JP2008088094A - Antipruritic agent - Google Patents
Antipruritic agent Download PDFInfo
- Publication number
- JP2008088094A JP2008088094A JP2006269952A JP2006269952A JP2008088094A JP 2008088094 A JP2008088094 A JP 2008088094A JP 2006269952 A JP2006269952 A JP 2006269952A JP 2006269952 A JP2006269952 A JP 2006269952A JP 2008088094 A JP2008088094 A JP 2008088094A
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- JP
- Japan
- Prior art keywords
- bht
- weight
- antipruritic agent
- present
- antipruritic
- 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
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- 239000003908 antipruritic agent Substances 0.000 title claims abstract description 47
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Classifications
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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
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
- A61K31/05—Phenols
-
- 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
-
- 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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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Dermatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
本発明は、かゆみ抑制効果に優れた鎮痒剤に関する。 The present invention relates to an antipruritic agent having an excellent itching suppression effect.
「かゆみ」は、「皮膚を掻破したいという観念を起こさせる感覚」と定義され、概ね不快となる感覚である。「かゆみ」を伴う症状としては、例えばアトピー性皮膚炎、しっしん、虫さされ、乾燥肌、知覚過敏肌等の多様なものがあり、その病態によって、抗ヒスタミン剤、局所麻酔剤、保湿剤等が使用されている。しかしながら、それらは、効力発揮まで時間を要するなど、適用者に充分な満足が得られていなかった。 “Itching” is defined as “a sensation that raises the idea of wanting to scratch the skin” and is a generally unpleasant sensation. Symptoms associated with “itch” include various forms such as atopic dermatitis, rash, insect bite, dry skin, and hypersensitive skin, and antihistamines, local anesthetics, moisturizers, etc. are used depending on the pathology Has been. However, they have not been fully satisfied with the applicator, for example, it takes time to exert their efficacy.
この様な背景から、かゆみを短時間で効果的に抑制し得る鎮痒剤が求められていた。かゆみを抑制する目的で使用される鎮痒剤は、従来から数多く知られており、例えば、特許文献1には天然油脂と抗酸化剤を配合した皮膚外用剤が開示されている。このような皮膚外用剤中には、保存剤、安定化剤、抗酸化剤等として一般的にブチルヒドロキシトルエンが0.01〜1%程度配合されている。しかしながら、ブチルヒドロキシトルエン自体にかゆみ抑制作用があることは知られていなかった。
本発明は、虫さされ、知覚過敏肌等のかゆみを効果的に抑制することが可能な鎮痒剤を提供することを主な目的とする。 The main object of the present invention is to provide an antipruritic agent capable of effectively suppressing itching such as insect hypersensitivity skin.
本発明者は、鋭意検討を重ねた結果、ブチルヒドロキシトルエン(以下BHTと略記することがある)自体に鎮痒作用があり、BHTを配合した製剤を皮膚に適用すると効果的にかゆみを抑制できることを見出した。BHTは化粧品等の外用剤に広く用いられる成分であるが、専ら酸化防止、安定化等を期待して配合される成分であり、かゆみの軽減を目的として用いることは全く想起されていなかった。本発明は、このような知見に基づき、さらに研究を重ねた結果、完成されたものである。 As a result of extensive studies, the present inventor has found that butylhydroxytoluene (hereinafter sometimes abbreviated as BHT) itself has an antipruritic action, and it is possible to effectively suppress itching when a preparation containing BHT is applied to the skin. I found it. BHT is a component that is widely used in external preparations such as cosmetics, but is a component that is exclusively formulated for anti-oxidation, stabilization, etc., and has never been recalled for use for the purpose of reducing itching. The present invention has been completed as a result of further research based on such knowledge.
本発明は、以下の鎮痒剤を提供する。
項1.ブチルヒドロキシトルエン(以下、BHTと示す)を有効成分とする鎮痒剤。
項2.BHTが製剤100重量%中に1.5重量%溶解状態で配合されている、項1に記載の鎮痒剤。
項3.BHTが固体状態で配合されている、項2に記載の鎮痒剤。
項4.固体状態のBHTが7.5〜40重量%配合されている、項3に記載の鎮痒剤。
項5.固体状態のBHTの粒子径が1000μm以下であることを特徴とする項3又は4に記載の鎮痒剤。
項6.粒子径350μm未満のBHT、粒子径350〜500μmのBHT、粒子径501〜1000μmのBHTを2種以上組み合わせて配合することを特徴とする項3〜5のいずれかに記載の鎮痒剤。
The present invention provides the following antipruritic agents.
Item 1. An antipruritic agent comprising butylhydroxytoluene (hereinafter referred to as BHT) as an active ingredient.
Item 2. Item 2. The antipruritic agent according to Item 1, wherein BHT is formulated in a dissolved state of 1.5% by weight in 100% by weight of the preparation.
Item 3. Item 3. The antipruritic agent according to Item 2, wherein BHT is blended in a solid state.
Item 4. Item 4. The antipruritic agent according to Item 3, wherein 7.5 to 40% by weight of BHT in a solid state is blended.
Item 5. Item 5. The antipruritic agent according to Item 3 or 4, wherein the solid BHT has a particle size of 1000 µm or less.
Item 6. Item 6. The antipruritic agent according to any one of Items 3 to 5, wherein BHT having a particle diameter of less than 350 µm, BHT having a particle diameter of 350 to 500 µm, and BHT having a particle diameter of 501 to 1000 µm are combined in combination.
本発明の鎮痒剤は、BHTを有効成分として含有するものである。BHTは鎮痒効果を発揮し、特に、溶解状態と固体状態の両方のBHTを存在させることにより、溶解状態のBHTの鎮痒作用に加えて、固体状態のBHTが患部に物理的な刺激を与えることができるのでかゆみの抑制に即効性がある。一般的に、かゆい部分を物理的に刺激すると、より一層かゆみが増強される傾向があるが、本発明の鎮痒剤は、いわゆるかゆみのぶり返しを抑えることができ、優れた鎮痒効果を奏するものである。 The antipruritic agent of the present invention contains BHT as an active ingredient. BHT exerts an antipruritic effect, and in particular, in the presence of both dissolved and solid BHT, solid BHT provides physical stimulation to the affected area in addition to the dissolved BHT antipruritic action Because it can, it has immediate effect in suppressing itching. In general, when the itchy part is physically stimulated, the itching tends to be further enhanced, but the antipruritic agent of the present invention can suppress the so-called itching and exhibits an excellent antipruritic effect. is there.
本発明において「かゆみ」とは、前述のように「皮膚を掻破したいという観念を起こさせる感覚」を指す。 In the present invention, “itch” refers to “a sensation that raises the idea of wanting to scratch the skin” as described above.
本発明の鎮痒剤は、有効成分としてBHTを含有することを主な特徴としている。以下、本発明の鎮痒剤の各成分、製造方法、適用等について説明する。 The antipruritic agent of the present invention is characterized mainly by containing BHT as an active ingredient. Hereinafter, each component, manufacturing method, application and the like of the antipruritic agent of the present invention will be described.
(1)ブチルヒドロキシトルエン(BHT)
本発明の鎮痒剤は、BHTを有効成分として含有する。ブチルヒドロキシトルエンは、白色結晶の形状を有する化合物であり、ジブチルヒドロキシトルエンとも呼ばれるが、両者は同じ化合物([(CH3)3C]2C6H2(CH3)OH)を指す。BHTは、従来、化粧料、医薬品、食品等の酸化防止剤、安定化剤等の用途で配合されている。
(1) Butylhydroxytoluene (BHT)
The antipruritic agent of the present invention contains BHT as an active ingredient. Butylhydroxytoluene is a compound having a white crystal shape and is also called dibutylhydroxytoluene, but both refer to the same compound ([(CH 3 ) 3 C] 2 C 6 H 2 (CH 3 ) OH). BHT is conventionally blended for uses such as antioxidants and stabilizers for cosmetics, pharmaceuticals, foods and the like.
BHTとしては、商業的に入手可能なものを用いることができ、例えば、ブチルヒドロキシトルエン(三栄化工株式会社)、ジブチルヒドロキシトルエン(イーストマン ケミカル ジャパン株式会社、上野製薬株式会社、株式会社エーピーアイコーポレーション、住友化学工業株式会社、長瀬産業株式会社、日揮ユニバーサル株式会社、三菱ウェルファーマ株式会社)等が挙げられる。 As BHT, commercially available products can be used. For example, butylhydroxytoluene (Sanei Chemical Co., Ltd.), dibutylhydroxytoluene (Eastman Chemical Japan Co., Ltd., Ueno Pharmaceutical Co., Ltd., API Corporation). , Sumitomo Chemical Co., Ltd., Nagase Sangyo Co., Ltd., JGC Universal Co., Ltd., Mitsubishi Pharma Co., Ltd.).
本発明におけるBHTの配合量は、とくに限定されないが、溶解状態のBHTで製剤100重量%中に1.5重量%以上であり、好ましくは2〜15重量%程度、より好ましくは5〜15重量%程度、さらに好ましくは7.5〜15重量%程度である。溶解状態のBHTがこの範囲内であると、特に優れた鎮痒効果を得ることができるとともに製剤として安定なものにすることができる。 The blending amount of BHT in the present invention is not particularly limited, but it is 1.5% by weight or more in 100% by weight of the dissolved BHT, preferably about 2 to 15% by weight, more preferably 5 to 15% by weight. %, More preferably about 7.5 to 15% by weight. When the dissolved BHT is in this range, a particularly excellent antipruritic effect can be obtained and the preparation can be made stable.
また、本発明において、溶解状態のBHTの配合量が少ない(例えば、5重量%以下)場合であっても、BHTを固体状態で存在させることにより、患部へ塗布する際に固体状態のBHTが患部に適度な物理的刺激を与え、かゆみを刺激感に置換し、優れた鎮痒効果を発揮することができる。ここで、「かゆみを刺激感に置換する」とは、短期的(瞬間的に)に皮膚感覚を「かゆみ」以外の刺激(例えば、掻いた感じ)を感じる状態にすることを指す。 Further, in the present invention, even when the amount of dissolved BHT is small (for example, 5% by weight or less), when BHT is present in the solid state, the BHT in the solid state can be obtained when applied to the affected area. Appropriate physical stimulation can be given to the affected area, itching can be replaced with a feeling of stimulation, and an excellent antipruritic effect can be exhibited. Here, “replacing itching with a sense of irritation” refers to making the skin sensation feel a stimulus (for example, a scratched feeling) other than “itching” in a short time (instantaneously).
本発明に使用されるBHTは固体状態で配合する場合、BHTの粒子径は1000μm以下程度であり、好ましくは1000〜50μm程度、より好ましくは1000〜100μm程度、さらに好ましくは1000〜180μm程度である。ここで、各粒子径を有するBHTは、BHTを乳鉢などで粉砕した後、各径を有する篩等に供することで得ることができる。 When the BHT used in the present invention is blended in a solid state, the particle diameter of the BHT is about 1000 μm or less, preferably about 1000 to 50 μm, more preferably about 1000 to 100 μm, and still more preferably about 1000 to 180 μm. . Here, BHT having each particle diameter can be obtained by pulverizing BHT with a mortar or the like and then applying it to a sieve having each diameter.
また、本発明においては異なる粒子径を有する固体状態のBHTを組み合わせて用いることによって、より優れた効果が得られることから、2種以上の粒子径を有するBHTを組み合わせて配合することが望ましく、例えば、粒子径350μm未満のBHT、粒子径350〜500μmのBHT、粒子径501〜1000μmのBHTを2種以上を組み合わせて用いることができる。好ましい組み合わせとしては、例えば、(a)501〜1000μm程度の粒子径を有するBHT及び350〜500μm程度の粒子径を有するBHTの組み合わせ;(b)350μm未満程度の粒子径を有するBHT及び350〜500μm程度の粒子径を有するBHTの組み合わせ等が挙げられる。 Further, in the present invention, by using a combination of BHT in a solid state having different particle sizes, a more excellent effect can be obtained. Therefore, it is desirable to combine BHTs having two or more particle sizes in combination. For example, BHT having a particle diameter of less than 350 μm, BHT having a particle diameter of 350 to 500 μm, and BHT having a particle diameter of 501 to 1000 μm can be used in combination of two or more. Preferred combinations include, for example, (a) a combination of BHT having a particle size of about 501 to 1000 μm and BHT having a particle size of about 350 to 500 μm; (b) BHT having a particle size of less than 350 μm and 350 to 500 μm Examples thereof include a combination of BHT having a particle size of about.
2種以上の粒子径を有するBHTを組み合わせて用いる場合、各粒子径を有するBHTの配合割合は、痒みの刺激感への置換作用を発揮し得る範囲であれば適宜設定することができるが、例えば、上記(a)の組み合わせであれば、350〜500μm程度の粒子径を有するBHT1重量部とした場合、501〜1000μm程度の粒子径を有するBHTを0.1〜10重量部程度、好ましくは0.25〜7.5重量部程度、より好ましくは0.5〜5重量部程度;上記(b)の組み合わせであれば、350〜500μm程度の粒子径を有するBHT1重量部とした場合、350μm未満程度の粒子径を有するBHTを、0.1〜10重量部程度、好ましくは0.25〜7.5重量部程度、より好ましくは0.5〜5重量部程度の割合で組み合わせて用いる。 When BHT having two or more particle sizes is used in combination, the blending ratio of BHT having each particle size can be set as appropriate as long as it can exert a substitution effect on the irritating feeling of itchiness. For example, in the case of the above combination (a), when 1 part by weight of BHT having a particle diameter of about 350 to 500 μm is used, BHT having a particle diameter of about 501 to 1000 μm is about 0.1 to 10 parts by weight, preferably About 0.25 to 7.5 parts by weight, more preferably about 0.5 to 5 parts by weight; in the case of the combination (b) above, 350 parts by weight of BHT having a particle diameter of about 350 to 500 μm BHT having a particle size of less than about 0.1 to 10 parts by weight, preferably about 0.25 to 7.5 parts by weight, more preferably about 0.5 to 5 parts by weight. It used after.
本発明の限定的解釈を望むものではないが、本発明の鎮痒剤に粒子径が不均一なBHTを配合することによって、さまざまな刺激感を与えることができ、より顕著に本発明の効果が奏されると考えられる。 Although a limited interpretation of the present invention is not desired, various stimuli can be imparted by blending BHT having a non-uniform particle size with the antipruritic agent of the present invention, and the effects of the present invention are more prominent. It is thought that it is played.
本発明の鎮痒剤における固体状態のBHTの配合量は、鎮痒効果と製剤としての安定性を考慮して、製剤100重量%中に7.5〜40重量%程度、好ましくは8〜35重量%程度、より好ましくは10〜30重量%程度である。 The blending amount of BHT in the solid state of the antipruritic agent of the present invention is about 7.5 to 40% by weight, preferably 8 to 35% by weight in 100% by weight of the preparation in consideration of the antipruritic effect and the stability as the preparation. The degree is more preferably about 10 to 30% by weight.
また、本発明の鎮痒剤におけるBHTの総量は、約1.5重量%以上、好ましくは約7.5重量%以上、より好ましくは9〜45重量%程度、さらに好ましくは10〜35重量%程度、とくに好ましくは10〜30重量%程度である。このような配合量であれば、本発明のかゆみの抑制効果がより顕著に発揮され、かつ製剤として安定したものとすることができる。 The total amount of BHT in the antipruritic agent of the present invention is about 1.5% by weight or more, preferably about 7.5% by weight or more, more preferably about 9 to 45% by weight, and still more preferably about 10 to 35% by weight. Particularly preferably, it is about 10 to 30% by weight. With such a blending amount, the itching suppression effect of the present invention can be exhibited more remarkably and can be stabilized as a preparation.
(2)その他の成分
本発明の鎮痒剤には、前記BHTの他、必要に応じてアルコールが配合される。アルコールはBHTを溶解する際に用いることができ、例えば、BHT1重量部に対して、アルコールを約3重量部より多く配合することでBHTを溶解させることができる。
(2) Other components The antipruritic agent of this invention is mix | blended with alcohol as needed other than said BHT. Alcohol can be used when dissolving BHT. For example, BHT can be dissolved by blending more than about 3 parts by weight of alcohol with respect to 1 part by weight of BHT.
本発明において使用されるアルコールとしては、化粧料、医薬品の分野において一般的に使用されているものであれば特に限定されないが、例えば、メタノール、エタノール、プロパノール、イソプロパノール、ブタノール、イソブタノール等の炭素数1〜6、好ましくは炭素数1〜3の低級アルコール;プロピレングリコール、ジプロピレングリコール、グリセリン、1,3−ブチレングリコール、ブチレングリコール、濃グリセリン、ポリエチレングリコール、マルチトール、マンニトール、ソルビトール等の多価アルコールなどが例示される。これらを1種単独で使用してもよく、2種以上を組み合わせて用いてもよい。また、低級アルコールは、無水、含水の別を問わない。本発明においては、(含水)エタノール、無水エタノール、イソプロパノールを用いることが好ましい。 The alcohol used in the present invention is not particularly limited as long as it is generally used in the cosmetics and pharmaceutical fields. For example, carbon such as methanol, ethanol, propanol, isopropanol, butanol, and isobutanol is used. A lower alcohol having 1 to 6 carbon atoms, preferably 1 to 3 carbon atoms; many such as propylene glycol, dipropylene glycol, glycerin, 1,3-butylene glycol, butylene glycol, concentrated glycerin, polyethylene glycol, maltitol, mannitol, sorbitol, etc. Examples thereof include monohydric alcohols. These may be used alone or in combination of two or more. The lower alcohol may be anhydrous or hydrated. In the present invention, it is preferable to use (hydrous) ethanol, absolute ethanol, or isopropanol.
本発明の鎮痒剤におけるアルコールの配合量は、本発明の効果を損なわない限り特に限定されないが、例えば、0〜92重量%程度、好ましくは5〜92重量%程度、より好ましくは5〜86.2重量%程度、さらに好ましくは5〜61重量%程度である。ただし、固体状態のBHTを含有させる場合は、製剤中のBHT1重量部に対して、アルコール約3重量部以下、好ましくは2重量部以下、より好ましくは1重量部以下となるようにすることが望ましい。 Although the compounding quantity of the alcohol in the antipruritic agent of this invention is not specifically limited unless the effect of this invention is impaired, For example, about 0-92 weight%, Preferably it is about 5-92 weight%, More preferably, it is 5-86. About 2% by weight, more preferably about 5 to 61% by weight. However, when BHT in a solid state is contained, the amount of alcohol should be about 3 parts by weight or less, preferably 2 parts by weight or less, more preferably 1 part by weight or less with respect to 1 part by weight of BHT in the preparation. desirable.
さらに、本発明の鎮痒剤には、必要に応じて水、水溶性高分子等を配合してもよい。水溶性高分子としては、従来公知のものを使用することができるが、例えばカルボキシビニルポリマー、ポリビニルアルコール、ポリビニルメチルエーテル、ポリビニルピロリドン、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、ヒドロキシエチルセルロース、プルラン、寒天、ゼラチン、アルギン酸及びその塩、カラギーナン、ガム類(例えばグアーガム、タマリンドガム、ローカストビーンガム、カラヤガム、トラガカントガム)等が挙げられる。これらを1種単独で使用してもよく、2種以上を組み合わせて用いてもよい。 Furthermore, you may mix | blend water, a water-soluble polymer, etc. with the antipruritic agent of this invention as needed. As the water-soluble polymer, conventionally known polymers can be used. For example, carboxyvinyl polymer, polyvinyl alcohol, polyvinyl methyl ether, polyvinyl pyrrolidone, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, pullulan, agar, gelatin , Alginic acid and salts thereof, carrageenan, gums (eg guar gum, tamarind gum, locust bean gum, Karaya gum, tragacanth gum) and the like. These may be used alone or in combination of two or more.
本発明の鎮痒剤における水の配合量は、例えば、0〜87重量%程度、好ましくは3〜86.2重量%程度、より好ましくは28〜80重量%程度;水溶性高分子の配合量は、例えば、0.5〜5重量%程度、好ましくは0.8〜4重量%程度、より好ましくは1〜3重量%程度である。 The amount of water in the antipruritic agent of the present invention is, for example, about 0 to 87% by weight, preferably about 3 to 86.2% by weight, more preferably about 28 to 80% by weight; For example, about 0.5 to 5% by weight, preferably about 0.8 to 4% by weight, more preferably about 1 to 3% by weight.
本発明の典型的な処方例としては、BHTを10〜35重量%、アルコールを5〜86.2重量%、水溶性高分子を0.8〜4重量%、水3〜86.2重量%含有する鎮痒剤が例示される。 Typical examples of the present invention include 10 to 35% by weight of BHT, 5 to 86.2% by weight of alcohol, 0.8 to 4% by weight of water-soluble polymer, and 3 to 86.2% by weight of water. The contained antipruritic agent is illustrated.
本発明の鎮痒剤には、上記以外にも必要に応じて、化粧料、医薬部外品、医薬品に一般的に用いられる各種成分、水性成分、油性成分、保湿成分、賦形剤、増粘剤、防腐剤、酸化防止剤、pH調整剤、担体、香料、色剤、薬剤等を単独又は2種以上を混合と組み合わせて各種剤型に調製することもできる。また、本発明の鎮痒剤には、本発明の効果を損なわない範囲内で、公知の局所麻酔剤、消炎剤、保湿剤等を含んでもよく、例えば、リドカイン、ジブカイン、塩酸ジブカイン、ジフェンヒドラミン、アミノ安息香酸エチル、デシットテシチン等の局所麻酔剤;マレイン酸クロルフェニラミン、ジフェンヒドラミン、塩酸ジフェンヒドラミン、グリチルレチン酸、グリチルリチン酸二カリウム、グリチルリチン酸モノアンモニウム、アラントイン、サリチル酸メチル等の消炎剤;l−メントール、dl−メントール、カンフル、dl−カンフル、乳酸メンチル等の清涼化剤;尿素、サリチル酸、ヒアルロン酸ナトリウム等の保湿剤;イソプロピルメチルフェノール(IPMP)、第四級アンモニウム塩(塩化ベンザルコニウム、塩化ベンゼトニウムなど)、塩酸クロルヘキシジン、スルファジアジン等の殺菌剤;硝酸オキシコナゾール、塩酸ブテナフィン、塩酸アモロルフィン、塩酸テルビナフィン、ラノコナゾール等の抗真菌剤;トウガラシチンキ、カプサイシン等の温熱成分等が挙げられる。 In addition to the above, the antipruritic agent of the present invention includes various components generally used in cosmetics, quasi-drugs, pharmaceuticals, aqueous components, oily components, moisturizing components, excipients, thickeners as necessary. Agents, preservatives, antioxidants, pH adjusters, carriers, fragrances, colorants, drugs and the like can be prepared in various dosage forms singly or in combination of two or more. Further, the antipruritic agent of the present invention may contain a known local anesthetic, anti-inflammatory agent, moisturizing agent and the like within a range not impairing the effects of the present invention, such as lidocaine, dibucaine, dibucaine hydrochloride, diphenhydramine, amino Local anesthetics such as ethyl benzoate and desittecitin; anti-inflammatory agents such as chlorpheniramine maleate, diphenhydramine, diphenhydramine hydrochloride, glycyrrhetinic acid, dipotassium glycyrrhizinate, monoammonium glycyrrhizinate, allantoin, methyl salicylate; l-menthol, dl- Refreshing agents such as menthol, camphor, dl-camphor and menthyl lactate; moisturizers such as urea, salicylic acid and sodium hyaluronate; isopropylmethylphenol (IPMP), quaternary ammonium salts (benzalkonium chloride, benzethoni chloride) Beam, etc.), fungicides such as chlorhexidine, sulfadiazine; nitric oxiconazole, butenafine hydrochloride, amorolfine hydrochloride, terbinafine hydrochloride, antifungal agents such as lanoconazole; capsicum tincture, thermal component of capsaicin and the like, and the like.
本発明の鎮痒剤の剤型としては、使用方法や適用部分に従って従来公知の剤型に調製することができるが、例えば、軟膏、ローション、ゲル、エアゾール剤等が挙げられる。 The dosage form of the antipruritic agent of the present invention can be prepared in a conventionally known dosage form according to the method of use and application part, and examples thereof include ointments, lotions, gels, aerosols and the like.
本発明の鎮痒剤には、所望の剤型とするための基剤が適当量含有される。例えば、これに限られるものではないが、パラフィン、ワセリン、スクワラン、パラフィン、白ロウ、プラスチベース、ポリエチレングリコール、マクロゴール、ラウロマクロゴール、シリコン油、シリコン、ポリソルベート、ポリオキシエチレン硬化ヒマシ油、オリーブ油、綿実油、大豆油、ヤシ油などの油系基剤;セタノール、ステアリルアルコールなどの高級アルコール;脂肪酸エステル(ミリスチン酸イソプロピル、ソルビタン脂肪酸エステルなど)、高級脂肪酸塩型乳化剤、高度精製卵黄レシチン、大豆レシチン、精製大豆レシチン、サラシミツロウ、プロピレンカーボネート、卵黄リン脂質、卵黄油、ヤシ油脂肪酸、ラウリル硫酸ナトリウム、その他イオン性、非イオン性界面活性剤などの乳化剤;リン酸、酢酸、塩酸、水酸化ナトリウムなどのpH調整剤;液化石油ガス、ジメチルエーテルなどの噴射剤などが挙げられる。 The antipruritic agent of the present invention contains an appropriate amount of a base for obtaining a desired dosage form. For example, but not limited to, paraffin, petrolatum, squalane, paraffin, white wax, plastibase, polyethylene glycol, macrogol, lauro macrogol, silicone oil, silicone, polysorbate, polyoxyethylene hydrogenated castor oil, olive oil, Oil bases such as cottonseed oil, soybean oil, coconut oil; higher alcohols such as cetanol and stearyl alcohol; fatty acid esters (isopropyl myristate, sorbitan fatty acid ester, etc.), higher fatty acid salt type emulsifiers, highly purified egg yolk lecithin, soybean lecithin, Purified soybean lecithin, white beeswax, propylene carbonate, egg yolk phospholipid, egg yolk oil, coconut oil fatty acid, sodium lauryl sulfate, and other ionic and nonionic surfactants; phosphoric acid, acetic acid, hydrochloric acid, hydroxylation pH adjusting agents such as thorium; liquefied petroleum gas, and the like propellants such as dimethyl ether.
本発明の鎮痒剤は、以上の成分を従来公知の方法に従って混合し、調製することができる。調製における温度、各成分の添加の順番、混合時間等の条件は、各成分の物理的又は化学的性質、濃度、機器の応力等に応じ、当該分野の技術常識に基づいて適宜設定することができるが、例えば次の方法が挙げられる。 The antipruritic agent of the present invention can be prepared by mixing the above components according to a conventionally known method. Conditions such as temperature in preparation, order of addition of each component, mixing time, etc. may be set as appropriate based on the common general technical knowledge in the field according to the physical or chemical properties of each component, concentration, instrument stress, etc. For example, the following method can be mentioned.
水溶性成分を水に溶解して水相を調製する。水相とは別に、アルコール溶解性成分及びBHTをアルコールに溶解してアルコール相を調製する。得られた水相及びアルコール相を均質になるように攪拌混合し、本発明の鎮痒剤を得ることができる。また、固体状態のBHTを配合する場合は、攪拌混合後にさらに添加することができる。 An aqueous phase is prepared by dissolving water-soluble components in water. Separately from the aqueous phase, an alcohol-soluble component and BHT are dissolved in alcohol to prepare an alcohol phase. The obtained aqueous phase and alcohol phase are stirred and mixed so as to be homogeneous, whereby the antipruritic agent of the present invention can be obtained. Moreover, when mix | blending BHT of a solid state, it can add further after stirring and mixing.
本発明の鎮痒剤は、かゆみ(掻痒感)を軽減する鎮痒剤として使用することができ、この目的において使用されるのであれば適用対象は特に限定されない。本発明の鎮痒剤の適用対象としては、例えば、しっしん、虫さされ、乾燥肌、知覚過敏肌等のかゆみを伴う症状が挙げられる。 The antipruritic agent of the present invention can be used as an antipruritic agent that reduces itching (itchiness), and the application target is not particularly limited as long as it is used for this purpose. Applicable objects of the antipruritic agent of the present invention include, for example, symptoms associated with itching such as rashes, insect bites, dry skin, and hypersensitive skin.
本発明の鎮痒剤を前記のかゆみの軽減を目的として使用する場合は、皮膚のかゆい部分に本発明の鎮痒剤の適量を塗り広げればよい。塗り広げることによって、BHTの鎮痒作用により、かゆみをぶりかえすことなく抑制することができる。さらに固体状態でBHTを配合した場合には適度な物理的な刺激が伴うためにさらに素早くかゆみを抑制することができる。 When the antipruritic agent of the present invention is used for the purpose of reducing the itching, an appropriate amount of the antipruritic agent of the present invention may be spread over the itchy part of the skin. By spreading the coating, it is possible to suppress the itch without changing itching by the antipruritic action of BHT. Furthermore, when BHT is blended in a solid state, itching can be suppressed more quickly because moderate physical stimulation is involved.
以下に実施例等を示して本発明をより詳細に説明するが、本発明はこれらに限定されない。 Hereinafter, the present invention will be described in more detail with reference to examples and the like, but the present invention is not limited thereto.
下記表1に示される処方に基づいて各種成分を配合し、製剤を得た。具体的には、水を攪拌しながらカルボキシビニルポリマーを徐々に添加し、さらに攪拌混合して水相を調製した。水相とは別に、アルコール(無水エタノール及びプロピレングリコール)、BHT(ブチルヒドロキシトルエン:三栄化工株式会社)及びトリエタノールアミンを攪拌混合してアルコール相を調製した。前記で得られた水相を攪拌しながら、アルコール相を徐々に添加し、さらに攪拌混合することによって各製剤を得た。固体状態のBHTを配合する場合は、水相とアルコール相を攪拌した後に添加し、さらに攪拌混合して製した。ここで、BHTは、乳鉢中で粉砕し、各径を有する篩で分類したものを用いた。 Various components were blended based on the formulation shown in Table 1 below to obtain a preparation. Specifically, carboxyvinyl polymer was gradually added while stirring water, and further stirred and mixed to prepare an aqueous phase. Separately from the aqueous phase, alcohol (anhydrous ethanol and propylene glycol), BHT (butylhydroxytoluene: Sanei Chemical Co., Ltd.) and triethanolamine were mixed with stirring to prepare an alcohol phase. While stirring the aqueous phase obtained above, the alcohol phase was gradually added and further stirred and mixed to obtain each preparation. When blending BHT in a solid state, the aqueous phase and the alcohol phase were added after stirring, and further mixed by stirring. Here, BHT used was crushed in a mortar and classified by a sieve having each diameter.
得られた製剤を常温(約25℃)にて1週間保存した後、その性状を目視により確認し、安定性を評価した。具体的には、分散性(BHT粒子の沈降や団粒化(粒子の凝集)の有無)、保型性(粘度低下等の初期性状と比較した場合の明らかな変化の有無)、BHT粒子が固体の性状を維持しているかどうか(軟化、溶解の有無)について確認した。これらの性状のいずれにも変化が無かった場合は○とし、いずれか1つでも変化が確認された場合は×とした。 The obtained preparation was stored at room temperature (about 25 ° C.) for 1 week, and then its properties were visually confirmed to evaluate the stability. Specifically, dispersibility (presence or absence of BHT particle sedimentation or agglomeration (aggregation of particles)), shape retention (presence or absence of obvious change when compared with initial properties such as viscosity reduction), BHT particles are It was confirmed whether or not the solid property was maintained (softening / dissolving). When there was no change in any of these properties, it was marked as ◯, and when any one of the changes was confirmed, it was marked as x.
さらに、安定性の評価結果が「○」の製剤を、虫さされ等によるかゆみを訴える被験者10名の患部に塗布し、各製剤の効果を5段階で評価した。評価は、非常にかゆい場合を1点、全くかゆくない場合を5点とした。また、製剤の適用しやすさ(塗布しにくい場合を1点、非常に塗布しやすい場合を5点)、かゆみの刺激感(掻いた感じ)への置換(刺激感に置換されにくい場合を1点、刺激感に置換されやすい場合を5点)に関する評価も併せて行った。なお、かゆみの刺激感への置換についての評価は、実施例1〜6と比較例1〜2の製剤を使用した場合のみ評価した。 Furthermore, a preparation with a stability evaluation result of “◯” was applied to the affected area of 10 subjects complaining of itching caused by insect bites and the like, and the effect of each preparation was evaluated in five stages. Evaluation was made 1 point when it was very itchy and 5 points when it was not itchy at all. In addition, ease of application of the preparation (1 point when it is difficult to apply, 5 points when it is very easy to apply), replacement of itching with a feeling of irritation (scratch feeling) (1 when it is difficult to be replaced with a feeling of irritation) In addition, evaluation was also performed on 5 points). In addition, evaluation about the substitution to the irritation feeling of an itch was evaluated only when the preparations of Examples 1 to 6 and Comparative Examples 1 and 2 were used.
各被験者による評点を合計し、合計点が45〜50点:◎、35〜45点:○、25〜35点;△、25点未満:×とした。 The score by each subject was totaled, and the total score was 45-50 points: ◎, 35-45 points: ○, 25-35 points; Δ, less than 25 points: x.
これらの評価結果を表1に示す。表中、CVPはカルボキシビニルポリマー、HPCはヒドロキシプロピルセルロース、PGはプロピレングリコール、EDTAはエチレンジアミン四酢酸を表す。 These evaluation results are shown in Table 1. In the table, CVP represents carboxyvinyl polymer, HPC represents hydroxypropylcellulose, PG represents propylene glycol, and EDTA represents ethylenediaminetetraacetic acid.
なお、比較例3は保型性を有さない液状を呈し、比較例6は白濁した軟膏状を呈した。 In addition, the comparative example 3 exhibited the liquid which does not have a shape retention property, and the comparative example 6 exhibited the cloudy ointment form.
表1に示される結果より、BHT(溶解状態)を含有する製剤(特に実施例7〜11)は、比較例4〜6等に含まれる鎮痒作用を有する化合物と同等以上の優れた痒み止め効果を発揮することが示された。さらに、溶解状態のBHTに加えて固体状態のBHTを含有する製剤(実施例1〜6)は、かゆみ止め効果に加えて、かゆみを刺激感に置換する作用にも優れていることが示された。すなわち、本発明における鎮痒剤は、即効性かつ持続性のあるかゆみ抑制効果に優れていることが示された。特に2種類の粒子径を有する固体状態のBHTを含有する鎮痒剤(実施例2〜6)は、より優れたかゆみを刺激感に置換する作用、すなわち即効性のある痒み抑制効果を発揮し得ることが示された。また、溶解状態のBHTを製剤中に1重量%と低濃度で含有した場合、かゆみ抑制効果はみられなかったが(比較例7)、固体状態のBHTと組み合わせて用いることで、かゆみを刺激感に置換する作用が溶解状態のBHTによるかゆみ抑制効果を補い、全体として優れたかゆみ抑制効果を発揮することが示された(実施例6)。 From the results shown in Table 1, the preparations containing BHT (dissolved state) (particularly Examples 7 to 11) have excellent anti-smearing effects equivalent to or better than the compounds having an antipruritic action contained in Comparative Examples 4 to 6 and the like. It was shown to exert. Furthermore, it is shown that the preparations (Examples 1 to 6) containing BHT in a solid state in addition to BHT in a dissolved state are excellent in the action of replacing itching with a stimulating feeling in addition to the anti-itching effect. It was. That is, it was shown that the antipruritic agent in the present invention is excellent in an immediate and long-lasting itch suppression effect. In particular, the antipruritic agent (Examples 2 to 6) containing BHT in a solid state having two types of particle diameters can exhibit an effect of substituting itching with a better sensation, that is, an immediate itch suppression effect. It was shown that. Moreover, when the dissolved BHT was contained in the preparation at a low concentration of 1% by weight, no itching suppression effect was observed (Comparative Example 7), but it was stimulated by using it in combination with the solid BHT. It was shown that the action of substituting with the feeling compensated for the itching suppression effect by the dissolved BHT, and exhibited an excellent itching suppression effect as a whole (Example 6).
一方、従来BHTと同様に安定化剤、酸化防止剤として知られている固体、液体の化合物を含有させた製剤(比較例1及び2)では、痒み止め効果は認められないばかりか、かゆみを刺激感に置換する作用も有していなかった。比較例3に至っては、製剤の安定性が悪く、実際に適用することができなかった。 On the other hand, in the preparations (Comparative Examples 1 and 2) containing solid and liquid compounds known as stabilizers and antioxidants as in the case of conventional BHT, not only the anti-itching effect is observed, but also itching. It did not have the effect of substituting irritation. In Comparative Example 3, the formulation was poor in stability and could not be actually applied.
以下に処方例を示す。 A prescription example is shown below.
(表2続き)
(Continued in Table 2)
処方例1〜23、25および26は、ゲル状製剤(軟膏剤)である。また、処方例24は、粘性の液状製剤である。処方例24は、噴射剤とともに充填してエアゾール剤に製することができる。 Formulation Examples 1 to 23, 25 and 26 are gel preparations (ointments). Moreover, the formulation example 24 is a viscous liquid preparation. Formulation Example 24 can be made into an aerosol by filling with a propellant.
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JPS63255219A (en) * | 1987-04-11 | 1988-10-21 | Teikoku Seiyaku Kk | Antipruritic plaster |
JPS63255224A (en) * | 1987-04-11 | 1988-10-21 | Teikoku Seiyaku Kk | Antipruritic plaster |
JPH04103526A (en) * | 1990-08-21 | 1992-04-06 | Taisho Pharmaceut Co Ltd | Aerosol for skin cooling |
JPH07126158A (en) * | 1993-10-27 | 1995-05-16 | Taisho Pharmaceut Co Ltd | Crotamiton-blended external preparation |
JP2001233764A (en) * | 2000-02-22 | 2001-08-28 | Hisamitsu Pharmaceut Co Inc | Antipruritic agent comprising n-substituted-o-toluidine derivative |
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JPS63255219A (en) * | 1987-04-11 | 1988-10-21 | Teikoku Seiyaku Kk | Antipruritic plaster |
JPS63255224A (en) * | 1987-04-11 | 1988-10-21 | Teikoku Seiyaku Kk | Antipruritic plaster |
JPH04103526A (en) * | 1990-08-21 | 1992-04-06 | Taisho Pharmaceut Co Ltd | Aerosol for skin cooling |
JPH07126158A (en) * | 1993-10-27 | 1995-05-16 | Taisho Pharmaceut Co Ltd | Crotamiton-blended external preparation |
JP2001233764A (en) * | 2000-02-22 | 2001-08-28 | Hisamitsu Pharmaceut Co Inc | Antipruritic agent comprising n-substituted-o-toluidine derivative |
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