JP2008515859A5

JP2008515859A5 -

Info

Publication number: JP2008515859A5
Application number: JP2007535189A
Authority: JP
Filing date: 2005-10-10
Publication date: 2008-11-27
Anticipated expiration: 2025-10-10

Description

二日酔い症状を予防および処置するため、ならびに、アセトアルデヒドと関連する肝臓損傷を予防および処置するための、アセトアルデヒドの血中濃度を低下させるための組成物の使用を示唆するいくつかの文献がある。例えばＵＳ５,２０２,３５４は、Ｌ−システインのようなアセトアルデヒド結合性物質、アスコルビン酸またはその塩、ジスルフィド型チアミン誘導体、またはその塩、および胆汁排出促進剤を含む組成物を記載する。ＵＳ４,５２８,２９５は、メチオニン、ビタミンＢ６およびクエン酸カリウムを含む組成物を記載する。 There are several publications that suggest the use of compositions to reduce blood levels of acetaldehyde to prevent and treat hangover symptoms and to prevent and treat liver damage associated with acetaldehyde. For example, US 5,202,354 describes a composition comprising an acetaldehyde-binding substance such as L-cysteine, ascorbic acid or a salt thereof, a disulfide-type thiamine derivative, or a salt thereof, and a bile elimination promoter. US 4,528,295 describes a composition comprising methionine, vitamin B6 and potassium citrate.

葉巻喫煙は紙巻きタバコ喫煙より長く続き得、故に、１５分より長くアセトアルデヒドを結合できる製剤が有利である。しかしながら、この時間は好ましくは３０分より短い。あるいは、葉巻喫煙者は、１本の葉巻喫煙中に１個を超える製剤を使用してよい。 Cigar smoking can last longer than cigarette smoking, and thus formulations that can bind acetaldehyde for more than 15 minutes are advantageous. However, this time is preferably less than 30 minutes. Alternatively, the cigar smoker may use more than one formulation during one cigar smoking.

用語“組成物”は、ここでは、所望により適当な担体と混合された、有効物質(複数もある)を含む、組成物を意味する。本組成物は口腔で使用するのに適当な局所製剤の形であり得る。 The term “composition” here means a composition comprising the active substance (s), optionally mixed with a suitable carrier. The compositions may be in the form of a suitable topical formulations for use in the oral cavity.

本発明の製剤は、好ましくは１から３００mgのアルデヒド結合性、特にアセトアルデヒド結合性物質を含み、より好ましくはその量は１から２５０mg、さらにより好ましくは１から２００mg、なおさらに好ましくは１から１５０mg、最も好ましくは１から１００mgである。目的が、アセトアルデヒドに加えて種々のアルデヒド類の結合であるとき、より高用量が特に好ましい。目的が、特に、アセトアルデヒドの結合であるならば、用量は低くてよい。 Ltd. agent of the present invention are preferably aldehyde binding 300mg 1, in particular comprising acetaldehyde-binding substance, more preferably 250mg of the amount 1, 200 mg and even more preferably from 1, even more 150mg preferably from 1 Most preferably from 1 to 100 mg. Higher doses are particularly preferred when the goal is the combination of various aldehydes in addition to acetaldehyde. If the purpose is in particular acetaldehyde binding, the dose may be low.

実施例９
紙巻きタバコ(１)を慣用法で製造する。本紙巻きタバコはフィルター(２)を含むか、またはフィルター無しでよい。システイン含有製剤(３)を上記の通り製造する。本製剤の形は、円形、卵形、凸形、爪形、環形、筒または方形状のような任意の適当な形態であり得る。本製剤(３)を紙巻きタバコ(１)に、ヒト使用に適当な接着剤様物質により取り付ける。図５Ａに示す通り、システイン組成物はボールの形であり、紙巻きタバコの喫煙時に口腔に置かれる部分に付着しており、図５Ｂは、紙巻きタバコと本製剤を断面図として示す。図６Ａにおいて、本製剤(３)は紙巻きタバコ(１)の先端にあり、紙巻きタバコのその部分は、喫煙時に口腔内に置かれる。図６Ｂはそれの断面図である。図７Ａにおいて、本製剤(３)は方形状であり、それは紙巻きタバコの先端の周りに曲がっており、紙巻きタバコ(１)のその部分は喫煙時に口腔内に置かれ、図７Ｂはその断面図である。図８において、筒(５)が紙巻きタバコ(１)のフィルター(２)の先端に取り付けられている。システインを含む製剤(３)は筒内に位置する。図９において、ホルダー(４)またはホルダー表面がシステイン(３)で含浸されている。図１０において、ホルダー(４)またはホルダー表面は、システイン含有組成物(３)で含浸されており、ホルダーの形は適当な特に葉巻を持つために適している。図１１において、紙巻きタバコ(１)のフィルター(２)またはフィルター表面はシステイン(３)で含浸されている。
Example 9
A cigarette (1) is produced in a conventional manner. The cigarette may include a filter (2) or no filter. A cysteine-containing preparation (3) is prepared as described above. The form of the formulation can be any suitable form, such as round, oval, convex, nail-shaped, ring-shaped, tube or square. This formulation (3) is attached to the cigarette (1) with an adhesive-like substance suitable for human use. As shown in FIG. 5A, the cysteine composition is in the form of a ball and is attached to the portion of the cigarette that is placed in the oral cavity when smoking, and FIG. 5B shows the cigarette and the formulation as a cross-sectional view. In FIG. 6A, the formulation (3) is at the tip of the cigarette (1), and that portion of the cigarette is placed in the oral cavity when smoking. FIG. 6B is a cross-sectional view thereof. In FIG. 7A, the formulation (3) has a square shape, which is bent around the tip of the cigarette, and that portion of the cigarette (1) is placed in the oral cavity during smoking, and FIG. It is. And has it 8, the cylinder (5) is attached to the distal end of the filter (2) of cigarettes (1). The preparation (3) containing cysteine is located in the cylinder. In FIG. 9, the holder (4) or the holder surface is impregnated with cysteine (3). In FIG. 10, the holder (4) or the holder surface is impregnated with a cysteine-containing composition (3) and the shape of the holder is suitable for having a suitable cigar. In FIG. 11, the filter (2) or filter surface of the cigarette (1) is impregnated with cysteine (3).

Claims

Use of a compound capable of binding aldehydes and comprising one or more free sulfhydryls and amino groups for the manufacture of a formulation for locally binding aldehydes in saliva during smoking, said formulation Comprises an effective amount of the aldehyde-binding substance (s) and a non-toxic carrier, which allows the release of the aldehyde-binding substance (s) during smoking of a single tobacco product. Use.

Use according to claim 1, characterized in that the carrier allows the release of aldehyde-binding substances into saliva under conditions that diffuse in the oral cavity in less than 30 minutes.

The formulation has the formula:

[Wherein R ¹ is hydrogen or an acyl group containing 1 to 4 carbon atoms;
R ² is a sulfhydryl group or sulfonic acid, and n is 1 or 2. ]
Use according to claim 1 or 2, characterized in that it comprises one or more compounds.

The formulation comprises L-cysteine, D-cysteine, cystine, cysteic acid, cysteine-glycine, threo- or erythro-β-phenyl-DL-cysteine, β-tetramethylene-DL-cysteine, methionine, D-penicillamine and its N-terminal dipeptide, semicarbazide, reduced glutathione, β-mercaptoethylamine, D, L-homocysteine, N-acetylcysteine, L-cysteinyl-L-valine, β, β-tetramethylene-DL-cysteine, cysteinyl-glycine One or more selected from the group consisting of: mercaptoethyl-glycine, tre- (5) -β-phenyl-DL-cysteine, erythro-β-phenyl-DL-cysteine, thiamine hydrochloride and mercaptan Characterized by containing substances Use as set forth in claim 1 in any one of 3.

Use according to any one of claims 1 to 4, characterized in that the formulation comprises an aldehyde-binding substance to which the aldehyde itself binds via both sulfhydryl and amino groups.

The aldehyde-binding substance is selected from the group consisting of L-cysteine, D-cysteine, a derivative of cysteine, and a substance that can be converted into cysteine, according to any one of claims 1 to 5. use.

7. Use according to any one of claims 1 to 6, characterized in that the aldehyde is acetaldehyde.

8. The carrier according to any one of the preceding claims, characterized in that the carrier comprises a substance selected from the group consisting of pharmaceutically acceptable diluents, sweeteners, flavoring agents and lubricants / glidents. Use according to 1.

9. The composition according to claim 1, wherein the composition is in the form of a formulation selected from chewable tablets, buccal tablets, sublingual tablets, candy, pastilles, lozenges, chewing gums or bubble gums and gels. Or use according to item 1.

Mouth and pharynx, larynx, a method for reducing the cancer risk of the esophagus and stomach, an effective amount of an aldehyde-binding substance (s), aldehyde binding to saliva under conditions that diffuse the mouth cavity material A method characterized in that aldehydes in saliva are locally bound during smoking by use of a composition comprising a carrier that allows for the release of the release (s).

11. The composition of claim 10, wherein the composition reduces the amount of one aldehyde during cigar, cigarette or pipe smoking to substantially the level of aldehydes in saliva prior to smoking. The method described.

12. A method according to claim 10 or 11, characterized in that the carrier comprises a substance selected from the group consisting of pharmaceutically acceptable diluents, sweeteners, flavoring agents and lubricants / flow agents.

13. The composition according to any of claims 10 to 12, characterized in that the composition is in the form of a formulation selected from chewable tablets, buccal tablets, sublingual tablets, candy, pastilles, lozenges, chewing gums or bubble gums and gels. The method according to claim 1.

In connection with smoking, at least one formulation is placed in the oral cavity, the formulation essentially releasing the aldehyde-binding substance (s) into saliva when using one tobacco product The method according to any one of claims 10 to 13.

15. A method according to any one of claims 10 to 14, characterized in that the composition is attached to a tobacco product, filter or holder.

16. A method according to claim 15, characterized in that the composition is attached to the part of the tobacco product, filter or holder that is placed in the oral cavity when smoking.

The composition, in contact with the saliva during smoking, when essentially using one of tobacco products, characterized in that the composition to release the aldehyde-binding substance (s) in saliva, The method according to claim 15 or 16.

18. A method according to any one of claims 15 to 17, characterized in that the composition is separable from tobacco products, filters or holders.

A composition comprising aldehyde-binding substance (s), wherein the composition is attached to a tobacco product, filter or holder for binding aldehydes in saliva during smoking ,Composition.

20. Composition according to claim 19, characterized in that it is attached to the part of the tobacco product, filter or holder that is placed in the oral cavity when smoking.

21. Composition according to claim 19 or 20, characterized in that the composition comprises a substance selected from the group consisting of pharmaceutically acceptable diluents, sweeteners, flavoring agents and lubricants / flow agents. .

22. A composition according to any one of claims 19 to 21, characterized in that the composition is in the form of a formulation selected from chewable tablets, buccal tablets, sublingual tablets, candy, pastilles, lozenges, chewing gums and gels. A composition according to 1.

23. Composition according to any one of claims 19 to 22, characterized in that the composition is attached to a tobacco product, filter or holder with or without the use of an adhesive-like substance. .

24. A composition according to any of claims 19 to 23, wherein the composition is attached using a structure for contacting the composition with a tobacco product, filter or holder.

25. A method according to any one of claims 19 to 24, wherein the composition is attached by impregnation and / or concentration and / or drying of the composition into a tobacco product, filter or holder.

26. The concentration according to any one of claims 19 to 25, wherein the concentration of the aldehyde binding substance (s) is higher on the surface of the tobacco product, filter or holder than inside the tobacco product, filter or holder. Composition.

27. A composition according to any one of claims 19 to 26, wherein the composition is attached to the surface of a tobacco product, filter or holder.

-Multiple cigarettes or cigarettes, and-multiple formulations containing aldehyde-binding substance (s) in an amount capable of binding aldehydes in saliva during smoking to the level at which the aldehyde was essentially prior to smoking. Including kit.

30. The kit of claim 28, wherein the formulation is capable of binding aldehydes in saliva during smoking of one, two or three cigars or cigarettes.

-A tobacco product, filter or holder; and-an amount of aldehyde attached to the tobacco product, filter or holder and capable of binding aldehydes in saliva during smoking to the level at which the aldehyde was essentially prior to smoking. Tobacco products, filters or holders comprising the composition comprising the substance (s).

31. Tobacco product according to claim 30, characterized in that the composition is attached to the part of the tobacco product, filter or holder that is placed in the oral cavity when smoking.

32. The tobacco product according to claim 30 or 31, wherein the composition comprises a substance selected from the group consisting of pharmaceutically acceptable diluents, sweeteners, flavoring agents and lubricants / flow agents.

33. A tobacco product according to any one of claims 30 to 32, wherein the composition is in the form of a formulation selected from chewable tablets, buccal tablets, sublingual tablets, candy, pastilles, lozenges, chewing gums and gels. .

34. A tobacco product according to any one of claims 30 to 33, wherein the composition is separable from a tobacco product, filter or holder.

35. A tobacco product according to any one of claims 30 to 34, wherein the composition is attached with or without an adhesive-like substance.

36. The tobacco product according to any one of claims 30 to 35, wherein the composition is attached using an arrangement for contacting the composition with a tobacco product, filter or holder.

37. A tobacco product according to any one of claims 30 to 36, wherein the composition is attached by impregnating and / or concentrating and / or drying the tobacco product, filter or holder of the composition.

38. The concentration of the aldehyde-binding substance (s) is higher on the surface of the tobacco product, filter or holder than on the interior of the tobacco product, filter or holder. Tobacco products.

39. A tobacco product according to any one of claims 30 to 38, wherein the composition is attached to the surface of a tobacco product, filter or holder.

40. The tobacco product according to any one of claims 30 to 39, wherein the tobacco product is a cigar, cigarette or pipe.