JP2000247873A - Composition for erasing sense of incompatibility at mucosal site - Google Patents

Composition for erasing sense of incompatibility at mucosal site

Info

Publication number
JP2000247873A
JP2000247873A JP11046466A JP4646699A JP2000247873A JP 2000247873 A JP2000247873 A JP 2000247873A JP 11046466 A JP11046466 A JP 11046466A JP 4646699 A JP4646699 A JP 4646699A JP 2000247873 A JP2000247873 A JP 2000247873A
Authority
JP
Japan
Prior art keywords
composition
adult
symptoms
local anesthetic
lidocaine
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
Application number
JP11046466A
Other languages
Japanese (ja)
Inventor
Ichiro Okudaira
一郎 奥平
Kenji Tsunoda
健司 角田
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Taisho Pharmaceutical Co Ltd
Original Assignee
Taisho Pharmaceutical Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Taisho Pharmaceutical Co Ltd filed Critical Taisho Pharmaceutical Co Ltd
Priority to JP11046466A priority Critical patent/JP2000247873A/en
Publication of JP2000247873A publication Critical patent/JP2000247873A/en
Pending legal-status Critical Current

Links

Abstract

PROBLEM TO BE SOLVED: To obtain the subject composition excellent in curing effect for mucosal site pain symptoms including pharyngodynia by including polyphenols and a local anesthetic. SOLUTION: This composition is obtained by including (A) polyphenols [phenolic compounds containing >=2 hydroxy groups in one molecule, which are found in tea, coffee, cacao, red wine, etc., (e.g. pyrogalloltannin, catechin, theaflavin)] and (B) a local anesthetic such as lidocaine, dibucaine or mepivacaine; wherein the amount of the ingredient A to be formulated is 250-6,000 mg/adult in terms of daily dose, and the amount of the ingredient B to be formulated is e.g. 3-75 mg/adult, 1-15 mg/adult, or 1.5-20 mg/adult, for lidocaine, dibucaine, or mepivacaine, respectively, in terms of daily dose. This composition is effective for mucosal sites subject to initial symptoms of cold such as the pharynx, nose and eyes, having curing effect on symptoms including rough throat, sneeze and snivel.

Description

【発明の詳細な説明】DETAILED DESCRIPTION OF THE INVENTION

【0001】[0001]

【発明の属する技術分野】本発明は、咽頭部をはじめと
する粘膜部位の違和感の解消に有効な組成物に関する。
BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a composition effective for relieving discomfort in mucous membranes including the pharynx.

【0002】[0002]

【従来の技術】風邪症候群は、ウイルスの感染により発
症するものと考えられているが、原因療法として有効な
抗ウイルス剤は未だ開発されておらず、専ら個々の風邪
症状の改善を目的とする対症療法を行うことが風邪治療
の中心となっている。
2. Description of the Related Art The cold syndrome is thought to be caused by infection with a virus. However, no effective antiviral agent has been developed as a causative treatment, and it is aimed solely at improving individual cold symptoms. Performing symptomatic treatment is central to cold treatment.

【0003】しかし、風邪症状が進行してしまった後で
は症状が複合的になり、対症療法の効果も緩慢なものに
なりがちであるため、いわゆる風邪の引きはじめに対処
することが重要である。
[0003] However, after the cold symptoms have progressed, the symptoms tend to be complex and the effect of symptomatic treatment tends to be slow, so it is important to deal with the beginning of the so-called cold.

【0004】ここで、風邪の初期症状としては、喉の痛
み、鼻がムズムズする、くしゃみ、目がしょぼしょぼす
るなど、粘膜部位に違和感を生じることが多い。このよ
うな粘膜部位の違和感は、そのほとんどが粘膜部位の充
血、腫脹、損傷などが原因であり、そのような違和感
は、新たなウイルス感染、細菌の二次感染などに暴露す
る機会をつくり出し、違和感の重症化や遷延化、全身症
状への拡大に結びつきやすい。したがって、粘膜部位の
違和感が生じる風邪の初期に、十分な対処をすることに
よって風邪症状の悪化を防止することが可能になる。
[0004] The initial symptoms of a cold often cause discomfort in the mucous membrane region, such as sore throat, stuffy nose, sneezing, and drizzling eyes. Most of such discomfort in mucosal sites is caused by hyperemia, swelling, damage, etc. of mucosal sites, and such discomfort creates opportunities for exposure to new viral infections, secondary bacterial infections, etc. It is likely to lead to severe and prolonged discomfort and spread to systemic symptoms. Therefore, it is possible to prevent the cold symptoms from worsening by taking sufficient measures in the early stage of a cold in which the mucous membrane part is uncomfortable.

【0005】従来、粘膜部位の違和感の改善には、殺菌
薬、消毒薬などをトローチ剤、ドロップ剤、スプレー剤
などで投与する方法が行われている。しかし、それらに
よる粘膜部位の違和感解消は一時的なものであり、粘膜
組織そのものの修復作用を有しないため、頻繁に投与し
なくてはならないなど煩雑である。その一方で、需要者
が購入しやすいのど飴などの需要が高まっているが、や
はり治療効果がないので一時的な違和感解消に過ぎな
い。
[0005] Conventionally, in order to improve the sense of discomfort at the mucosal site, a method of administering a bactericide, a disinfectant, or the like using a troche, a drop, a spray, or the like has been performed. However, the elimination of discomfort at the mucosal site due to these is temporary, and does not have a repairing effect on the mucosal tissue itself. On the other hand, there is a growing demand for candy and the like, which are easy for consumers to purchase, but since it has no therapeutic effect, it is only a temporary relief of discomfort.

【0006】したがって、粘膜部位の違和感を持続的に
解消することができる薬剤の開発が望まれていた。
[0006] Therefore, there has been a demand for the development of a drug capable of continuously eliminating the discomfort of the mucosal site.

【0007】ポリフェノール類は、茶などの中に多く含
まれていることが知られており、茶中のポリフェノール
が各種のウイルスや細菌の感染を防御することが知られ
ている(特許第2727471号、特開平3−1068
20、特開平3−246227)。しかしながら、風邪
罹患後に粘膜部位の違和感を除去・軽減するような作用
は知られていない。
[0007] It is known that polyphenols are contained in a large amount in tea and the like, and it is known that the polyphenol in tea protects against infections of various viruses and bacteria (Japanese Patent No. 2727471). JP-A-3-1068
20, JP-A-3-246227). However, there is no known effect of removing or reducing the discomfort at the mucosal site after a cold.

【0008】[0008]

【発明が解決しようとする課題】本発明は、咽頭部、
鼻、目などの粘膜部位の違和感の除去または軽減を図る
のに有効な、使用感の優れた粘膜適用組成物を提供する
ことを目的とする。
SUMMARY OF THE INVENTION The present invention provides a pharynx,
An object of the present invention is to provide a composition for mucosal application that is effective for removing or reducing discomfort in mucous membrane sites such as the nose and eyes, and has an excellent feeling in use.

【0009】[0009]

【課題を解決するための手段】本発明者らは、課題を解
決すべく鋭意研究を重ねた結果、ポリフェノール類およ
び局所麻酔薬を配合した組成物には、咽頭部をはじめと
する粘膜部位の違和感の改善に著しい効果が有ることを
見出し本発明を完成した。
Means for Solving the Problems The inventors of the present invention have conducted intensive studies to solve the problems, and as a result, a composition containing polyphenols and a local anesthetic has been added to a mucosal region such as the pharynx. The present inventor has found that there is a remarkable effect on improvement of discomfort, and completed the present invention.

【0010】すなわち本発明は、ポリフェノール類およ
び局所麻酔薬からなる組成物である。
That is, the present invention is a composition comprising a polyphenol and a local anesthetic.

【0011】[0011]

【発明の実施の形態】本発明でポリフェノール類とは、
茶、コーヒー、カカオ、赤ワイン、チョコレートなどに
含まれる、1分子中に水酸基を2個以上含むフェノール
性化合物であり、具体的には加水分解型タンニン、縮合
型タンニン、ピロガロールタンニン、カテコールタンニ
ン、タンニン酸、カテキン、エピカテキン、ロイコアン
トシアニジン類、テアフラビン、リスベラトロールなど
があげられる。
BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, polyphenols are
A phenolic compound containing two or more hydroxyl groups in one molecule contained in tea, coffee, cacao, red wine, chocolate, etc., specifically, hydrolyzable tannin, condensed tannin, pyrogallol tannin, catechol tannin, tannin Acid, catechin, epicatechin, leucoanthocyanidins, theaflavin, resveratrol and the like.

【0012】ポリフェノール類の配合量は、成人で一日
当たり250〜6000mgが好ましく、500〜500
0mgがさらに好ましい。
The compounding amount of the polyphenol is preferably 250 to 6000 mg per day for an adult, and 500 to 500 mg per day.
0 mg is more preferred.

【0013】本発明で局所麻酔薬とは医薬品などで一般
的に用いられるものを使用することができるが、好まし
いものとしてリドカイン、ジブカイン、メピバカインお
よびそれらの塩類などをあげることができる。
In the present invention, as the local anesthetic, those generally used in pharmaceuticals and the like can be used. Preferred examples thereof include lidocaine, dibucaine, mepivacaine and salts thereof.

【0014】本発明において、局所麻酔薬は通常医薬品
に配合可能な量を配合することができる。具体的には1
日量でリドカインは3〜75mg、好ましくは5〜60mg
であり、ジブカインは1〜15mg、好ましくは2〜10
mgであり、メピバカインは1.5〜20mg、好ましくは
2.5〜15mgである。この投薬量は年齢、体重、病状
により適宜増減することができる。
In the present invention, the local anesthetic can be added in an amount which can be usually added to a medicine. Specifically 1
Lidocaine 3 to 75 mg, preferably 5 to 60 mg daily
And 1 to 15 mg of dibucaine, preferably 2 to 10
mg, and mepivacaine is 1.5 to 20 mg, preferably 2.5 to 15 mg. This dosage can be appropriately increased or decreased depending on the age, weight, and medical condition.

【0015】本発明の組成物が有効な粘膜部位とは、咽
頭、鼻、目などの風邪の初期症状が起こりやすい部位で
あり、症状としては、のどあれ、声がれ、のどの不快
感、のどの痛み、のどのはれ、くしゃみ、鼻みず、鼻づ
まり、目の疲れ、目のかすみ、結膜充血などの症状のこ
とである。
The mucosal site where the composition of the present invention is effective is a site where the initial symptoms of a cold such as the pharynx, nose and eyes are likely to occur, and the symptoms include throat, voice, throat discomfort, Sore throat, sore throat, sneezing, nasal stuffiness, nasal congestion, eye fatigue, blurred eyes, conjunctival congestion, etc.

【0016】本発明の組成物は、必要に応じて他の薬効
成分、賦形剤、滑沢剤、崩壊剤、界面活性剤、溶解補助
剤、緩衝剤、保存剤、香料、色素、甘味剤・嬌味剤、清
涼化剤、着色剤などを使用して、常法により、トローチ
剤、ドロップ剤、舐剤、口腔内溶解剤、ストリーム剤、
スプレー剤、含嗽剤、点鼻薬、洗鼻薬、点眼剤などに調
製することができる。
The composition of the present invention may contain, if necessary, other active ingredients, excipients, lubricants, disintegrants, surfactants, solubilizers, buffers, preservatives, flavors, pigments, sweeteners. -Using lozenges, fresheners, coloring agents, etc., in the usual manner, troches, drops, licks, oral dissolving agents, stream agents,
It can be prepared into sprays, mouthwashes, nasal drops, nasal washes, eye drops and the like.

【0017】本発明の組成物は、風邪薬、鎮咳去痰薬、
鼻炎用薬、咽喉頭用薬、風邪予防薬、口腔内殺菌用薬、
口腔内消炎薬、口臭除去薬、点眼薬などに用いることが
できる。
The composition of the present invention comprises a cold medicine, an antitussive expectorant,
Rhinitis medicine, pharyngolaryngeal medicine, cold prevention medicine, oral disinfectant medicine,
It can be used as an antiphlogistic for oral cavity, a breath freshener, an eye drop, and the like.

【0018】[0018]

【発明の効果】本発明により、咽頭部をはじめとする粘
膜部位の疼痛症状(のどの痛み)をはじめとする幅広い
違和感に対する改善効果が著しく向上した粘膜部位用組
成物を提供することが可能になった。
Industrial Applicability According to the present invention, it is possible to provide a composition for a mucous membrane part in which the effect of improving a wide variety of discomfort including pain symptoms (throat pain) of the mucous membrane part including the pharynx is significantly improved. became.

【0019】[0019]

【実施例】以下、実施例および試験例により本発明をさ
らに詳細に説明する。
The present invention will be described in more detail with reference to the following Examples and Test Examples.

【0020】実施例 表1に示した処方をグリセリン4mlおよび精製水で全量
20mlにして溶解させ、実施例1〜6および比較例1〜
6をストリーム剤として製した。
Examples The formulations shown in Table 1 were dissolved in 4 ml of glycerin and purified water to make a total volume of 20 ml.
No. 6 was prepared as a stream agent.

【0021】試験例 実施例1〜6および比較例1〜6を、咽頭部に違和感を
感じる風邪症候群患者に対し1群5名ずつで、1日6回
3日間使用させ、使用前後の咽頭部の症状をアンケート
形式で回答させた。なお、症状は「5点:非常に耐えら
れない違和感を感じる」「4点:非常に違和感を感じ
る」「3点:違和感を感じる」「2点:軽度の違和感を
感じる」「1点:わずかに違和感を感じる」「0点:ま
ったく違和感を感じない」の6段階で評価し、投与後に
2点以上点数が減った者を有効と判定した。有効人数お
よび有効率を表1に示した。
Test Examples Examples 1 to 6 and Comparative Examples 1 to 6 were used by a group of five patients with cold sensation who felt discomfort in the pharynx six times a day for three days. The symptoms were answered in a questionnaire format. Symptoms are “5 points: I feel very intolerable”, “4 points: I feel very uncomfortable”, “3 points: I feel uncomfortable”, “2 points: I feel a slight discomfort”, “1 point: Slight” The subjects were evaluated on a 6-point scale of “I feel uncomfortable”, “0 point: I do not feel any discomfort”, and those who lost 2 or more points after administration were judged to be effective. Table 1 shows the effective number of persons and the effective rate.

【0022】[0022]

【表1】 配合量および有効率 (1日量;mg) [Table 1] Compounding amount and effective rate (daily dose; mg)

【0023】実施例7 下記の各成分及び分量を秤量し均一に混合した後、得ら
れた混合粉末を直打法により1剤重量300mgになるよ
うに打錠し、トローチ剤を得た。
Example 7 After the following components and amounts were weighed and uniformly mixed, the resulting mixed powder was tableted by a direct compression method so that one tablet weighed 300 mg to obtain a troche.

【0024】 タンニン酸 2000g リドカイン 50g 塩酸クロルヘキシジン 15g 塩化リゾチーム 30g(力価) 乳糖 150g 低置換度ヒドロキシプロピルセルロース 125g ステアリン酸マグネシウム 15g 硬化ヒマシ油 15g。Tannic acid 2000 g Lidocaine 50 g Chlorhexidine hydrochloride 15 g Lysozyme chloride 30 g (titer) Lactose 150 g Low-substituted hydroxypropylcellulose 125 g Magnesium stearate 15 g Hardened castor oil 15 g

【0025】実施例8下記の各成分及び分量を秤量し均
一に混合した後、水飴と練り合わせ舐剤2600gを得
た。
Example 8 The following components and amounts were weighed and uniformly mixed, and 2600 g of a syrup mixed with starch syrup was obtained.

【0026】 エピガロカテキン 1500g リドカイン 60g 塩化セチルピリジニウム 3g 塩化リゾチーム 30g(力価) 乳糖 120g 低置換度ヒドロキシプロピルセルロース 100g ステアリン酸マグネシウム 15g 水飴 772g。Epigallocatechin 1500 g Lidocaine 60 g Cetylpyridinium chloride 3 g Lysozyme chloride 30 g (titer) Lactose 120 g Low-substituted hydroxypropylcellulose 100 g Magnesium stearate 15 g Water syrup 772 g.

【0027】実施例9下記の各成分及び分量を秤量し均
一に混合した後、精製水100mlに溶解し洗鼻薬を製
した。
Example 9 The following components and amounts were weighed and uniformly mixed, and then dissolved in 100 ml of purified water to prepare a nasal rinse.

【0028】 ロイコアントシアニン 5000mg メピバカイン 10mg 塩化セチルピリジニウム 6mg 塩酸リドカイン 500mg dl−メントール 500mg。Leucoanthocyanin 5000 mg Mepivacaine 10 mg Cetylpyridinium chloride 6 mg Lidocaine hydrochloride 500 mg dl-Menthol 500 mg.

【0029】実施例10 下記の各成分及び分量を秤量し均一に混合した後、精製
水100mlに溶解し点眼剤を製した。
Example 10 The following components and amounts were weighed and uniformly mixed, and then dissolved in 100 ml of purified water to prepare eye drops.

【0030】 没食子酸ナトリウム 4500mg 塩酸ジブカイン 10mg 塩化デカリニウム 1.5mg 塩化リゾチーム 45mg(力価) 塩酸リドカイン 500mgSodium gallate 4500 mg dibucaine hydrochloride 10 mg decalinium chloride 1.5 mg lysozyme chloride 45 mg (titer) lidocaine hydrochloride 500 mg

───────────────────────────────────────────────────── 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 11/00 A61K 31/00 611 43/00 643 A61K 31/167 31/165 602 31/445 31/445 31/47 31/47 Fターム(参考) 4C076 AA12 AA24 AA49 BB01 BB22 BB24 BB25 CC01 CC10 CC35 DD38 FF15 4C086 AA02 BC21 BC28 MA02 MA03 MA04 MA13 MA17 MA35 MA52 MA57 MA58 MA59 NA14 ZA21 ZA33 ZA34 ZA59 ZB33 4C206 AA02 CA19 CA20 FA31 MA02 MA03 MA04 MA33 MA37 MA55 MA72 MA77 MA78 MA79 NA14 ZA21 ZA33 ZA34 ZA59 ZB33──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. 7 Identification symbol FI Theme coat ゛ (Reference) A61P 11/00 A61K 31/00 611 43/00643 A61K 31/167 31/165 602 31/445 31/445 31/47 31/47 F-term (reference) 4C076 AA12 AA24 AA49 BB01 BB22 BB24 BB25 CC01 CC10 CC35 DD38 FF15 4C086 AA02 BC21 BC28 MA02 MA03 MA04 MA13 MA17 MA35 MA52 MA57 MA58 MA59 NA14 ZA21 ZA33 ZA34 ZA59 ZB33 CA4CA MA03 MA04 MA33 MA37 MA55 MA72 MA77 MA78 MA79 NA14 ZA21 ZA33 ZA34 ZA59 ZB33

Claims (4)

【特許請求の範囲】[Claims] 【請求項1】 ポリフェノール類および局所麻酔薬から
なる組成物。
1. A composition comprising a polyphenol and a local anesthetic.
【請求項2】 ポリフェノール類および局所麻酔薬から
なる粘膜部位用組成物。
2. A composition for a mucosal site comprising a polyphenol and a local anesthetic.
【請求項3】 局所麻酔薬がリドカイン、ジブカイン、
メピバカインおよびそれらの塩類から選ばれる1種また
は2種以上である請求項1または2に記載の組成物。
3. The local anesthetic is lidocaine, dibucaine,
3. The composition according to claim 1, wherein the composition is one or more selected from mepivacaine and salts thereof.
【請求項4】 トローチ剤、ドロップ剤、舐剤、口腔内
溶解剤、ストリーム剤、スプレー剤、含嗽剤、点鼻薬、
洗鼻薬および点眼剤から選ばれるいずれかの形態である
請求項1〜3のいずれかに記載の組成物。
4. Lozenges, drops, lozenges, oral dissolving agents, streams, sprays, gargles, nasal drops,
The composition according to any one of claims 1 to 3, which is in any form selected from a nasal wash and an eye drop.
JP11046466A 1999-02-24 1999-02-24 Composition for erasing sense of incompatibility at mucosal site Pending JP2000247873A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP11046466A JP2000247873A (en) 1999-02-24 1999-02-24 Composition for erasing sense of incompatibility at mucosal site

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP11046466A JP2000247873A (en) 1999-02-24 1999-02-24 Composition for erasing sense of incompatibility at mucosal site

Publications (1)

Publication Number Publication Date
JP2000247873A true JP2000247873A (en) 2000-09-12

Family

ID=12747958

Family Applications (1)

Application Number Title Priority Date Filing Date
JP11046466A Pending JP2000247873A (en) 1999-02-24 1999-02-24 Composition for erasing sense of incompatibility at mucosal site

Country Status (1)

Country Link
JP (1) JP2000247873A (en)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002326941A (en) * 2001-05-01 2002-11-15 Naomasa Morita Agent for ophthalmic use
FR2927256A1 (en) * 2008-02-13 2009-08-14 Top Pharm Sarl Lab Composition, useful for treating inflammatory disease of respiratory track, comprises alpha-amylase enzyme and local anesthetic
WO2014038593A3 (en) * 2012-09-05 2014-05-01 テイカ製薬株式会社 Granulated material for tablet that rapidly disintegrates in mouth

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002326941A (en) * 2001-05-01 2002-11-15 Naomasa Morita Agent for ophthalmic use
FR2927256A1 (en) * 2008-02-13 2009-08-14 Top Pharm Sarl Lab Composition, useful for treating inflammatory disease of respiratory track, comprises alpha-amylase enzyme and local anesthetic
WO2014038593A3 (en) * 2012-09-05 2014-05-01 テイカ製薬株式会社 Granulated material for tablet that rapidly disintegrates in mouth
US9463165B2 (en) 2012-09-05 2016-10-11 Teika Pharmaceutical Co., Ltd. Granular material for orally fast disintegrating tablets

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