JP5170973B2 - Topical skin preparation - Google Patents
Topical skin preparation Download PDFInfo
- Publication number
- JP5170973B2 JP5170973B2 JP2006092523A JP2006092523A JP5170973B2 JP 5170973 B2 JP5170973 B2 JP 5170973B2 JP 2006092523 A JP2006092523 A JP 2006092523A JP 2006092523 A JP2006092523 A JP 2006092523A JP 5170973 B2 JP5170973 B2 JP 5170973B2
- Authority
- JP
- Japan
- Prior art keywords
- skin
- weight
- gel
- lower alcohol
- external
- 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.)
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/216—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
- A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
- A61K31/245—Amino benzoic acid types, e.g. procaine, novocaine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/42—Amides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
- A61P23/02—Local anaesthetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/74—Biological properties of particular ingredients
- A61K2800/75—Anti-irritant
Landscapes
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- Life Sciences & Earth Sciences (AREA)
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- Organic Chemistry (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
本発明は、掻痒感の改善作用を有する皮膚外用剤に関する。 The present invention relates to an external preparation for skin having an effect of improving pruritus.
皮膚の掻痒感（かゆみ）は耐え難く、不快な症状である。その原因は、敏感肌、アトピー性皮膚炎、虫さされによる炎症など多種多様である。さらに、敏感肌は、表皮バリアが崩壊したタイプ（例えば乾燥肌）、炎症タイプ、知覚過敏タイプに分類される。知覚過敏タイプ以外は皮膚表面に何らかの器質的障害を伴うので、投与する薬剤の性質、剤型などに注意を要する。一方で、知覚過敏タイプは皮膚の性状は健常であるものの、かゆみ知覚神経が過敏であるために掻痒感を感じる症状である。 The itching of the skin (itching) is an unbearable and unpleasant symptom. The causes are various, such as sensitive skin, atopic dermatitis, inflammation caused by insect bites. Furthermore, sensitive skin is classified into a type in which the epidermal barrier is disrupted (for example, dry skin), an inflammation type, and a hypersensitive type. Other than the hypersensitivity type, there are some organic disorders on the skin surface, so care must be taken in the nature and dosage form of the administered drug. On the other hand, the hypersensitivity type is a symptom of pruritus because the itch sensory nerve is hypersensitive although the skin property is healthy.
これら多様なかゆみ症状を改善するため、抗炎症成分を配合した外用剤や保湿成分を配合した外用剤、活性剤フリーの低刺激性外用剤などの種々の外用剤が開発されており、また、とりわけ乾燥肌などに対する製剤の技術が多く見受けられるが（特許文献１、特許文献２参照）、かゆみを知覚しなくなるまでの時間が長いか、または持続性に欠けるなどの改善を要するものであった。特に、知覚過敏型の掻痒感の場合、皮膚表面は健常であるため、薬剤の浸透性が低くなり、改善の要望が顕著に高かった。
本発明は、かゆみを素早く他の感覚（清涼感、灼熱感）に置換し、かゆみを抑制し、これらの置換作用、抑制作用が持続する外用剤の提供を目的とする。 An object of the present invention is to provide an external preparation that quickly replaces itchiness with other sensations (cool feeling, burning sensation), suppresses itchiness, and maintains these replacement action and suppression action.
本発明者は、上記従来技術の問題点に鑑み鋭意検討を重ねた結果、局所麻酔剤、尿素、清涼化剤、低級アルコール及び水を特定の割合で含有させた外用剤が、かゆみを素早く清涼感や灼熱感に置き換えることができ、さらにかゆみを抑制し、これらの作用が持続する製剤となることを見出し、本発明を完成させた。 As a result of intensive studies in view of the above-mentioned problems of the prior art, the present inventor has rapidly improved the itching of an external preparation containing a local anesthetic, urea, a cooling agent, a lower alcohol and water at a specific ratio. The present invention has been completed by finding that it can be replaced with a feeling of sensation and a burning sensation, and further, itching is suppressed and these effects are sustained.
すなわち、本発明は下記の皮膚外用剤に係るものである。
項１．局所麻酔剤０．３〜５重量％、尿素３〜２０重量％、清涼化剤３〜１１重量％、低級アルコール１２〜４０重量％及び水を含有する皮膚外用剤。
項２．皮膚外用剤に含有される水及び低級アルコールの重量比率が水／低級アルコールで表すと０．６〜７．０である項１に記載の皮膚外用剤。
項３．局所麻酔剤がリドカイン、ジブカイン、プロカイン又はこれらの塩、アミノ安息香酸エチル及びテシットデシチンからなる群から選択される１種又は２種以上である項１又は２に記載の皮膚外用剤。
項４．清涼化剤がｌ−メントール、ｄｌ−メントール、ｄ−カンフル、ｄｌ−カンフル、薄荷油及び樟脳油からなる群から選択される１種又は２種以上である項１〜３のいずれかに記載の皮膚外用剤。
項５．低級アルコールが無水エタノール、エタノール、メタノール及びイソプロパノールからなる群から選択される１種又は２種以上である項１〜４のいずれかに記載の皮膚外用剤。
項６．低級アルコール含有量が２０〜３９重量％である項１〜５のいずれかに記載の皮膚外用剤。
項７．ゲル剤である項１〜６のいずれかに記載の皮膚外用剤。
項８．掻痒感改善用である項１〜７のいずれかに記載の皮膚外用剤。
項９．知覚過敏型掻痒感改善用である項１〜８のいずれかに記載の皮膚外用剤。
That is, the present invention relates to the following external preparation for skin.
Item 1. A topical skin preparation containing 0.3 to 5% by weight of a local anesthetic, 3 to 20% by weight of urea, 3 to 11% by weight of a refreshing agent, 12 to 40% by weight of a lower alcohol and water.
Item 2. Item 2. The topical skin preparation according to Item 1, wherein the weight ratio of water and lower alcohol contained in the topical skin preparation is 0.6 to 7.0 in terms of water / lower alcohol.
Item 3. Item 3. The topical skin preparation according to Item 1 or 2, wherein the local anesthetic is one or more selected from the group consisting of lidocaine, dibucaine, procaine or a salt thereof, ethyl aminobenzoate, and tesitdecitine.
Item 4. Item 4. The refreshing agent according to any one of Items 1 to 3, wherein the refreshing agent is one or more selected from the group consisting of l-menthol, dl-menthol, d-camphor, dl-camphor, thin cargo oil and camphor oil. Skin external preparation.
Item 5. Item 5. The skin external preparation according to any one of Items 1 to 4, wherein the lower alcohol is one or more selected from the group consisting of absolute ethanol, ethanol, methanol, and isopropanol.
Item 6. Item 6. The topical skin preparation according to any one of Items 1 to 5, wherein the lower alcohol content is 20 to 39% by weight.
Item 7. Item 7. The skin external preparation according to any one of Items 1 to 6, which is a gel.
Item 8. Item 8. The skin external preparation according to any one of Items 1 to 7, which is used for improving pruritus.
Item 9. Item 10. The external preparation for skin according to any one of Items 1 to 8, which is used for improving hypersensitivity pruritus.
本発明の皮膚外用剤は、局所麻酔剤０．３〜５重量％、尿素３〜２０重量％、清涼化剤３〜１１重量％、低級アルコール１２〜４０重量％及び水を含有することを特徴とする。上記の各成分を上記の範囲の量で配合した本発明の皮膚外用剤は、かゆみを素早く他の感覚（清涼感、灼熱感）に置き換えることができ、さらにかゆみを抑制し、これらの置換作用、抑制作用が持続する、掻痒感の改善に優れたものである。 The external preparation for skin of the present invention contains 0.3 to 5% by weight of a local anesthetic, 3 to 20% by weight of urea, 3 to 11% by weight of a refreshing agent, 12 to 40% by weight of a lower alcohol, and water. And The external preparation for skin according to the present invention, in which each of the above components is blended in an amount within the above range, can quickly replace itching with other sensations (cool feeling, burning sensation), further suppress itching, and replace these actions. In addition, the inhibitory action lasts and is excellent in improving pruritus.
本発明において、局所麻酔剤は０．３〜５重量％、好ましくは０．５〜４重量％含有され、外用剤の分野で利用されうるものを特に制限なく使用できる。局所麻酔剤は１種のみ含有されていても２種以上含有されていてもよい。局所麻酔剤の例としては、リドカイン、ジブカイン、プロカイン、テトラカイン、ブピパカイン、メピパカイン、クロロプロカイン、プロパラカイン、メプリルカイン又はこれらの塩、安息香酸アルキルエステル（例えばアミノ安息香酸エチル、塩酸パラブチルアミノ安息香酸ジエチルアミノエチル）、オルソカイン、オキセサゼイン、オキシポリエントキシデカン、ロートエキス、ペルカミンパーゼ、テシットデシチンなどが挙げられる。上記の塩としては、塩酸塩などが挙げられる。好ましい局所麻酔剤は、リドカイン、ジブカイン、プロカイン又はこれらの塩、アミノ安息香酸エチル、テシットデシチンであり、より好ましい局所麻酔剤はリドカイン、ジブカイン、プロカイン又はこれらの塩、アミノ安息香酸エチルである。 In the present invention, the local anesthetic is contained in an amount of 0.3 to 5% by weight, preferably 0.5 to 4% by weight, and those that can be used in the field of external preparations can be used without particular limitation. Only one kind of local anesthetic may be contained, or two or more kinds thereof may be contained. Examples of local anesthetics include lidocaine, dibucaine, procaine, tetracaine, bupipacaine, mepipacaine, chloroprocaine, proparacaine, meprilucaine or salts thereof, benzoic acid alkyl esters (for example, ethyl aminobenzoate, diethylamino parabutylaminobenzoate hydrochloride) Ethyl), orthocaine, oxesasein, oxypolyentoxydecane, funnel extract, percamin ase, tesit decitine and the like. Examples of the salt include hydrochloride. Preferred local anesthetics are lidocaine, dibucaine, procaine or salts thereof, ethyl aminobenzoate, tesitdecitine, and more preferred local anesthetics are lidocaine, dibucaine, procaine or salts thereof, ethyl aminobenzoate.
本発明において、尿素は３〜２０重量％、好ましくは５〜２０重量％含有され、外用剤の分野で利用されうるものを特に制限なく使用できる。 In the present invention, urea is contained in an amount of 3 to 20% by weight, preferably 5 to 20% by weight, and those that can be used in the field of external preparations can be used without particular limitation.
本発明において、清涼化剤は３〜１１重量％、好ましくは４〜７重量％含有され、外用剤の分野で利用されうるものを特に制限なく使用できる。清涼化剤は１種のみ含有されていても２種以上含有されていてもよい。清涼化剤の例としては、ｌ−メントール、ｄｌ−メントール、ｄ−カンフル、ｄｌ−カンフル、薄荷油、樟脳油、乳酸メンチル、クーリングエージェント、リモネン、チモール、ウイキョウ油、ユーカリ油、キシリトールなどが挙げられる。好ましい清涼化剤は、ｌ−メントール、ｄｌ−メントール、ｄ−カンフル、ｄｌ−カンフル、薄荷油、樟脳油であり、より好ましい清涼化剤は、ｌ−メントール、ｄｌ−メントール、ｄ−カンフル、ｄｌ−カンフルである。 In the present invention, the refreshing agent is contained in an amount of 3 to 11% by weight, preferably 4 to 7% by weight, and those that can be used in the field of external preparations can be used without particular limitation. Only one kind of cooling agent may be contained, or two or more kinds may be contained. Examples of the refreshing agent include l-menthol, dl-menthol, d-camphor, dl-camphor, thin cargo oil, camphor oil, menthyl lactate, cooling agent, limonene, thymol, fennel oil, eucalyptus oil, xylitol and the like. It is done. Preferred refreshing agents are l-menthol, dl-menthol, d-camphor, dl-camphor, light cargo oil, camphor oil, and more preferred refreshing agents are l-menthol, dl-menthol, d-camphor, dl. -It is camphor.
本発明において、低級アルコールは外用剤の分野で利用されうるものを特に制限なく使用できる。低級アルコールは１２〜４０重量％、好ましくは２０〜３９重量％含有され、好ましい範囲では塗布感が特に良好である。低級アルコールは１種のみ含有されていても２種以上含有されていてもよい。低級アルコールの例としては、無水エタノール、エタノール、メタノール、イソプロパノール又はこれらの変性アルコール（フェニル変性アルコール、８−アセチル化ショ糖変性アルコールなど）などが挙げられる。好ましい低級アルコールは、無水エタノール、エタノール、メタノール、イソプロパノールであり、より好ましい低級アルコールは、無水エタノール、エタノール、イソプロパノールである。 In the present invention, any lower alcohol that can be used in the field of external preparations can be used without particular limitation. The lower alcohol is contained in an amount of 12 to 40% by weight, preferably 20 to 39% by weight, and the coating feeling is particularly good in the preferred range. Only one type of lower alcohol may be contained, or two or more types may be contained. Examples of lower alcohols include absolute ethanol, ethanol, methanol, isopropanol, or modified alcohols thereof (phenyl-modified alcohol, 8-acetylated sucrose-modified alcohol, etc.). Preferred lower alcohols are absolute ethanol, ethanol, methanol and isopropanol, and more preferred lower alcohols are absolute ethanol, ethanol and isopropanol.
本発明において、水は特に明示する場合を除き、精製水を表す。水の含有量は上記の各成分が上記の範囲の含有量となる量であれば特に制限されないが、水及び低級アルコールの重量比率が水／低級アルコールで表すと０．６〜７．０となる量が好ましく、０．７〜６．０となる量がより好ましく、０．９〜６．０となる量がより一層好ましい。水及び低級アルコールの重量比率をこの範囲にすると、使用者がより早く、強くかゆみの置換を感じることができ、さらにかゆみの抑制効果に優れる。 In the present invention, water represents purified water unless otherwise specified. The water content is not particularly limited as long as each of the above components is in the above range, but the weight ratio of water and lower alcohol is 0.6 to 7.0 when expressed as water / lower alcohol. An amount of 0.7 to 6.0 is more preferable, and an amount of 0.9 to 6.0 is even more preferable. When the weight ratio of water and lower alcohol is within this range, the user can feel the itch substitution more quickly and strongly, and further, the itch suppression effect is excellent.
また、本発明の皮膚外用剤は、必要に応じて他の有効成分を本発明の効果を損なわない範囲において含有することが可能である。他の有効成分としては、例えば、ステロイド剤（デキサメタゾン、塩酸デキサメタゾン、塩酸ヒドロコルチゾン、吉草酸プレドニゾロン、酢酸プレドニゾロン等）、抗ヒスタミン剤（ジフェンヒドラミン、塩酸ジフェンヒドラミン、マレイン酸クロルフェニラミン等）、抗炎症剤（グリチルレチン酸、グリチルリチン酸二カリウム、グリチルレチン酸モノアンモニウム、アラントイン、サリチル酸、サリチル酸グリコール等）、殺菌剤（塩化ベンザルコニウム、塩化デカリニウム、塩化ベンゼトニウム、イソプロピルメチルフェノール、塩酸クロルヘキシジン、グルコン酸クロルヘキシジン、アンモニア水、スルファジアジン、乳酸、フェノール等）、鎮痒剤（クロタミトン等）、皮膚保護剤（コロジオン、ヒマシ油等）などが挙げられる。 Moreover, the skin external preparation of this invention can contain another active ingredient in the range which does not impair the effect of this invention as needed. Examples of other active ingredients include steroids (dexamethasone, dexamethasone hydrochloride, hydrocortisone hydrochloride, prednisolone valerate, prednisolone acetate, etc.), antihistamines (diphenhydramine, diphenhydramine hydrochloride, chlorpheniramine maleate, etc.), anti-inflammatory agents (glycyrrhetinic acid, etc.) , Dipotassium glycyrrhizinate, monoammonium glycyrrhetinate, allantoin, salicylic acid, glycol salicylate, etc., bactericides (benzalkonium chloride, decalinium chloride, benzethonium chloride, isopropylmethylphenol, chlorhexidine hydrochloride, chlorhexidine gluconate, aqueous ammonia, sulfadiazine, Lactic acid, phenol, etc.), antipruritic agents (crotamiton, etc.), skin protectants (collodion, castor oil, etc.) and the like.
また、本発明の皮膚外用剤は、必要に応じて添加剤を本発明の効果を損なわない範囲において含有することが可能である。添加剤としては、例えば、基剤（アルギン酸ナトリウム、ゼラチン、コーンスターチ、トラガントガム、メチルセルロース、ヒドロキシエチルセルロース、カルボキシメチルセルロース、キサンタンガム、カラギーナン、マンナン、アガロース、デキストリン、カルボキシメチルデンプン、ポリビニルアルコール、ポリアクリル酸ナトリウム、メトキシエチレン−無水マレイン酸共重合体、ポリビニルエーテル、ポリビニルピロリドン、カルボキシビニルポリマー、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、プルラン等のポリマー類；ミツロウ、オリーブ油、カカオ油、ゴマ油、ダイズ油、ツバキ油、ラッカセイ油、牛油、豚油、鶏油、ラノリン等の油脂類；白色ワセリン、黄色ワセリン、パラフィン、流動パラフィン、セレシンワックス、スクワラン、軽質流動パラフィン、マイクロクリスタリンワックス等の炭化水素類；ゲル化炭化水素（例えば、商品名プラスチベース、ブリストルマイヤーズスクイブ社製）；ステアリン酸等の高級脂肪酸；セタノール、オクチルドデカノール、ステアリルアルコール等の高級アルコール；ポリエチレングリコール（例えば、マクロゴール４００、マクロゴール４０００等）；プロピレングリコール、グリセリン、ジプロピレングリコール、１，３−ブチレングリコール、濃グリセリン等の多価アルコール；モノオレイン酸エステル、ステアリン酸グリセリド、ミリスチン酸オクチルドデシル、ミリスチン酸イソプロピル等の脂肪酸エステル類；生理食塩水、リン酸緩衝液等）、溶解補助剤（ポリビニルピロリドン等）、無機充填剤（タルク、カオリン、ベントナイト、酸化亜鉛、酸化チタン等）、老化防止剤、ｐＨ調節剤（トリエタノールアミン等）、保湿剤（セラミド、レシチン等）、防腐剤（パラオキシ安息香酸メチル、パラオキシ安息香酸プロピル、クエン酸、クエン酸ナトリウム、ホウ酸、ホウ砂等）、粘稠剤（コンドロイチン硫酸ナトリウム等）、酸化防止剤（ジブチルヒドロキシトルエン等）などが使用できる。好ましい添加剤としては、ポリマー類、多価アルコール、無機充填剤、溶解補助剤、ｐＨ調整剤、防腐剤、酸化防止剤などが挙げられる。また、本発明の皮膚外用剤は実質的に脂分を含まないことが望ましい。 Moreover, the skin external preparation of this invention can contain an additive in the range which does not impair the effect of this invention as needed. Examples of additives include bases (sodium alginate, gelatin, corn starch, tragacanth gum, methyl cellulose, hydroxyethyl cellulose, carboxymethyl cellulose, xanthan gum, carrageenan, mannan, agarose, dextrin, carboxymethyl starch, polyvinyl alcohol, sodium polyacrylate, methoxy Polymers such as ethylene-maleic anhydride copolymer, polyvinyl ether, polyvinyl pyrrolidone, carboxyvinyl polymer, hydroxypropylcellulose, hydroxypropylmethylcellulose, pullulan; beeswax, olive oil, cacao oil, sesame oil, soybean oil, camellia oil, peanut oil Oils such as beef oil, pork oil, chicken oil, lanolin; white petrolatum, yellow petrolatum, paraffin, fluid Hydrocarbons such as fin, ceresin wax, squalane, light liquid paraffin, microcrystalline wax; gelled hydrocarbon (for example, trade name Plastibase, manufactured by Bristol-Myers Squibb); higher fatty acids such as stearic acid; cetanol, octyldodecanol Higher alcohols such as stearyl alcohol; polyethylene glycol (eg, macrogol 400, macrogol 4000, etc.); polyhydric alcohols such as propylene glycol, glycerin, dipropylene glycol, 1,3-butylene glycol, concentrated glycerin; monooleic acid Esters, stearic acid glycerides, fatty acid esters such as octyldodecyl myristate, isopropyl myristate; physiological saline, phosphate buffer, etc.), solubilizer (polyvinyl pyrrole) ), Inorganic fillers (talc, kaolin, bentonite, zinc oxide, titanium oxide, etc.), anti-aging agents, pH regulators (triethanolamine, etc.), moisturizers (ceramide, lecithin, etc.), preservatives (paraoxybenzoic acid) Methyl acid, propyl paraoxybenzoate, citric acid, sodium citrate, boric acid, borax and the like), thickeners (such as sodium chondroitin sulfate), antioxidants (such as dibutylhydroxytoluene) and the like can be used. Preferred additives include polymers, polyhydric alcohols, inorganic fillers, solubilizers, pH adjusters, preservatives, antioxidants and the like. Moreover, it is desirable that the external preparation for skin of the present invention contains substantially no fat.
本発明の皮膚外用剤の剤型は、皮膚に適用可能なものであれば特に限定されるものではなく、例えば、軟膏剤、クリーム剤、ゲル剤、リニメント剤、ローション剤、乳剤、粉剤、懸濁剤、エアゾール剤、液剤などや、基剤を支持体上に支持させた硬膏剤、パップ剤、テープ剤、プラスター剤などが挙げられる。好ましくは、ゲル剤、クリーム剤、ローション剤、乳剤、懸濁剤、液剤であり、さらに好ましくは、ゲル剤である。 The dosage form of the external preparation for skin of the present invention is not particularly limited as long as it can be applied to the skin. For example, it is an ointment, cream, gel, liniment, lotion, emulsion, powder, suspension. Examples thereof include turbid agents, aerosol agents, liquid agents, and plasters, poultices, tape agents, plaster agents and the like in which a base is supported on a support. Preferred are gels, creams, lotions, emulsions, suspensions and liquids, and more preferred are gels.
上記支持体は、その剤型（例えば、パップ剤、テープ剤等）に応じて適宜選択されるが、薬物が不透過又は難透過性で柔軟なものが好ましく、例えば、酢酸セルロース、エチルセルロース、ポリエチレン、ポリプロピレン、ポリ塩化ビニル、酢酸ビニル−塩化ビニル共重合体、エチレン−酢酸ビニル共重合体、エチレン−酢酸ビニル−一酸化炭素共重合体、エチレン−ブチルアクリレート−一酸化炭素共重合体、ポリ塩化ビニリデン、ポリウレタン、ナイロン、ポリエチレンテレフタレート、ポリブチレンテレフタレートなどの樹脂フィルム；アルミニウムシート、織布、不織布など、及びこれらの積層シートなどが挙げられる。 The support is appropriately selected according to the dosage form (for example, a poultice, a tape, etc.), but the drug is preferably impermeable or hardly permeable and flexible. For example, cellulose acetate, ethyl cellulose, polyethylene , Polypropylene, polyvinyl chloride, vinyl acetate-vinyl chloride copolymer, ethylene-vinyl acetate copolymer, ethylene-vinyl acetate-carbon monoxide copolymer, ethylene-butyl acrylate-carbon monoxide copolymer, polychlorinated Examples thereof include resin films such as vinylidene, polyurethane, nylon, polyethylene terephthalate, and polybutylene terephthalate; aluminum sheets, woven fabrics, nonwoven fabrics, and laminated sheets thereof.
本発明の皮膚外用剤の使用量は、疾患の種類や症状の程度、患部の大きさなどによって異なるが、通常１回、１患部当たり５０〜５００ｍｇ、好ましくは１００〜３５０ｍｇであり、使用回数は１日に１回又はそれ以上の適当な回数とすることができる。 The amount of the external preparation for skin use of the present invention varies depending on the type of disease, the degree of symptoms, the size of the affected area, etc., but is usually once, 50 to 500 mg, preferably 100 to 350 mg per affected area. The number of times can be one or more times a day.
本発明の皮膚外用剤は、その剤型に応じた常法により製造することができる。例えば、ゲル剤を製造する場合、水などに水溶性有効成分、ポリマー類を分散させ、別にアルコール類などに、他の有効成分を溶解させ、これらを合わせて、真空乳化機などの密閉条件下で撹拌混合できる機器で撹拌混合することによりゲル剤を製造できる。 The skin external preparation of this invention can be manufactured by the conventional method according to the dosage form. For example, when producing a gel, water-soluble active ingredients and polymers are dispersed in water, etc., and other active ingredients are dissolved in alcohols, etc., and these are combined and sealed under conditions such as a vacuum emulsifier. The gel can be produced by stirring and mixing with an apparatus capable of stirring and mixing in the above.
本発明の皮膚外用剤は、掻痒感の改善、特に、皮膚の性状が健常な者が感じるかゆみ、神経が過敏であるが故に感じてしまうかゆみ、例えば、繊維刺激や化粧品の塗布などの軽度な刺激でも惹起されるかゆみの抑制（知覚過敏型掻痒感改善用）に効果を発揮する。 The external preparation for skin of the present invention improves itching feeling, particularly itching felt by persons with normal skin properties, and itching felt because the nerves are hypersensitive, for example, mild irritation such as fiber irritation and cosmetic application. It is effective in suppressing itching caused by stimuli (for improving perceptual itching sensation).
本発明の皮膚外用剤が皮膚に適用されると、かゆみが素早く清涼感や灼熱感といったかゆみ以外の感覚に置換され、かゆみが抑制され、これらの置換効果、抑制効果が持続する。このような効果は本発明の構成により発揮され、意外にも清涼化剤に通常保湿剤として用いられている尿素を組み合わせることが大きく関与すると推測される。 When the external preparation for skin of the present invention is applied to the skin, itching is quickly replaced with a sensation other than itching such as a refreshing feeling or a burning sensation, and the itching is suppressed, and these replacement effects and suppressing effects are sustained. Such an effect is exhibited by the configuration of the present invention, and it is surmised that it is surprisingly important to combine urea, which is usually used as a moisturizing agent, with a cooling agent.
以下、本発明を実施例等により詳細に説明するが、本発明はこれらに限定されるものではない。なお、表中の数値の単位はｇ（グラム）である。 EXAMPLES Hereinafter, although an Example etc. demonstrate this invention in detail, this invention is not limited to these. In addition, the unit of the numerical value in a table | surface is g (gram).
実施例１
表１に示す成分、すなわち局所麻酔剤（リドカイン）２重量％、尿素１０重量％、清涼化剤（ｌ−メントール）４重量％、低級アルコール（無水エタノール）１２重量％、水６７重量％、ジフェンヒドラミン１重量％、ＣＶＰ（カルボキシビニルポリマー）１重量％及びグリセリン３重量％を含有するゲル剤を製造した。すなわち、水に尿素を溶解し、撹拌しながらＣＶＰを加えて水相を調製し、水相とは別に無水エタノールにリドカイン、ｌ−メントール、ジフェンヒドラミン、グリセリンを溶解、混和して有機相を調製し、水相を撹拌しながらここに有機相を徐々に添加し、撹拌混合してゲル剤を調製した。
Example 1
Ingredients shown in Table 1, that is, 2% by weight of local anesthetic (lidocaine), 10% by weight of urea, 4% by weight of cooling agent (l-menthol), 12% by weight of lower alcohol (anhydrous ethanol), 67% by weight of water, diphenhydramine A gel containing 1% by weight, 1% by weight of CVP (carboxyvinyl polymer) and 3% by weight of glycerin was prepared. In other words, urea is dissolved in water, CVP is added with stirring to prepare an aqueous phase, and apart from the aqueous phase, lidocaine, l-menthol, diphenhydramine, and glycerin are dissolved and mixed in absolute ethanol to prepare an organic phase. The organic phase was gradually added to the water phase while stirring, and the mixture was stirred and mixed to prepare a gel.
実施例２〜１４
表２及び３に示す成分を使用し、実施例１と同様にしてゲル剤を製造した。
Examples 2-14
A gel was prepared in the same manner as in Example 1 using the components shown in Tables 2 and 3.
比較例１〜７
表１に示す成分を使用し、実施例１と同様にしてゲル剤を製造した。
Comparative Examples 1-7
Using the components shown in Table 1, a gel was prepared in the same manner as in Example 1.
比較例８
ジフェンヒドラミン、リドカイン、ｌ−メントール、モノステアリン酸グリセリルを混合し、加熱溶解し、油相を製造した。これとは別に、水、尿素、エタノール及びグリセリンを混合し、加熱溶解し、ここに油相を加えた。撹拌しながらカルボキシビニルポリマー、トリエタノールアミンを加えて乳剤を製造した。
Comparative Example 8
Diphenhydramine, lidocaine, l-menthol and glyceryl monostearate were mixed and dissolved by heating to produce an oil phase. Separately, water, urea, ethanol and glycerin were mixed and dissolved by heating, and the oil phase was added thereto. A carboxyvinyl polymer and triethanolamine were added with stirring to produce an emulsion.
比較例９
表１に示す成分を使用し、ワセリンを４０〜６０℃に加温し液状になったところに各成分を加え、撹拌混合し、冷却して油系軟膏剤を製造した。
Comparative Example 9
The components shown in Table 1 were used, and each component was added to the liquid when heated to 40-60 ° C., stirred and mixed, and cooled to produce an oil-based ointment.
試験例１
実施例１〜１４及び比較例１〜７のゲル剤、比較例８の乳剤、比較例９の軟膏剤を使用して皮膚のかゆみに関する官能試験を行った。皮膚が乾燥肌でない健常な状態の者を被験者（６名）とし、被験者がかゆみを発生した時にかゆみの発生した部位に実施例及び比較例の製剤を塗布してもらい、ＳＤ法などで用いられる意味尺度を利用して５段階（最低１点、最高５点）で評価をしてもらった。評価項目及び評価方法は次のとおりである。結果を表に示した。なお、表中、ＣＶＰはカルボキシビニルポリマー、ＤＰＧはジプロピレングリコール、ＰＧはポリエチレングリコールを意味する。
Test example 1
Using the gels of Examples 1 to 14 and Comparative Examples 1 to 7, the emulsion of Comparative Example 8, and the ointment of Comparative Example 9, a sensory test for itching of the skin was performed. A healthy person whose skin is not dry is a subject (six), and when the subject develops itching, the preparations of Examples and Comparative Examples are applied to the site where itching occurs, and used in the SD method or the like. Using the semantic scale, they were evaluated in five levels (minimum 1 point, maximum 5 points). Evaluation items and evaluation methods are as follows. The results are shown in the table. In the table, CVP means carboxyvinyl polymer, DPG means dipropylene glycol, and PG means polyethylene glycol.
評価項目
かゆみ以外の感覚（清涼感／灼熱感）の強さ
かゆみ以外の感覚（清涼感／灼熱感）の速さ
かゆみの抑制効果
かゆみ以外の感覚及びかゆみ抑制効果の持続性
評価方法
被験者６名のつけた５段階評価の点の合計点を次の区分で表した。
◎：２４〜３０点
○：１８〜２３点
△：１２〜１７点
×：６〜１１点
Evaluation item Strength of sensation other than itching (coolness / burning) Speed of sensation other than itching (cooling / burning) Suppression effect of itchiness Sustainability of sensation other than itchiness and itchiness evaluation method Evaluation method 6 subjects The total score of the five-point evaluation points marked is shown in the following categories.
◎: 24 to 30 points ○: 18 to 23 points Δ: 12 to 17 points ×: 6 to 11 points
実施例１〜１４の製剤と比較例１〜８の製剤との比較より、局所麻酔剤、尿素、清涼化剤、低級アルコール及び水を含有し、それら各成分が本発明の範囲で含有される場合に、４種類の評価項目全てにおいて「○」又は「◎」の評価（１８点以上の評価）となることが示された。また、比較例９の製剤は従来の軟膏剤のモデルであるが、実施例１〜１４の製剤は従来の軟膏剤と比較しても各評価項目において優れていた。 From the comparison between the preparations of Examples 1 to 14 and the preparations of Comparative Examples 1 to 8, it contains a local anesthetic, urea, a cooling agent, a lower alcohol and water, and each of these components is contained within the scope of the present invention. In this case, it was shown that all four types of evaluation items were evaluated as “◯” or “◎” (evaluation of 18 points or more). Moreover, although the formulation of the comparative example 9 is a model of the conventional ointment, the formulation of Examples 1-14 was excellent in each evaluation item compared with the conventional ointment.
また、実施例１〜４および１０の製剤については使用感（ベタツキ）の評価も行った。その結果、実施例１の製剤と比較して実施例２〜４及び１０の製剤はベタツキが少なく優れていた（データ示さず）。すなわち、低級アルコールの量が２０〜３９重量％の範囲にあると使用感に優れていた。 Moreover, the usability (stickiness) was also evaluated for the preparations of Examples 1 to 4 and 10. As a result, compared with the preparation of Example 1, the preparations of Examples 2 to 4 and 10 were excellent with little stickiness (data not shown). That is, when the amount of the lower alcohol was in the range of 20 to 39% by weight, the feeling in use was excellent.
処方例
表４に示した組成を、常法によりクリーム剤、乳剤、液剤、エアゾール剤、ゲル剤に製した。なお、エアゾール剤は、薬液：噴射剤＝１：４でアルミ缶に充填し、エアゾール剤とした。また、表中、ＢＨＴはジブチルヒドロキシトルエンを意味する。
Formulation Example The composition shown in Table 4 was prepared into creams, emulsions, solutions, aerosols and gels by conventional methods. The aerosol agent was filled in an aluminum can with chemical solution: propellant = 1: 4 to obtain an aerosol agent. In the table, BHT means dibutylhydroxytoluene.
本発明の皮膚外用剤は、かゆみの抑制を目的とした皮膚外用剤の分野で有用である。 The external preparation for skin of the present invention is useful in the field of external preparation for skin intended to suppress itching.
Claims (8)
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| JP2006092523A JP5170973B2 (en) | 2006-03-29 | 2006-03-29 | Topical skin preparation |
| PCT/JP2007/056879 WO2007111370A1 (en) | 2006-03-29 | 2007-03-29 | Agent for external application to the skin |
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| JP5761678B2 (en) * | 2008-05-20 | 2015-08-12 | 株式会社大塚製薬工場 | Anti-itching agent for external use on skin |
| US8142592B2 (en) | 2008-10-02 | 2012-03-27 | Mylan Inc. | Method for making a multilayer adhesive laminate |
| EP2450036B1 (en) | 2009-07-02 | 2016-06-15 | Yamaguchi University | Surface anesthetic agent |
| JP5756676B2 (en) * | 2011-05-18 | 2015-07-29 | 株式会社クロイスターズ | Topical skin preparation |
| KR102597992B1 (en) * | 2020-08-25 | 2023-11-06 | 이나래 | Composition for relieving and treating anal itching and anal pad comprising same |
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| JP3575033B2 (en) * | 1993-10-28 | 2004-10-06 | 大正製薬株式会社 | External preparation |
| JP3487633B2 (en) * | 1994-04-28 | 2004-01-19 | 祐徳薬品工業株式会社 | Skin disease treatment emulsion |
| JP3486477B2 (en) * | 1995-03-29 | 2004-01-13 | 株式会社資生堂 | External preparation for skin |
| JPH11255640A (en) * | 1998-03-12 | 1999-09-21 | Shiseido Co Ltd | Emulsified preparation for external use for skin |
| AU2001252600A1 (en) * | 2000-04-26 | 2001-11-07 | Kowa Co. Ltd. | Urea-containing gel preparation |
| JP2002114688A (en) * | 2000-10-02 | 2002-04-16 | Tanpei Seiyaku Kk | Skin care preparation |
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| JP2003012497A (en) * | 2001-04-25 | 2003-01-15 | Eisai Co Ltd | Urea-containing composition for external use |
| JP2005001994A (en) * | 2003-04-14 | 2005-01-06 | Shiseido Co Ltd | Urea-containing aerosol preparation |
| JP2005263660A (en) * | 2004-03-17 | 2005-09-29 | Shiseido Co Ltd | Urea-containing external preparation for skin |
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