JP2002145764A - Composition for pharyngeal mucous membrane - Google Patents

Composition for pharyngeal mucous membrane

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Publication number
JP2002145764A
JP2002145764A JP2000343058A JP2000343058A JP2002145764A JP 2002145764 A JP2002145764 A JP 2002145764A JP 2000343058 A JP2000343058 A JP 2000343058A JP 2000343058 A JP2000343058 A JP 2000343058A JP 2002145764 A JP2002145764 A JP 2002145764A
Authority
JP
Japan
Prior art keywords
acid
composition
pharyngeal mucosa
polyphenol
pharyngeal
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.)
Withdrawn
Application number
JP2000343058A
Other languages
Japanese (ja)
Inventor
Takafumi Ohashi
隆文 大橋
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 JP2000343058A priority Critical patent/JP2002145764A/en
Publication of JP2002145764A publication Critical patent/JP2002145764A/en
Withdrawn legal-status Critical Current

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  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for pharyngeal mucous membrane considerably reducing an uncomfortable feeling at the pharynx and masked in bitterness. SOLUTION: This composition for pharyngeal mucous membrane considerably reduced in an uncomfortable taste such as an astringent taste by polyphenol is obtained by formulating the polyphenol, ethanol and concentrated glycerin.

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、咽頭部の違和感を
感じる際に使用する咽頭粘膜用組成物に関する。
TECHNICAL FIELD The present invention relates to a composition for pharyngeal mucosa used when the pharynx is uncomfortable.

【0002】[0002]

【従来の技術】咽頭部の違和感を感じる場合の代表的な
例は、上気道を中心とする局所炎症性症状に倦怠感等の
種々の全身症状を伴う疾患である風邪症候群等のウイル
ス性の呼吸器感染症に感染した場合である。上気道の炎
症症状である咽頭部の充血や腫れは、風邪症候群の罹患
の際に高い頻度で発現する症状であり、この症状の自覚
症状である咽頭部の疼痛症状等の違和感の除去・緩解が
対症療法の中心的役割を占めている。
2. Description of the Related Art A typical example of a person who feels discomfort in the pharynx is a viral illness such as a cold syndrome which is a disease accompanied by various systemic symptoms such as malaise as well as local inflammatory symptoms mainly in the upper respiratory tract. In case of infection with respiratory infection. Pharyngeal hyperemia or swelling, which is an inflammatory symptom of the upper respiratory tract, is a symptom that frequently occurs when a person has the cold syndrome, and removal / remission of discomfort such as pharyngeal pain, which is a subjective symptom of this symptom. Plays a central role in symptomatic treatment.

【0003】この他、アレルギーや大気汚染等による咽
頭粘膜の刺激が粘膜表面を傷害し、このことに伴う咽頭
部の充血や腫れも違和感として捉えられることが知られ
ているが、対処法は対症療法が主体となっている。
[0003] In addition, it is known that irritation of the pharyngeal mucosa due to allergy or air pollution damages the mucosal surface, and consequent redness and swelling of the pharynx can be perceived as uncomfortable. Therapy is the main.

【0004】対症療法では、一般に殺菌消毒薬、消炎酵
素薬、局所麻酔薬、漢方薬又はヨウ素類を有効成分とし
たトローチ剤、ドロップ剤、舐剤、含嗽剤、ストリーム
剤又はスプレー剤等の経口投与剤型で用いることが行わ
れている。
[0004] In symptomatic treatment, generally, a troche, a drop, a lick, a gargle, a stream, a spray, or the like containing a bactericidal disinfectant, an anti-inflammatory enzyme, a local anesthetic, a Chinese medicine or iodine as an active ingredient is used. It has been used in dosage forms.

【0005】また、咽頭部粘膜の腫脹や損傷は、新たな
ウイルス感染や細菌の二次感染や各種アレルゲン、大気
汚染物質の暴露の機会をつくり出し、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リスクを負
う。
[0005] In addition, swelling and damage of the pharyngeal mucosa create new viral infections, secondary infections of bacteria, exposure to various allergens and air pollutants, and increase the severity of the discomfort, prolong the discomfort, and cause systemic symptoms. Take risks that can easily lead to expansion.

【0006】ポリフェノールは、茶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
(特許登録第2727471号、特開平3−106820号、特開平
3−246227号)。
[0006] It is known that a large amount of polyphenol is contained in tea, and it is known that the polyphenol in tea protects against infection of various viruses and bacteria (Patent Registration No. 2724771, JP-A-3-106820, JP-A-3-246227).

【0007】ポリフェノールは、加水分解性タンニン又
は縮合型タンニンに大きく区分でき、特に加水分解性タ
ンニンは、非常に強い渋味等の不快な味を有する。ま
た、ポリフェノールは、安定性が低く、特に液剤中では
分解されやすい。従って、効力、持続時間、利便性及び
使用感の優れた薬剤の開発が望まれている。
[0007] Polyphenols can be broadly classified into hydrolyzable tannins and condensed tannins. In particular, hydrolyzable tannins have an unpleasant taste such as a very strong astringency. In addition, polyphenols have low stability and are easily decomposed particularly in liquid preparations. Therefore, development of a drug excellent in efficacy, duration, convenience and feeling of use is desired.

【0008】[0008]

【発明が解決しようとする課題】本発明の目的は、咽頭
部の違和感の除去あるいは軽減を図るため、効力、持続
時間、利便性及び使用感が優れた咽頭粘膜用組成物を提
供することにある。
SUMMARY OF THE INVENTION An object of the present invention is to provide a composition for pharyngeal mucosa which is excellent in efficacy, duration, convenience and usability in order to remove or reduce discomfort in the pharynx. is there.

【0009】[0009]

【課題を解決するための手段】本発明者らは、上述の課
題を解決すべく鋭意研究を重ねた結果、有効成分として
ポリフェノール、基剤としてエタノール及び濃グリセリ
ンを配合することにより、ポリフェノールの渋味等の不
快な味を緩和し、著しく使用感を改善できる咽頭粘膜用
組成物が得られることを見出した。さらに無機酸または
無機酸から成る緩衝液を配合することによりポリフェノ
ールが長時間安定に存在する咽頭粘膜用組成物を得るこ
とができることを見出し、本発明を完成した。
Means for Solving the Problems The present inventors have conducted intensive studies to solve the above-mentioned problems, and as a result, by blending polyphenol as an active ingredient and ethanol and concentrated glycerin as bases, the reduction of polyphenols has been achieved. It has been found that a composition for pharyngeal mucosa that can alleviate unpleasant taste such as taste and can significantly improve the feeling of use can be obtained. Further, they have found that a composition for pharyngeal mucosa in which a polyphenol is stably present for a long time can be obtained by blending an inorganic acid or a buffer solution comprising an inorganic acid, thereby completing the present invention.

【0010】[0010]

【発明の実施形態】本発明の咽頭粘膜用組成物は、有効
成分としてポリフェノールと、基剤としてエタノールと
濃グリセリンを配合され、エタノールと濃グリセリンの
配合が重量比で1:2.3〜9であり、組成物全量に対
してポリフェノールが0.2〜5%配合されることが好
ましい。ポリフェノール、エタノール及び濃グリセリン
の最も好ましい配合の重量比は、2:20:80であ
る。さらに本発明の咽頭粘膜組成物に無機酸または無機
酸から成る緩衝液を適量配合してpHを1〜3に調整す
るとポリフェノールを長時間安定に存在させることがで
きる。ポリフェノールの配合が組成物全量の0.2%未
満であるとウイルス感染予防効果が期待できず、また5
%より多くなると不快な味を緩和することができない。
BEST MODE FOR CARRYING OUT THE INVENTION The composition for pharyngeal mucosa according to the present invention comprises polyphenol as an active ingredient, ethanol and concentrated glycerin as bases, and the blending ratio of ethanol and concentrated glycerin is 1: 2.3 to 9 by weight. It is preferable that 0.2 to 5% of polyphenol is blended with respect to the total amount of the composition. The weight ratio of the most preferred formulation of polyphenol, ethanol and concentrated glycerin is 2:20:80. Further, when the pH is adjusted to 1 to 3 by adding an appropriate amount of an inorganic acid or a buffer solution comprising an inorganic acid to the pharyngeal mucosa composition of the present invention, the polyphenol can be stably present for a long time. If the amount of the polyphenol is less than 0.2% of the total amount of the composition, the effect of preventing virus infection cannot be expected, and 5
%, The unpleasant taste cannot be alleviated.

【0011】本発明おいて、ポリフェノールとしては、
加水分解性タンニンが好ましく、また、加水分解性タン
ニンとしては、タンニン酸、没食子酸、没食子酸誘導
体、ガロイル没食子酸、ルテオン酸、エラジン酸又はこ
れらの類縁物質並びにこれらの塩類が挙げられ、最も好
ましくはタンニン酸である。
In the present invention, polyphenols include:
Hydrolysable tannins are preferred, and the hydrolysable tannins include tannic acid, gallic acid, gallic acid derivatives, galloyl gallic acid, luteonic acid, ellagic acid or their analogous substances and salts thereof, and most preferably. Is tannic acid.

【0012】無機酸または無機から成る緩衝液は、人へ
の投与が可能な無機酸または無機酸から成る緩衝液であ
れば特に限定されない。例えば無機酸としては、塩酸、
リン酸、ホウ酸または臭化水素酸が挙げられる。また、
無機酸から成る緩衝液としては、塩酸−塩化カリウム緩
衝液、塩酸−グリシン緩衝液またはリン酸−グリシン緩
衝液が挙げられる。無機酸または無機から成る緩衝液
は、好ましくは、塩酸、リン酸、ホウ酸、臭化水素酸ま
たは塩酸−塩化カリウム緩衝液塩酸である。使用感を考
慮すると、最も好ましくは塩酸である。
The inorganic acid or the buffer comprising an inorganic acid is not particularly limited as long as it is an inorganic acid or a buffer comprising an inorganic acid which can be administered to a human. For example, as the inorganic acid, hydrochloric acid,
Phosphoric acid, boric acid or hydrobromic acid. Also,
Examples of the buffer composed of an inorganic acid include a hydrochloric acid-potassium chloride buffer, a hydrochloric acid-glycine buffer, and a phosphate-glycine buffer. The buffer consisting of an inorganic acid or inorganic is preferably hydrochloric acid, phosphoric acid, boric acid, hydrobromic acid or hydrochloric acid-potassium chloride buffer hydrochloric acid. Considering the feeling in use, hydrochloric acid is most preferred.

【0013】本発明の咽頭粘膜用組成物は、風邪薬、鎮
咳去痰薬、鼻炎用薬、咽頭用薬、風邪予防薬、口腔内殺
菌用薬、口腔内消炎薬、口臭除去薬等に用いることがで
き、さらに必要により医薬部外品、医療用具等幅広い形
態で用いることができる。
The composition for pharyngeal mucosa of the present invention is used for cold medicine, antitussive expectorant, rhinitis medicine, pharyngeal medicine, cold prevention medicine, oral disinfectant, oral antiphlogistic, bad breath remover, etc. It can be used in a wide variety of forms such as quasi-drugs and medical devices as needed.

【0014】本発明の咽頭粘膜用組成物は、他に必要に
応じて、抗アレルギー薬、解熱鎮痛薬、消炎酵素類、気
管支拡張薬、鎮咳薬、去痰薬、交感神経興奮薬、抗コリ
ン薬、カフェイン類、ビタミン薬、他の生薬類、香料等
の成分を適宜に配合することができる。なお、これらの
成分は単独または相互に混合して用いることができ、通
常は医薬品製造指針(1995年版・薬業時報社)に収載され
ている一般用医薬品の鎮咳去痰薬の基準及び含嗽剤、歯
科口腔用剤の記載に準拠して配合される。
The composition for pharyngeal mucosa of the present invention may further comprise, if necessary, an antiallergic drug, an antipyretic analgesic, an anti-inflammatory enzyme, a bronchodilator, an antitussive, an expectorant, a sympathomimetic, an anticholinergic. Ingredients such as caffeine, vitamins, other crude drugs, and fragrances can be appropriately blended. These ingredients can be used alone or in combination with each other.Normally, the standards for antitussive expectorants and gargles for over-the-counter drugs listed in the Pharmaceutical Manufacturing Guidelines (1995 Pharmaceutical Times Co., Ltd.), It is blended according to the description of the dental oral preparation.

【0015】本発明の咽頭粘膜用組成物は、常法により
調製することができる。必要に応じて固形剤の場合には
賦形剤、滑沢剤、崩壊剤等を、液剤の場合には界面活性
剤、溶解補助剤、緩衝剤等を使用することができる。ま
た、この他保存剤、香料、色素、甘味剤・嬌味剤、清涼
化剤、着色剤等を使用することができる。
The composition for pharyngeal mucosa of the present invention can be prepared by a conventional method. Excipients, lubricants, disintegrating agents and the like can be used in the case of solid preparations, and surfactants, solubilizing agents, buffers and the like can be used in the case of liquid preparations as needed. In addition, other preservatives, flavors, pigments, sweeteners / flavors, fresheners, coloring agents, and the like can be used.

【0016】[0016]

【発明の効果】有効成分として不快な味を有するポリフ
ェノール、エタノール及び濃グリセリンを配合すること
により、ポリフェノールの渋味等の不快な味を著しく改
善し、咽頭部の違和感を低減することができる。さらに
無機酸または無機酸から成る緩衝液を加えることによ
り、液剤中でポリフェノールが長時間安定に存在する咽
頭粘膜用組成物が得られる。
According to the present invention, an unpleasant taste such as astringent taste of polyphenol can be remarkably improved by blending polyphenol, ethanol and concentrated glycerin having an unpleasant taste as an active ingredient, and discomfort in the pharynx can be reduced. Further, by adding an inorganic acid or a buffer solution composed of an inorganic acid, a composition for pharyngeal mucosa in which the polyphenol is stably present in the solution for a long time can be obtained.

【0017】[0017]

【実施例】以下、実施例及び試験例を挙げ本発明をさら
に詳しく説明するが、本発明は下記の例に限定されるも
のではない。
The present invention will be described in more detail with reference to the following examples and test examples, but the present invention is not limited to the following examples.

【0018】実施例1 下記の各成分及び分量を秤量し均一に溶解し1000gの咽
頭粘膜用薬剤を得た。 タンニン酸 20.0g エタノール 194.0g 濃グリセリン 774.0g l-メントール 12.0g
Example 1 The following components and amounts were weighed and uniformly dissolved to obtain 1000 g of a drug for pharyngeal mucosa. Tannic acid 20.0 g Ethanol 194.0 g Concentrated glycerin 774.0 g l-menthol 12.0 g

【0019】実施例2 下記の各成分及び分量を秤量し均一に溶解し、塩酸でp
H2に調製し、ルゴール液2000gを得た。
Example 2 The following components and amounts were weighed and dissolved uniformly,
The mixture was adjusted to H2 to obtain 2000 g of Lugol's solution.

【0020】 タンニン酸 26.0g ヨウ素 10.0g ヨウ化カリウム 20.0g 濃グリセリン 1032.9g ハッカ油 0.4g エタノール 255.7g 塩酸 655.0gTannic acid 26.0 g Iodine 10.0 g Potassium iodide 20.0 g Concentrated glycerin 1032.9 g Mint oil 0.4 g Ethanol 255.7 g Hydrochloric acid 655.0 g

【0021】実施例3 下記の各成分及び分量を秤量し均一に溶解し、塩酸でp
H1に調製し、1000gの点鼻薬を得た。 没食子酸ナトリウム 20.0g 塩化ベンゼトニウム 0.2g 日局グリセリン 60.0g エタノール 7.0g 塩酸 100.0g 精製水 適量
Example 3 The following components and amounts were weighed and uniformly dissolved.
H1 to give 1000 g of nasal drops. Sodium gallate 20.0 g Benzethonium chloride 0.2 g JP glycerin 60.0 g Ethanol 7.0 g Hydrochloric acid 100.0 g Purified water qs

【0022】試験例1 渋味マスキング試験 試験方法 被験薬として実施例1を用い、下記処方の対照薬をスト
リーム剤として用いた。これらを健常者48名に口腔内を
洗浄後、1日6回3日間使用させ、被験薬と対照薬の渋
味の印象を比較した。なお、印象は「5点:非常に耐え
られない渋味を感じる」「4点:非常に渋味を感じる」
「3点:渋味を感じる」「2点:軽度の渋味を感じる」
「1点:わずかに渋味を感じる」「0点:まったく渋味
を感じない」の6段階で評価し、2点以上点数が減った
者の人数及び比率を算出した。
Test Example 1 Astringency masking test Test method Example 1 was used as a test drug, and a control drug having the following formulation was used as a stream agent. The oral cavity was washed by 48 healthy persons and used for 6 days a day for 3 days, and the impression of astringency of the test drug and the control drug was compared. In addition, impression is "5 points: feel very unbearable astringency""4 points: feel very astringent"
"3 points: Feel the astringency""2 points: Feel the mild astringency"
The evaluation was made on a six-point scale of "1 point: slightly felt astringency" and "0 point: no feeling of astringency", and the number and ratio of those who scored 2 or more points were reduced.

【0023】対照薬処方(全量1000g) タンニン酸 80g 精製水 適量Control formulation (1000 g total) 80 g tannic acid Purified water

【0024】結果 渋味マスキング試験の結果を下記に示す。この判定にお
いて、本発明の被験薬群の方が対照薬群より優ってお
り、渋味を低減することが示された。
Results The results of the astringency masking test are shown below. In this determination, the test drug group of the present invention was superior to the control drug group, and it was shown that astringency was reduced.

【0025】対照薬の評価と被験薬の評価の差(対照薬
評価点−被験薬評価点) 点差 人数 5点 2人 4点 21人 3点 19人 2点 4人 1点 1人 0点 0人 −1点 1人
Difference between control drug evaluation and test drug evaluation (control drug evaluation point-test drug evaluation point) Point difference Number of people 5 points 4 points 21 points 3 points 19 points 2 points 4 points 1 point 1 point 0 points 0 Person -1 point 1 person

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 31/04 A61P 31/04 31/12 31/12 Fターム(参考) 4C076 AA12 BB21 CC31 DD22Z DD37A DD37E DD38A DD38E FF15 4C086 AA01 AA02 EA03 MA01 MA04 MA56 NA09 NA14 ZA59 4C206 AA01 AA02 DA19 KA01 MA01 MA04 MA37 MA76 NA09 NA13 ZA59 Continued on the front page (51) Int.Cl. 7 Identification symbol FI Theme coat II (reference) A61P 31/04 A61P 31/04 31/12 31/12 F term (reference) 4C076 AA12 BB21 CC31 DD22Z DD37A DD37E DD38A DD38E FF15 4C086 AA01 AA02 EA03 MA01 MA04 MA56 NA09 NA14 ZA59 4C206 AA01 AA02 DA19 KA01 MA01 MA04 MA37 MA76 NA09 NA13 ZA59

Claims (8)

【特許請求の範囲】[Claims] 【請求項1】ポリフェノール、エタノール及び濃グリセ
リンを配合する咽頭粘膜用組成物
1. A composition for the pharyngeal mucosa comprising a polyphenol, ethanol and concentrated glycerin.
【請求項2】ポリフェノールが、加水分解性タンニンで
ある請求項1記載の咽頭粘膜用組成物
2. The composition for pharyngeal mucosa according to claim 1, wherein the polyphenol is a hydrolyzable tannin.
【請求項3】加水分解性タンニンが、タンニン酸、没食
子酸、没食子酸誘導体、ガロイル没食子酸、ルテオン
酸、エラジン酸及びこ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2記載の咽頭粘膜用組成物
3. The method according to claim 2, wherein the hydrolyzable tannin is one or more selected from tannic acid, gallic acid, gallic acid derivatives, galloyl gallic acid, luteonic acid, ellagic acid and salts thereof. Composition for pharyngeal mucosa
【請求項4】エタノールと濃グリセリンの配合が重量比
で1:2.3〜9である請求項1〜3記載の咽頭粘膜用
組成物
4. The composition for pharyngeal mucosa according to claim 1, wherein the weight ratio of ethanol and concentrated glycerin is 1: 2.3-9.
【請求項5】咽頭粘膜用組成物の全量に対してポリフェ
ノールが0.2〜5%配合される請求項1〜4記載の咽
頭粘膜用組成物
5. The composition for pharyngeal mucosa according to claim 1, wherein the polyphenol is incorporated in an amount of 0.2 to 5% based on the total amount of the composition for pharyngeal mucosa.
【請求項6】咽頭粘膜用組成物に、更に無機酸または無
機酸から成る緩衝液を配合する請求項1〜5記載の咽頭
粘膜用組成物
6. The composition for pharyngeal mucosa according to claim 1, further comprising an inorganic acid or a buffer solution comprising an inorganic acid.
【請求項7】pHが1〜3の範囲である請求項1〜6記
載の咽頭粘膜用組成物
7. The composition for pharyngeal mucosa according to claim 1, wherein the pH is in the range of 1 to 3.
【請求項8】無機酸または無機酸から成る緩衝液が、塩
酸、リン酸、ホウ酸、臭化水素酸及び塩酸−塩化カリウ
ム緩衝液から選ばれる1種または2種である請求項6記
載の咽頭粘膜用組成物
8. The method according to claim 6, wherein the inorganic acid or the buffer comprising the inorganic acid is one or two selected from hydrochloric acid, phosphoric acid, boric acid, hydrobromic acid and hydrochloric acid-potassium chloride buffer. Composition for pharyngeal mucosa
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007039262A1 (en) * 2005-09-30 2007-04-12 Dsm Ip Assets B.V. Novel compositions containing polyphenols

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007039262A1 (en) * 2005-09-30 2007-04-12 Dsm Ip Assets B.V. Novel compositions containing polyphenols
JP2009510003A (en) * 2005-09-30 2009-03-12 ディーエスエム アイピー アセッツ ビー.ブイ. NOVEL COMPOSITION CONTAINING POLYPHENOL

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