効果を示し、さらにＡＵＧ
（０−４）で比較すると、抑制率は１７％となった。一
方、ゴシュユ投与群ではピーク時間が１時間遅れ、２時
間目をピークに以後対１５．群２と同様に漸次低下した
。血中濃度抑制率は０５時間目て４１％（ｐ＜０．０５
）、１時間目で２４％（ｐ＜０、 ｌ Ｏ）を示し、Ａ
ＵＣ（０−４）の抑制率は１４％であった。以」二のこ
と力）る、チクセツニンジン及びゴシュユのいずれも本
投与量では若干効果は弱いものの、塩化カルニチンと同
様、消化管からのアルコール吸収抑制作用により血中ア
ルコール濃度を低レベルに抑えることが示された。First, in control group 2, the blood concentration reached a maximum value of 1.2 my/m (1.2 my/m) 1 hour after alcohol administration, and then gradually decreased and almost disappeared by the 4th hour. It showed a similar trend to control group 2, but after administration 2
The concentration remained lower than that of control group 2 until the 3rd hour. In other words, the inhibitory effect was 42% (P<0.lO) at 055 hours, and 13% at the peak hour 1, and furthermore, AUG
(0-4), the suppression rate was 17%. On the other hand, in the Goshuyu-administered group, the peak time was delayed by 1 hour, and the peak time was 15% after the 2nd hour. As in Group 2, it gradually decreased. The blood concentration suppression rate was 41% at 05 hours (p<0.05
), 24% (p<0, lO) at 1 hour, A
The inhibition rate of UC(0-4) was 14%. Both ginseng and goshuyu are slightly less effective at this dose, but similar to carnitine chloride, they suppress blood alcohol concentration to a low level by inhibiting alcohol absorption from the gastrointestinal tract. It was shown that
上記と同様の実験を、キキョウ、クコシ、およびダイズ
サボニンについても行った。以下にその概要を示す。Experiments similar to those described above were also conducted for bellflower, wolfberry, and soybean sabonin. The outline is shown below.
実験方法
ダイズサポニンは１０％、キキョウ流エキスは４０％、
クコシ流エキスは２０％ｌ容液を１％ＣＭＣ水溶液にて
調製したものを１０ｍＱ／ｋｇの容量で投与した。Experimental method: 10% soybean saponin, 40% bellflower extract,
A 20% l volume of the Lycium chinensis extract was prepared with a 1% CMC aqueous solution and administered at a volume of 10 mQ/kg.
対照群３には１％ＣＭＣ水溶液を１０ｘｆｆ／＆ｙの容
量で投与した。Control group 3 was administered a 1% CMC aqueous solution at a volume of 10xff/&y.
実験結果
対照群３、ダイズサポニン投与群、キキョウ投与群およ
びクコシ投与群の血中アルコール濃度の時間的推移を第
５図に示した。Experimental Results Figure 5 shows the time course of blood alcohol concentration in the control group 3, the soybean saponin administration group, the bellflower administration group, and the wolfberry administration group.
ダイズサポニンおよびクコシはアルコール投与後０５．
１時間目に血中アルコール濃度を低下し、またキキョウ
は０．５〜３時間目まで明らかに血中濃度を低下した。Soybean saponin and wolfberry were administered at 05.00 days after alcohol administration.
Blood alcohol concentration decreased at 1 hour, and bellflower clearly decreased blood alcohol concentration from 0.5 to 3 hours.
実験例２ （１）実験動物 実験例１で用いたラットと同じものを実験に供した。Experimental example 2 (1) Experimental animals The same rats used in Experimental Example 1 were used for the experiment.
（２）実験方法
本実験では胃腸機能調製剤である塩化カルニチ１
ン及び健胃生薬のうちチクセツニンジンについてアルコ
ール吸収抑制作用の用量反応を調べた。(2) Experimental method In this experiment, we investigated the dose-response of alcohol absorption inhibitory effects for carnitine chloride, a gastrointestinal function regulator, and ginseng, a herbal medicine for stomach health.
ラットをアルコール単独（蒸留水）投与群（対照群１）
、アルコール単独（ＩＷ／Ｖ％ＣＭＣ）投与群（対照群
２）、塩化カルニチン（１，０，１５，２，０，４、Ｏ
ｐｌ ｋｇ）投与群、及びチクセツニンジン（２゜５．
５．０．１０．０ｇ／ｋｇ）投与群の９群に分け、１君
Ｙ５例とした。Rats given alcohol alone (distilled water) group (control group 1)
, alcohol alone (IW/V%CMC) administration group (control group 2), carnitine chloride (1,0,15,2,0,4, O
pl kg) administration group, and ginseng (2°5.
The mice were divided into 9 groups (5.0.10.0g/kg) administration groups, with 5 cases of 1st grade.
アルコールはエチルアルコールの２０ｖ／ｖ％希釈水溶
液を金側に１０ｍＱ／ｋｇの容量て経口投与し、被験薬
はアルコール投与１時間前に以下の通り経口投与した。For alcohol, a 20 v/v% diluted aqueous solution of ethyl alcohol was orally administered to the gold side at a volume of 10 mQ/kg, and the test drug was orally administered 1 hour before alcohol administration as follows.
すなわち塩化カルニチンはｌ０１１５．２０．４０ｗ／
ｖ％水溶液を１０ｍ（１／に９の容量で投与し、チクセ
ツニンジンエキス末は２５．５０、 １００ｗ／ｖ％と
なるよう］％ＣＭＣ水溶液で調製した溶液をｒｏｔｔｔ
（１／ｋｇ投与した。対照群１のラットには被験薬の代
わりに蒸留水を、対照群２のラットには１％ＣＭＣ水ｉ
＄１ｆｆｌを１Ｃ）＋（１／に９の容量で投与した。That is, carnitine chloride is 10115.20.40w/
A solution prepared with 10 m of a v% aqueous solution (administered at a volume of 1/9, and the ginseng extract powder was 25.50% and 100w/v%) was prepared using a %CMC aqueous solution.
(1/kg was administered. Rats in control group 1 received distilled water instead of the test drug, rats in control group 2 received 1% CMC water i.
$1ffl was administered in a volume of 1C)+(1/9).
いずれの投与群もアルコール投与液１時開目に２−
実験１と同じ方法で採血し、血中アルコール濃度を測定
した。In both administration groups, blood was collected at 1:00 a.m. in the same manner as in Experiment 1, and the blood alcohol concentration was measured.
（３）実験結果
以下の表１に塩化カルニチン及びチクセツニンジンのア
ルコール投与液１時開目の血中濃度及びそれぞれの対照
群に対する抑制率を示した。また、これらの用量反応曲
線を第３図に示した。(3) Experimental Results Table 1 below shows the blood concentrations of carnitine chloride and ginseng in the alcoholic administration solution at 1 o'clock opening, and the respective inhibition rates relative to the control group. Moreover, these dose-response curves are shown in FIG.
すなわち、横軸に対数用量、縦軸に抑制率をとって表１
のデータをプロットした。その結果、塩化カルニチン及
びチクセツニンジンはいずれも用量依存的な血中アルコ
ール濃度低下作用、すなわちアルコール吸収抑制作用を
有することか明らかとなった。従って、実験例１て示し
た血中アルコール濃度の時間的推移は、ピーク時の１時
間目における血中濃度か用量依存的であることから、用
量を上げることにより、さらに低い血中濃度の推移曲線
か得られるものと予想される。また、直線回帰広により
ＥＤ５ｏを求めることか可能であり、表１に示したよう
に塩化カルニチンは１８４ｇ／ｋｇ、チクセツニンジン
エキスは３．８３１１１／に９となっている。That is, Table 1 shows the logarithmic dose on the horizontal axis and the inhibition rate on the vertical axis.
The data were plotted. As a result, it was revealed that both carnitine chloride and Panax ginseng have a dose-dependent effect of lowering blood alcohol concentration, that is, an effect of inhibiting alcohol absorption. Therefore, since the time course of blood alcohol concentration shown in Experimental Example 1 is dependent on the blood concentration in the first hour at its peak or the dose, increasing the dose will result in an even lower blood alcohol concentration. It is expected that a curved line will be obtained. It is also possible to determine the ED5o by linear regression, and as shown in Table 1, carnitine chloride is 184 g/kg, and ginseng extract is 3.83111/9.
実験例３ （１）実験動物 実験例１で用いたラットと同じものを実験に供した。Experimental example 3 (1) Experimental animals The same rats used in Experimental Example 1 were used for the experiment.
（２）実験方法
ラットをアルコール単独投与群（対照群）と塩化カルニ
チン投与ＢＹの２群に分け、前者は３０例、後者は２０
例とした。(2) Experimental method Rats were divided into two groups: an alcohol-only administration group (control group) and a carnitine chloride administration group, with 30 cases in the former and 20 cases in the latter.
As an example.
アルコールはエチルアルコールの２０ｖ／ｖ％希釈水溶
ｌ夜を金側に１０ ｙｎＱ／ｋｇの容量で経口投与した
。その１時間後に塩化カルニチン投与群には２５ｗ／ｖ
％塩化カルニチン水溶液を、対照群には蒸留水をいずれ
も１０ｙｔｔＱ／ｋｇの容量で経口投与した。As for alcohol, a 20v/v% diluted aqueous solution of ethyl alcohol was orally administered to the gold side at a dose of 10ynQ/kg. One hour later, the carnitine chloride administration group received 25 w/v.
% carnitine chloride aqueous solution and distilled water to the control group at a volume of 10 yttQ/kg.
対照群はアルコール投与後０５．１．１５．２．３．４
時間目に、被験薬投与群は１５．２．３．４時間目に、
５例ずつ実験例１と同じ方法で採血し、血中アルコール
濃度を測定した。Control group: 05.1.15.2.3.4 after alcohol administration
At 15.2.3.4 hours, the test drug administration group
Blood was collected from each of the five cases in the same manner as in Experimental Example 1, and the blood alcohol concentration was measured.
（３）実験結果
第４図に示したように、対照群に比へ塩化カルニチン投
与群では１５．２．３時間後に１５．１９．３７％の有
意な（Ｐ＜０．０５）低下か認められた。(3) Experimental results As shown in Figure 4, a significant decrease of 15.19.37% (P<0.05) was observed in the carnitine chloride administration group compared to the control group after 15.2.3 hours. It was done.
従って、本発明のアルコール吸収抑制剤はアルコール投
与後に用いた場合も、それ以降のアルコール吸収を抑制
することにより血中に移行するアルコール量を減少せし
めることが示された。Therefore, it has been shown that even when the alcohol absorption inhibitor of the present invention is used after alcohol administration, it suppresses subsequent alcohol absorption, thereby reducing the amount of alcohol transferred into the blood.
製剤例１
５
［液剤］
組成
塩化カルニチン ２ｏｏ乃
チクセツニン／ンエキス ５０ｍｇ
コ／ユニ末 １００７１ｇ白糖
１０００Ｍクエン酸
’１０ｍｇ香料 ０．０３ｍＱ
上記成分を配合し、水を加えて全量を３０７ＩＣとし、
これを１回服用量とする。Formulation Example 1 5 [Liquid] Composition Carnitine chloride 2oo no tixetunin/n extract 50mg Co/Uni powder 10071g white sugar
1000M citric acid
'10mg fragrance 0.03mQ
Blend the above ingredients, add water to make the total amount 307IC,
This is considered a single dose.
製剤例２
［顆粒剤／粉末剤］
組成
塩化カルニチン ２００ｘｇ
チクセツニンジンエキス ３ｈ＋９
ゴンユユ末 ５０即
白糖 １１０■
乳糖、 ８００Ｍ
ヒドロキシプロピル
メチルセルロース １０即
６
上記の割合で混合した後、少量の水を加えて練合機で連
合、製粒、乾燥後分包し、これを１回服用量とする。Formulation Example 2 [Granule/Powder] Composition Carnitine chloride 200xg Panax ginseng extract 3h+9 Gonyuyu powder 50 Instant white sugar 110■ Lactose, 800M Hydroxypropyl methyl cellulose 10 Instant 6 After mixing in the above ratio, add a small amount of water and knead. After combining, granulating, and drying, the mixture is divided into packages, each of which is used as a single dose.
製剤例３
［錠剤／カプセル剤］
組成
塩化カルニチン １１００ｚ
チクセツニンジンエキス ２０７！１？ゴンユユ末
３０ｖｒｇ乳糖
９６ｍ９
ステアリン酸マグネシウム ４ｍｇ
合 計 ４００尻？上記の割合で混
合し打錠する。カプセル剤の場合はこれを粉砕し、ステ
アリン酸マグネシウムを混ぜ、カプセル充填機にて充填
する。１回服用量は２錠あるいは２カプセルとする。Formulation Example 3 [Tablets/Capsules] Composition Carnitine Chloride 1100z Panax Ginseng Extract 207!1? end of gonyuyu
30vrg lactose
96m9 Magnesium stearate 4mg Total 400 butts? Mix in the above ratio and tablet. In the case of capsules, this is crushed, mixed with magnesium stearate, and filled with a capsule filling machine. Each dose is 2 tablets or 2 capsules.
哀獣
１ 、 Ｅ、Ｍ、 Ｐ、Ｗｉｄｍａｒｋ ： Ｕｄｅ
ｒ ｄｉｅ ｅｉｎｗｉｒｋｕｎｇｖｏｎ ａｍ＋ｎｏ
ｓａｕｒｅｎ ａｕｆ ｄｅｎ ａｌｋｏｈｏｌｇｅｈ
ａｌｔ ｄｅｓ ｂｌｕｔｅｓ、 Ｂ ｉｏｃｈｅｍ、
Ｚ、、 ２６５・２３７．１合計 １５０ｏ１
１ｇ
９３３
Ｋｅｎｎｅｔｈ Ｂｌｕｍ Ｊａｃｋ Ｅ、Ｗａ
ｌｌａｃｅａｎｄ Ｒｉｃｈａｒｄ Ｎ、 Ｆ ｒ
ｉｅｄｍａｎ ： Ｒｅｄｕｃｔｉｏｎ ｏｆ ａｃｕ
ｔｅａｌｃｏｈｏｌｉｃ １ｎｔｏｘｉｃａｔｉｏｎ
ｂｙ ａ ａｍｉｎｏ ａｃｉｄｓ ： ｇｌｙ
ｃｉｎｅ ａｎｄ ５ｅｒｉｎｅ、 Ｌ ｉｆｅ Ｓ
ｃｉｅｎｃｅｓ。Sad beast 1, E, M, P, Widmark: Ude
r die einwirkungvon am+no
sauren auf den alkoholgeh
alt des brutes, Biochem,
Z,, 265・237.1 total 150o1
1g 933 Kenneth Blum Jack E, Wa
llace and Richard N, F r
iedman: Reduction of acu
tealcoholic toxicity
by a amino acids: gly
cine and 5erine, Life S
sciences.
＋４ ：５５７．１９７４
小橋恭−他：アルコール吸収抑制剤、公開特許公報（出
願Ｎｏ、平０１−２６５９１８）９９１
Ｒｏｓｅｎ、Ｈ，Ｍ、、 Ｙｏｓｉｍｕｒａ、Ｎ、
ｅＬ ａｌ、 ： Ｐｌａｓｍａ ａｍｉｎｏ ｐａｔ
ｔｅｒｎｓ ｉｎ ｈｅｐａｔｉｃ ｅｎｃｅｐｈａｌ
ｏｐａｔｈｙ ｏｆ ｄｉｌＴｅｒｉｎｇ ｅｔｉｏｌ
ｏｇｙ、 Ｇａｓｔｒｏｅｎｔｅｒｌｏｇｙ、 ７２
： ４８３〜４８７． １９７７Ｓｈａｗ Ｓ、
Ｌｉｅｂｅｒ Ｃ，Ｓ、 ： Ｐｌａｓｍａ ａｍｉｎ
。+4:557.1974 Kyo Kobashi et al.: Alcohol absorption inhibitor, published patent publication (Application No. 01-265918) 991 Rosen, H, M, Yoshimura, N,
eL al, : Plasma amino pat
terns in hepatic encephal
pathy of diltering etiol
ogy, Gastroenterlogy, 72
: 483-487. 1977Shaw S,
Lieber C,S: Plasma amine
.
ａｃｉｄ ａｂｎｏｒｍａｌｉｔｉｅｓ ｉｎ ｔｈｅ
ａｌｃｏｈｌｉｃ ： ｒｅｓｐｅｃｔｉｖｅ ｒｏ
ｌｅ ｏｆ ａｌｃｏｈｌ、 ｎｕｔｒｉｔｉｏｎ ａ
ｎｄ １ｉｖｅｒ １ｎｊｕｒｙ、 Ｇｓｔｒｏｅｎｔ
ｅｒｏｌｏｇｙ、 ７４ ： ６７７〜６８２，１９
７８゜
Ｂａｎｋｓ、Ｗ、 Ｌ、 Ｊ ｒ、、 Ｋ１１ｎｅ、
Ｅ、 Ｓ、、 Ｈｉｇｇｎｓ、 Ｅ、 Ｓ 、 ： Ｈ
ｅｐａｔｉｃ ｃｏｍｐｏｓｉｔｉｏｎ ａｎｄ ｍｅ
ｔａｂｏｌｉｓｍ ａｆｔｅｒ ｅｔｈａｎｏｌ ｃ
ｏｎｓｕｍｐｓ＋ｏｎ ｉｎ ｒａｔｓｆｅｄ １ｉ
ｑｕｉｄ ｐｕｒｉｒｉｅｄ ｄｉｅｔｓ、 Ｊ、Ｎ
ｕｔｒ、＋ １００：５８１〜５９４． １９７０
７、Ｍφｒｌａｎｄ、 ｊ、、 Ｆ Ｉｅｎｇｓｒｕ
ｄ、 Ｒ，、ｅｔ ａｌ、 ： Ｈｅｐａｔｉｃ ａｍ
ｉｎｏ ａｃｉｄ １ｅｖｅｌｓ ｉｎ ｒａｔ
ｓ ａｆｔｅｒ １ｏｎｇ−ｔｅｒｍ ｅｔｈａｎｏ
ｌ ｆｅｅｄｉｎｇ、 Ｂｉｏｃｈｅｍ Ｐｈａ
ｒｍａｃｏｌ、、 ２８ ： ４２３〜４２７． １
９７８゜８、 Ｂｕｃｈｅｒ、Ｔｈ、、 ａｎｄ
Ｈ，Ｒｅｄｅｔｚｋｉ、 Ｋ１１ｎ、Ｗｓｃｈｒ、
２９ ： ６１５． １９５ ］acid abnormalities in the
alcoholic: specific
le of alcohol, nutrition a
nd 1iver 1njury, Gstroent
Erology, 74: 677-682, 19
78゜Banks, W, L, J r,, K11ne,
E, S, Higgns, E, S, :H
epatic composition and me
tabolism after ethanol c
onsumps+on in ratsfed 1i
Quid Puriried Diets, J,N
utr, +100:581-594. 1970 7, Mφrland, j,, F Iengsru
d, R, et al: Hepatic am
ino acid 1 level in rat
s after 1ong-term ethanol
l feeding, Biochem Pha
rmacol, 28: 423-427. 1
978°8, Bucher, Th,, and
H, Redetzki, K11n, Wshr,
29: 615. 195]
第１図および第４図は塩化カルニチン投与による血中ア
ルコール濃度の推移を示すグラフ、第２図はチクセツニ
ンジンまたはゴシュユ投与による血中アルコール濃度の
推移を示すグラフ、第３図は塩化カルニチンおよびチク
セツニンジンの用量反応曲線を示すグラフ、第５図はキ
キコウ、クコシ、またはダイズサポニン投与による血中
アルコール濃度の推移を示すグラフである。
手続補正書
１．事件の表示
千歳 ２年 特許願 第０６５０５６号２、発明の
名称
アルコール吸収抑制剤
３、補正をする者
事件との関係 特許出願人
名称 ロート製薬株式会社
４、代理人
自 発
６、補正の対象
明細書の「発明の詳細な説明」の欄
７、補正の内容
明細書中、以下の箇所を補正する。
１）４頁１行、「文献４．５．６」を「文献１．２．３
」に訂正する。
２）同頁３行、「（文献７）」を「（文献４）」に訂正
する。
３）７頁１８行、ｒｏ、 ３ｊをｒｏ、ｏＩＪに訂正す
る。
４）９頁１２行、「（文献８）」を「（文献５）」に訂
正する。
５）１２頁１行、「１０％」を「ｌｏｗ／ｖ％」に訂正
する。
６）同頁２行、ｒ４０％」およびｒ２０％」をそれぞれ
ｒ４０ｗ／ｖ％」およびｒ２０ｗ／ｖ％ｊに訂正する。
７）１８頁１８行、「１．」から１９頁９行、ｒ１９９
１．Ｊまでを削除する。
８）同頁１０行、「４．」を「１．」に訂正する。
９）同頁１４行、「５．」を「２．」に訂正す一
１０）同頁１９行、「６．」を「３．」に訂正する。
１１）２０頁４行、「７．」を「４．１に訂正する。
１２）同頁８行、「８．」を「５．１に訂正する。
以
上Figures 1 and 4 are graphs showing changes in blood alcohol concentration due to administration of carnitine chloride, Figure 2 is a graph showing changes in blood alcohol concentration due to administration of ginseng or goshuyu, and Figure 3 is a graph showing changes in blood alcohol concentration due to administration of carnitine chloride and FIG. 5 is a graph showing a dose-response curve for ginseng, and FIG. 5 is a graph showing changes in blood alcohol concentration due to administration of Kikikou, Lycium mulberry, or soybean saponin. Procedural amendment 1. Indication of the case Chitose 2 years Patent Application No. 065056 2, Name of the invention Alcohol absorption inhibitor 3, Person making the amendment Relationship to the case Patent applicant name Rohto Pharmaceutical Co., Ltd. 4, Sponsored by the agent 6, Details subject to amendment In column 7 of the "Detailed Description of the Invention" of the book, the following parts in the description of the contents of the amendment are amended. 1) On page 4, line 1, change "Reference 4.5.6" to "Reference 1.2.3"
” is corrected. 2) On the same page, line 3, "(Reference 7)" is corrected to "(Reference 4)." 3) On page 7, line 18, correct ro, 3j to ro, oIJ. 4) On page 9, line 12, "(Reference 8)" is corrected to "(Reference 5)." 5) On page 12, line 1, correct "10%" to "low/v%". 6) On the same page, 2 lines, correct "r40%" and "r20%" to "r40w/v%" and r20w/v%j, respectively. 7) Page 18, line 18, "1." to page 19, line 9, r199
1. Delete up to J. 8) On the same page, line 10, correct "4." to "1.". 9) On line 14 of the same page, correct “5.” to “2.” -10) On line 19 of the same page, correct “6.” to “3.” 11) On page 20, line 4, “7.” is corrected to “4.1.” 12) On page 20, line 8, “8.” is corrected to “5.1.”
Claims (1)
シからなる群から選ばれる生薬粉末またはエキス、ダイ
ズサポニンおよび塩化カルニチンのいずれか１種あるい
は２種以上を有効成分とするアルコール吸収抑制剤。1. An alcohol absorption inhibitor containing one or more of the following as active ingredients: herbal medicine powder or extract selected from the group consisting of ginseng, goshuyu, bellflower, and wolfberry, soybean saponin, and carnitine chloride.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2065056A JP2891738B2 (en) | 1990-03-15 | 1990-03-15 | Alcohol absorption inhibitor |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2065056A JP2891738B2 (en) | 1990-03-15 | 1990-03-15 | Alcohol absorption inhibitor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP10303805A Division JP3088707B2 (en) | 1998-10-26 | 1998-10-26 | Absorption inhibitor |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH03264534A true JPH03264534A (en) | 1991-11-25 |
| JP2891738B2 JP2891738B2 (en) | 1999-05-17 |
Family
ID=13275914
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2065056A Expired - Fee Related JP2891738B2 (en) | 1990-03-15 | 1990-03-15 | Alcohol absorption inhibitor |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP2891738B2 (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5998421A (en) * | 1996-06-12 | 1999-12-07 | Kyowa Hakko Kogyo Co., Ltd. | Lipid metabolism ameliorants |
| JP2003081856A (en) * | 2001-09-10 | 2003-03-19 | Tadashi Goino | Antihyperlipemic composition and method for producing the same |
| US6902748B1 (en) | 1999-12-22 | 2005-06-07 | Jang Saeng Doraji Co., Ltd | Medicines manufactured from old platycodon extracts |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011051742A1 (en) * | 2009-10-28 | 2011-05-05 | Modutech S.A. | Preparation comprising amino acids and plants and its activity in the alcohol detoxification |
-
1990
- 1990-03-15 JP JP2065056A patent/JP2891738B2/en not_active Expired - Fee Related
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5998421A (en) * | 1996-06-12 | 1999-12-07 | Kyowa Hakko Kogyo Co., Ltd. | Lipid metabolism ameliorants |
| US6214831B1 (en) | 1996-06-12 | 2001-04-10 | Kyowa Hakko Kogyo Co., Ltd. | Pharmaceutical composition containing evodiamine compound and method for improving lipid metabolism or antiobesity |
| US6902748B1 (en) | 1999-12-22 | 2005-06-07 | Jang Saeng Doraji Co., Ltd | Medicines manufactured from old platycodon extracts |
| JP2003081856A (en) * | 2001-09-10 | 2003-03-19 | Tadashi Goino | Antihyperlipemic composition and method for producing the same |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2891738B2 (en) | 1999-05-17 |
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