JP2022020578A - Cosmetic external preparation and cosmetic - Google Patents

Cosmetic external preparation and cosmetic Download PDF

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JP2022020578A
JP2022020578A JP2021116514A JP2021116514A JP2022020578A JP 2022020578 A JP2022020578 A JP 2022020578A JP 2021116514 A JP2021116514 A JP 2021116514A JP 2021116514 A JP2021116514 A JP 2021116514A JP 2022020578 A JP2022020578 A JP 2022020578A
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external preparation
fat
cosmetic
agent
acid
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英淑 権
Eishuku Gon
千明 原
Chiaki Hara
文男 神山
Fumio Kamiyama
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CosMED Pharmaceutical Co Ltd
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CosMED Pharmaceutical Co Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/047—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates having two or more hydroxy groups, e.g. sorbitol
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    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
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    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
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    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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    • A61K31/66—Phosphorus compounds
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
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    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
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    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A—HUMAN NECESSITIES
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    • 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
    • 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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    • 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
    • A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
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    • 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
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A—HUMAN NECESSITIES
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    • 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
    • A61K8/55—Phosphorus compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
    • A61K8/66—Enzymes
    • A—HUMAN NECESSITIES
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    • A61K8/67—Vitamins
    • A—HUMAN NECESSITIES
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    • A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L15/00—Chemical aspects of, or use of materials for, bandages, dressings or absorbent pads
    • A61L15/16—Bandages, dressings or absorbent pads for physiological fluids such as urine or blood, e.g. sanitary towels, tampons
    • A61L15/20—Bandages, dressings or absorbent pads for physiological fluids such as urine or blood, e.g. sanitary towels, tampons containing organic materials
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    • A61L15/16—Bandages, dressings or absorbent pads for physiological fluids such as urine or blood, e.g. sanitary towels, tampons
    • A61L15/22—Bandages, dressings or absorbent pads for physiological fluids such as urine or blood, e.g. sanitary towels, tampons containing macromolecular materials
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Abstract

To provide novel administration means of a valuable material having fat-dissolving action.SOLUTION: A tape agent, a patch agent or a cataplasm which contains any one or more kinds of a fat-decomposing agent, a fat-dissolving agent or a fat metabolism promoter, is aimed at fat reduction or/and partial slimming or/and tightening of skin.SELECTED DRAWING: None

Description

本発明は、皮下の脂肪分解・溶解を目的とする外用剤及び化粧料に関する。詳しくは、有価成分として脂肪溶解剤等を主成分として含有する外用剤及び化粧料の技術分野に関する。 The present invention relates to an external preparation and a cosmetic for the purpose of subcutaneous lipolysis / dissolution. More specifically, the present invention relates to the technical fields of external preparations and cosmetics containing a fat dissolving agent or the like as a main component as a valuable component.

脂肪の皮下蓄積は、脂肪細胞の機能障害と関連があり、蓄積されたトリグリセリドが酵素的に分解されて、脂肪酸、グリセロールおよび／またはグリセロールエステルに再分解されている。様々な理由で、脂肪細胞中でトリグリセリドの蓄積が起こり、脂肪の皮下蓄積が生じることになる。その結果、過体重、治療上・美容上の問題点となる。 Subcutaneous accumulation of fat is associated with adipocyte dysfunction, where the accumulated triglycerides are enzymatically degraded and redistributed into fatty acids, glycerol and / or glycerol esters. For various reasons, triglyceride accumulation occurs in adipocytes, resulting in subcutaneous fat accumulation. As a result, there are problems in overweight, treatment and beauty.

この皮下の脂肪蓄積や肥満のうち過度の脂肪層を呈する肥満に対しては、脂肪の皮下蓄積を除去する組成物を直接皮下に注入する方法がとられている。これには、サノフィ社（Sanofi-Aventis）のリポスタビル（Lipostabil）に代表されるホスファチジルコリン製剤が使用されている（特許文献１、２）。一方において、デオキシコール酸の皮下注射も知られている。しかし、施術時の痛みや肌腫れなど安全性の点から問題視される状況にあり、リスクの高い方法といえる。また、注射の場合、一定面積に対して注射針を皮下で振って注入しなければならない。さらに、注入した液のむらによって脂肪溶解の都合が変わり、肌の凹凸が生じる。
特許文献３はホスファチジルコリンを用いたワックスのような剤型、特許文献４はカルニチン誘導体からなる液剤を提案している。しかしながら、パッチ剤、パップ剤、テープ剤等の皮膚外用剤についての開発は全くなされていなかった。 For obesity showing an excessive fat layer among the subcutaneous fat accumulation and obesity, a method of directly injecting a composition for removing the subcutaneous fat accumulation is adopted. For this, a phosphatidylcholine preparation represented by Lipostabil of Sanofi-Aventis is used (Patent Documents 1 and 2). On the other hand, subcutaneous injection of deoxycholic acid is also known. However, it can be said that it is a high-risk method because it is in a situation where it is regarded as a problem from the viewpoint of safety such as pain and swelling of the skin during the treatment. In addition, in the case of injection, the injection needle must be shaken subcutaneously for a certain area to inject. Furthermore, the convenience of fat dissolution changes depending on the unevenness of the injected liquid, and unevenness of the skin occurs.
Patent Document 3 proposes a wax-like dosage form using phosphatidylcholine, and Patent Document 4 proposes a liquid preparation composed of a carnitine derivative. However, no development has been made on external skin preparations such as patches, paps, and tapes.

特表２００７－５０９０８５号公報Japanese Patent Publication No. 2007-509085 特表２００７－５１５４３９号公報Special Table 2007-515439A 再表２００９－１２３０８６号公報Re-table 2009-12308 No. 特開２００６－１６３８３号公報Japanese Unexamined Patent Publication No. 2006-16383

本発明の目的は、脂肪溶解作用を有する有価物の新たな投与手段を提供することにある。具体的には脂肪分解、脂肪溶解作用を有する有価物を含有するパッチ状、テープ状、あるいはパップ状の外用剤及び化粧料である。 An object of the present invention is to provide a new means for administering a valuable substance having a fat dissolving action. Specifically, it is a patch-like, tape-like, or pap-like external preparation and cosmetic containing valuable resources having lipolytic and lipolytic effects.

現在まで脂肪溶解を目的とする経皮吸収製剤は全く存在しなかったので、上記の有価物を経皮吸収製剤化する際、有価物の濃度、皮膚適用の頻度等に関する知見は全くなく、有価物の組み合わせ、製剤の安定性及び皮膚移行性をどのようにして確保するのかが重要課題となった。本発明者らは、このような課題を解決し、脂肪溶解作用を有する有価物を含有する外用剤及び化粧料の製造に成功し、本発明を完成するに至った。 Since there has been no transdermal preparation for the purpose of fat dissolution until now, there is no knowledge about the concentration of valuables, frequency of skin application, etc. when converting the above valuables into transdermal preparations, which is valuable. How to ensure the combination of substances, the stability of the pharmaceutical product and the transferability to the skin became important issues. The present inventors have solved such a problem and succeeded in producing an external preparation and a cosmetic containing a valuable resource having a fat-dissolving action, and have completed the present invention.

本発明者らは、パッチ剤、パップ剤、テープ剤等のシート型貼付剤型に有効成分として脂肪溶解剤等を含有させると、有価成分が経皮吸収され脂肪低減又は/及び部分痩せ又は/及び肌引き締めに効果を有する外用剤もしくは化粧料として使用できることを発見し、本発明を完成した。
本発明は、以下に示す通りである。
〔１〕脂肪分解剤、脂肪溶解剤又は脂肪代謝促進剤のいずれか１種以上を含有し、脂肪低減又は/及び部分痩せ又は/及び肌引き締めを目的とする外用剤又は化粧料。
〔２〕脂肪分解剤、脂肪溶解剤及び脂肪代謝促進剤からなる群から選ばれる１種以上の脂肪減少に働く成分を０．１質量％以上含有する脂肪低減又は/及び部分痩せ又は/及び肌引き締めを目的とする外用剤又は化粧料。
〔３〕脂肪分解剤がリパーゼである、〔１〕又は〔２〕に記載の外用剤又は化粧料。
〔４〕リパーゼとＭｇ塩及びＣａ塩とが含まれている、〔３〕に記載の外用剤又は化粧料。
〔５〕脂肪溶解剤がホスファチジルコリン、アデノシン三リン酸及びそのナトリウム塩ならびにデオキシコール酸及びその塩からなる群より選ばれる１種以上である、〔１〕又は〔２〕に記載の外用剤又は化粧料。
〔６〕脂肪代謝促進剤がアミノ酸、Ｌ－カルニチン、イノシトール、カプサイシン及びカフェインからなる群より選ばれる１種以上である、〔１〕又は〔２〕に記載の外用剤又は化粧料。
〔７〕アミノ酸がチロシン、セリン、トレオニン、フェニルアラニン、トリプトファン、イソロイシン、リジン、アルギニン、ベタイン、ヒスチジン、グルタミン、グリシン及びシステインからなる群より選ばれる１種以上である、〔６〕に記載の外用剤又は化粧料。
〔８〕外用剤又は化粧料が貼付シートである、〔１〕～〔７〕のいずれかに記載の外用剤又は化粧料。
〔９〕アクリル系、ゴム系又はシリコーン系粘着剤を基剤とする、〔８〕に記載の外用剤又は化粧料。
〔１０〕水溶性樹脂を基剤とする、〔８〕に記載の外用剤又は化粧料。
〔１１〕ホスファチジルコリンと、アスタキサンチン、酢酸トコフェロール、トコフェロール、パルミチン酸アスコルビル及びジエタノールアミンからなる群より選ばれる1種以上とが共存する外用剤又は化粧料。
〔１２〕デオキシコール酸ナトリウムと酸性物質とが共存する外用剤又は化粧料。
〔１３〕膏体と支持体シートとから構成され、該膏体がアクリル系、ゴム系又はシリコーン系粘着剤中に脂肪分解剤、脂肪溶解剤又は脂肪代謝促進剤のいずれか１種以上を含有し、該支持体シートが不織布、織布、編み布又はポリウレタンフィルムであり、該膏体厚みが５～２００μｍである、〔１〕～〔９〕のいずれかに記載の外用剤又は化粧料。
〔１４〕支持体シートが厚み３～５０μｍのポリウレタンフィルムであり、膏体がロール状粘性シートであり、該膏体厚みが５～１００μｍである、〔１３〕に記載の外用剤又は化粧料。
〔１５〕〔８〕～〔１０〕のいずれかに記載の外用剤又は化粧料の製造方法であって、下記（a）、（b）、又は（c）の工程を含む製造方法：
（a）基剤が溶液型粘着剤の場合、
粘着剤溶液、並びに、脂肪分解剤、脂肪溶解剤及び脂肪代謝促進剤からなる群より選ばれる少なくとも１種の有価物を均一に混合する工程、
得られた粘着剤溶液を離型シート上に塗布し、溶媒を乾燥させる工程、並びに
乾燥させた粘着剤層を必要に応じ支持体シートに積層する工程；
（b）基剤がホットメルト型粘着剤の場合、
粘着性組成物、並びに、脂肪分解剤、脂肪溶解剤及び脂肪代謝促進剤からなる群より選ばれる少なくとも１種の有価物を高温で均一混錬する工程、並びに
得られた粘着剤混合物を離型シートあるいは支持体シートに塗布する工程；
（c）基剤がパップ基剤の場合、
水溶性樹脂、脂肪分解剤、脂肪溶解剤及び脂肪代謝促進剤からなる群より選ばれる少なくとも１種の有価物、並びに、水を均一混錬する工程、並びに
得られた水溶性樹脂組成物を離型シートあるいは支持体シートに塗布する工程。 When the present inventors include a fat dissolving agent or the like as an active ingredient in a sheet-type patch type such as a patch, a poultice, or a tape, the valuable component is percutaneously absorbed to reduce fat or / and partially lose weight or /. And discovered that it can be used as an external preparation or cosmetic having an effect on skin tightening, and completed the present invention.
The present invention is as shown below.
[1] An external preparation or cosmetic containing one or more of a lipolytic agent, a fat dissolving agent or a fat metabolism promoting agent, for the purpose of reducing fat and / and partially thinning or / and tightening the skin.
[2] Fat reduction or / and partial thinning or / and skin containing 0.1% by mass or more of one or more components acting on fat reduction selected from the group consisting of lipolytic agents, fat dissolving agents and fat metabolism promoting agents. External agents or cosmetics for the purpose of tightening.
[3] The external preparation or cosmetic according to [1] or [2], wherein the lipolytic agent is lipase.
[4] The external preparation or cosmetic according to [3], which contains lipase, Mg salt and Ca salt.
[5] The external preparation or cosmetic according to [1] or [2], wherein the fat-dissolving agent is at least one selected from the group consisting of phosphatidylcholine, adenosine triphosphate and sodium salts thereof, and deoxycholic acid and salts thereof. Fee.
[6] The external preparation or cosmetic according to [1] or [2], wherein the fat metabolism promoter is at least one selected from the group consisting of amino acids, L-carnitine, inositol, capsaicin and caffeine.
[7] The external preparation according to [6], wherein the amino acid is at least one selected from the group consisting of tyrosine, serine, threonine, phenylalanine, tryptophan, isoleucine, lysine, arginine, betaine, histidine, glutamine, glycine and cysteine. Or cosmetics.
[8] The external preparation or cosmetic according to any one of [1] to [7], wherein the external preparation or cosmetic is a sticking sheet.
[9] The external preparation or cosmetic according to [8], which is based on an acrylic, rubber-based or silicone-based adhesive.
[10] The external preparation or cosmetic according to [8], which is based on a water-soluble resin.
[11] An external preparation or cosmetic in which phosphatidylcholine and one or more selected from the group consisting of astaxanthin, tocopherol acetate, tocopherol, ascorbyl palmitate and diethanolamine coexist.
[12] An external preparation or cosmetic in which sodium deoxycholate and an acidic substance coexist.
[13] The plaster is composed of a plaster and a support sheet, and the plaster contains one or more of a lipolytic agent, a lipolytic agent or a fat metabolism promoter in an acrylic, rubber or silicone adhesive. The external preparation or cosmetic according to any one of [1] to [9], wherein the support sheet is a non-woven fabric, a woven cloth, a knitted cloth or a polyurethane film, and the plaster thickness is 5 to 200 μm.
[14] The external preparation or cosmetic according to [13], wherein the support sheet is a polyurethane film having a thickness of 3 to 50 μm, the plaster is a roll-shaped viscous sheet, and the plaster has a thickness of 5 to 100 μm.
[15] The method for producing an external preparation or cosmetic according to any one of [8] to [10], which comprises the following steps (a), (b), or (c):
(A) When the base is a solution type adhesive
A step of uniformly mixing a pressure-sensitive adhesive solution and at least one valuable resource selected from the group consisting of a lipolytic agent, a lipolytic agent and a fat metabolism promoter.
A step of applying the obtained pressure-sensitive adhesive solution on a release sheet and drying the solvent, and a step of laminating the dried pressure-sensitive adhesive layer on the support sheet as needed;
(B) When the base is a hot melt type adhesive
A step of uniformly kneading the tacky composition and at least one valuable material selected from the group consisting of a lipolytic agent, a lipolytic agent and a fat metabolism promoter at a high temperature, and a release of the obtained pressure-sensitive adhesive mixture. The process of applying to a sheet or support sheet;
(C) If the base is a pap base,
Release at least one valuable resource selected from the group consisting of a water-soluble resin, a lipolytic agent, a lipolytic agent and a fat metabolism promoter, a step of uniformly kneading water, and the obtained water-soluble resin composition. The process of applying to a mold sheet or support sheet.

本発明によれば、適用部位の皮下脂肪を容易かつ均一に溶解することができる。
本発明の外用剤の一態様であるテープ型経皮吸収製剤、パッチ型経皮吸収製剤、パップ型経皮吸収製剤等は、脂肪溶解剤を皮下組織に拡散しやすい効果が期待できるものであり、肥満部位の皮下脂肪を分解、燃焼又は溶解し、部分痩せ、眼袋の低減や小顔ラインを作る。また、たるみ部分の皮下脂肪を溶解することによる引き締め効果が期待できる。 According to the present invention, the subcutaneous fat at the application site can be easily and uniformly dissolved.
The tape-type transdermal absorption preparation, patch-type transdermal absorption preparation, pap-type transdermal absorption preparation, etc., which are one aspect of the external preparation of the present invention, can be expected to have the effect of easily diffusing the adipose tissue into the subcutaneous tissue. , Decomposes, burns or dissolves subcutaneous fat in obese areas, partially thins, reduces eye bags and creates small face lines. In addition, a tightening effect can be expected by dissolving the subcutaneous fat in the slack portion.

実施例８のシート状製剤を支持体側から見た底面図Bottom view of the sheet-shaped pharmaceutical product of Example 8 as viewed from the support side. 腹部の皮下脂肪厚の変化を示すグラフGraph showing changes in subcutaneous fat thickness in the abdomen 二の腕の皮下脂肪厚の変化を示すグラフGraph showing changes in subcutaneous fat thickness of the upper arm

本発明の外用剤及び化粧料は、脂肪溶解作用を有する有価物が基剤に溶解分散されてなる組成物であり、本組成物が支持体シートの一面に積層されていることがより好ましい。本発明の外用剤又は化粧料は、脂肪低減又は/及び部分痩せ又は/及び肌引き締めを目的として好適に用いられる。 The external preparation and cosmetics of the present invention are compositions in which valuable resources having a fat-dissolving action are dissolved and dispersed in a base, and it is more preferable that the composition is laminated on one surface of a support sheet. The external preparation or cosmetic of the present invention is suitably used for the purpose of reducing fat and / and partially thinning and / and tightening the skin.

上記支持体シートとしては、特に限定されず、従来からテープ型経皮吸収製剤、パッチ型経皮吸収製剤、パップ型経皮吸収製剤等の支持体シートとして一般に使用されているシートが好ましく、例えば、酢酸セルロース、エチルセルロース、ポリエチレン樹脂、ポリプロピレン樹脂、エチレン－プロピレン共重合体、エチレン－酢酸ビニル共重合体、塩化ビニル系樹脂、塩化ビニリデン樹脂、酢酸ビニル－塩化ビニル共重合体、ポリアミド系樹脂、ポリエステル樹脂、ＡＢＳ樹脂、ＳＩＳ樹脂、ＳＥＢＳ樹脂、ＰＩＢ系樹脂、ウレタン樹脂、シリコーン樹脂、アルミニウム等のシートが挙げられる。又、これらのシートは、上記材料の繊維の織布又は不織布であってもよいし、これらのシート、織布及び不織布の積層シートであってもよい。 The support sheet is not particularly limited, and a sheet generally used as a support sheet for a tape-type transdermal absorption preparation, a patch-type percutaneous absorption preparation, a pap-type percutaneous absorption preparation, or the like is preferable, for example. , Cellulose acetate, ethyl cellulose, polyethylene resin, polypropylene resin, ethylene-propylene copolymer, ethylene-vinyl acetate copolymer, vinyl chloride resin, vinylidene chloride resin, vinyl acetate-vinyl chloride copolymer, polyamide resin, polyester Examples thereof include sheets of resin, ABS resin, SIS resin, SEBS resin, PIB resin, urethane resin, silicone resin, aluminum and the like. Further, these sheets may be woven fabrics or non-woven fabrics of the fibers of the above materials, or may be laminated sheets of these sheets, woven fabrics and non-woven fabrics.

上記基剤は、特に限定されず、従来から経皮吸収製剤の基剤として使用されている基剤が使用可能であり、テープ型経皮吸収製剤やパッチ型経皮吸収製剤の場合は粘着剤であり、テープ型経皮吸収製剤の場合は皮膚に対して粘着性が優れ、糊残りなく剥離できることが必要なので、アクリル系粘着剤及びゴム系粘着剤が好適に使用される。又、パップ型製剤の場合は、一般に水溶性樹脂と水よりなる基剤が使用される。 The above-mentioned base is not particularly limited, and a base conventionally used as a base of a transdermal absorption preparation can be used, and in the case of a tape-type transdermal absorption preparation or a patch-type percutaneous absorption preparation, an adhesive. Therefore, in the case of a tape-type transcutaneous absorption preparation, it is necessary that it has excellent adhesiveness to the skin and can be peeled off without adhesive residue. Therefore, an acrylic pressure-sensitive adhesive and a rubber-based pressure-sensitive adhesive are preferably used. Further, in the case of a pap-type preparation, a base composed of a water-soluble resin and water is generally used.

上記アクリル系粘着剤としては、炭素数４～１８の脂肪族アルコールと（メタ）アクリル酸のエステルである（メタ）アクリル酸アルキルエステルの（共）重合体及び（メタ）アクリル酸アルキルエステルと官能性モノマーとの（共）重合体が好適に使用される。 The acrylic pressure-sensitive adhesive is functional with a (co) polymer of an aliphatic alcohol having 4 to 18 carbon atoms and a (meth) acrylic acid alkyl ester, which is an ester of (meth) acrylic acid, and a (meth) acrylic acid alkyl ester. A (co) polymer with a sex monomer is preferably used.

上記（メタ）アクリル酸アルキルエステルとしては、例えば（メタ）アクリル酸ブチル、（メタ）アクリル酸イソブチル、（メタ）アクリル酸ヘキシル、（メタ）アクリル酸オクチル、（メタ）アクリル酸２－エチルヘキシル、（メタ）アクリル酸イソオクチル、（メタ）アクリル酸デシル、（メタ）アクリル酸イソデシル、（メタ）アクリル酸ラウリル、（メタ）アクリル酸ステアリル等が挙げられる。 Examples of the (meth) acrylic acid alkyl ester include butyl (meth) acrylic acid, isobutyl (meth) acrylic acid, hexyl (meth) acrylic acid, octyl (meth) acrylic acid, 2-ethylhexyl (meth) acrylic acid, and ( Examples thereof include isooctyl acrylate (meth), decyl (meth) acrylate, isodecyl (meth) acrylate, lauryl (meth) acrylate, and stearyl (meth) acrylate.

上記官能性モノマーとしては、例えば、（メタ）アクリル酸２－ヒドロキシエチル、（メタ）アクリル酸ヒドロキシプロピル、（メタ）アクリル酸、マレイン酸、無水マレイン酸、フマル酸、クロトン酸、マレイン酸ブチル、アクリルアミド、ジメチルアクリルアミド、ジエチルアクリルアミド、ブトキシメチルアクリルアミド、エトキシメチルアクリルアミド、メチロール（メタ）アクリルアミド、ジメチルアミノアクリレート、Ｎ－ビニル－２－ピロリドン等が挙げられる。 Examples of the functional monomer include 2-hydroxyethyl (meth) acrylate, hydroxypropyl (meth) acrylate, (meth) acrylic acid, maleic acid, maleic anhydride, fumaric acid, crotonic acid, and butyl maleate. Examples thereof include acrylamide, dimethylacrylamide, diethylacrylamide, butoxymethylacrylamide, ethoxymethylacrylamide, methylol (meth) acrylamide, dimethylaminoacrylate, N-vinyl-2-pyrrolidone and the like.

更に、（メタ）アクリル酸アルキルエステルと共重合可能な重合性モノマーが共重合されてもよく、重合性モノマーとしては、例えば、酢酸ビニル、スチレン、α－メチルスチレン、塩化ビニル、アクリロニトリル、エチレン、プロピレン、ブタジエン等が挙げられる。尚、（共）重合体の（メタ）アクリル酸アルキルエステル成分は５０質量％以上であるのが好ましい。
具体的にはアクリル酸アルキルエステルの共重合体、及びアクリル酸アルキルエステルを主とするアクリル酸、アクリルアミド、酢酸ビニル、等との共重合体である。これらの粘着剤中に皮膚粘着性を改善するためミリスチン酸イソプロピルあるいはパルミチン酸イソプロピルのような可塑剤を添加してもよい。 Further, a polymerizable monomer copolymerizable with the (meth) acrylic acid alkyl ester may be copolymerized, and examples of the polymerizable monomer include vinyl acetate, styrene, α-methylstyrene, vinyl chloride, acrylonitrile, and ethylene. Examples thereof include propylene and butadiene. The (meth) acrylic acid alkyl ester component of the (co) polymer is preferably 50% by mass or more.
Specifically, it is a copolymer of acrylic acid alkyl ester, and a copolymer of acrylic acid, acrylamide, vinyl acetate, etc. mainly containing acrylic acid alkyl ester. A plasticizer such as isopropyl myristate or isopropyl palmitate may be added to these adhesives to improve skin adhesion.

粘着層（膏体）の厚さは５μｍ～２００μｍが望ましく、１０μｍ～２００μｍがより望ましい。粘着層（膏体）の厚さは５μ～１００μｍであることも望ましい。具体的には、HiPAS（登録商標）粘着剤（アクリルエステル、コスメディ製薬（株）製）、MASCOS１０（商品名）粘着剤（アクリルエステル、コスメディ製薬（株）製）、が好適に使用できる。 The thickness of the adhesive layer (plaster) is preferably 5 μm to 200 μm, more preferably 10 μm to 200 μm. It is also desirable that the thickness of the adhesive layer (plaster) is 5 μm to 100 μm. Specifically, HiPAS (registered trademark) adhesive (acrylic ester, manufactured by Cosmed Pharmaceutical Co., Ltd.) and MASCOS10 (trade name) adhesive (acrylic ester, manufactured by Cosmed Pharmaceutical Co., Ltd.) can be preferably used. ..

更に、アクリル系共重合体は金属キレート化合物で後架橋されているのが好ましい。適度の凝集力と粘着性を得るためには、金属キレート化合物をアクリル系共重合体１００質量部に対し０．０５～２．０質量部添加するのが好ましい。 Further, the acrylic copolymer is preferably post-crosslinked with a metal chelate compound. In order to obtain appropriate cohesive force and adhesiveness, it is preferable to add 0.05 to 2.0 parts by mass of the metal chelate compound with respect to 100 parts by mass of the acrylic copolymer.

上記金属キレート化合物としては、例えば、アルミニウムアセチルアセトネート、アルミニウムグリシネート、水酸化アルミニウムゲル等が挙げられ、これらは単独で用いられても併用されてもよい。 Examples of the metal chelate compound include aluminum acetylacetonate, aluminum glycinate, and aluminum hydroxide gel, which may be used alone or in combination.

上記ゴム系粘着剤としては、天然ゴム、ポリイシプレン、ポリイソブチレン、ポリブタジエン、スチレン－ブタジエン共重合体、スチレン－ブタジエン－スチレン共重合体、スチレン－イソプレン共重合体、スチレン－イソプレン－スチレン共重合体、ウレタンゴム等のゴムを主体とする従来公知のゴム系粘着剤が使用できる。 Examples of the rubber-based pressure-sensitive adhesive include natural rubber, polyisiprene, polyisobutylene, polybutadiene, styrene-butadiene copolymer, styrene-butadiene-styrene copolymer, styrene-isoprene copolymer, and styrene-isoprene-styrene copolymer. Conventionally known rubber-based adhesives mainly composed of rubber such as urethane rubber can be used.

上記ゴム系粘着剤は、必要に応じて、ロジン系樹脂、ポリテルペン系樹脂、クマロン－インデン系樹脂、石油系樹脂、テルペン－フェノール系樹脂、脂環式炭化水素などの粘着付与剤を含有していてもよい。粘着付与剤の含有量は、特に限定されるものではないが、一般にゴム系粘着剤と粘着付与剤の合計量の２０～８０質量％である。
上記ゴム系粘着剤には、更に、流動パラフィン、液状ポリブテン、液状ポリイソプレン、鉱油ラノリン、液状ポリアクリレート、スクワラン、オリーブ油などの可塑剤、充填剤、老化防止剤等が添加されていてもよい。 The rubber-based pressure-sensitive adhesive contains a tackifier such as a rosin-based resin, a polyterpene-based resin, a kumaron-inden-based resin, a petroleum-based resin, a terpene-phenol-based resin, and an alicyclic hydrocarbon, if necessary. You may. The content of the tackifier is not particularly limited, but is generally 20 to 80% by mass of the total amount of the rubber-based pressure-sensitive adhesive and the tackifier.
Further, a plasticizer such as liquid paraffin, liquid polybutene, liquid polyisoprene, mineral oil lanolin, liquid polyacrylate, squalane, olive oil, a filler, an antiaging agent and the like may be added to the rubber-based pressure-sensitive adhesive.

上記水溶性樹脂としては、例えば、アラビアガム、トラガンガム、ローカストビーンガム、グアーガム、エコーガム、カラヤガム、寒天、でんぷん、カラゲナン、アルギン酸、アルギン酸塩、アルギン酸プロピレングリコール、デキストラン、デキストリン、アミロース、ゼラチン、コラーゲン、プルラン、ペクチン、アミロペクチン、アミロペクチンセミグリコール酸ナトリウム、キチン、アルブミン、カゼイン、ポリグルタミン酸などの天然ポリマー、メチルセルロース、エチルセルロース、プロピルセルロース、エチルメチルセルロース、ヒドロキシセルロース、ヒドロキシエチルセルロース、ヒドロキシプロピルメチルセルロース、ヒドロキシプロピルスターチ、カルボキメチルシスターチ、アルカリ金属カルボキシメチルセルロース、アルカリ金属セルロース硫酸塩、セルロースアセテートフタレート、デンプン－アクリル酸グラフト共重合体、架橋ゼラチン、無水フタル酸変性ゼラチン、コハク酸変性ゼラチンなどの半合成ポリマー、ポリビニルアルコール、ポリビニルピロリドン、ポリビニルメチルエーテル、メチルビニルエステル、ポリアクリル酸塩（例えば、ポリアクリル酸ナトリウム）、カルボキシビニルポリマー、ビニルピロリドン－アクリル酸エチル共重合体、ビニルピロリドンースチレン共重合体、ビニルピロリドン－酢酸ビニル共重合体、酢酸ビニル－（メタ）アクリル酸共重合体、酢酸ビニルークロトン酸共重合体、ポリビニルスルホン酸、ポリイタコン酸、ポリヒドロキシエチルアクリレート、ポリアクリルアミド、スチレン－マレイン酸無水物共重合体、エチレン－マレイン酸無水物共重合体、アクリルアミド－アクリル酸共重合体などの合成ポリマーが挙げられる。 Examples of the water-soluble resin include Arabic gum, tragan gum, locust bean gum, guar gum, echo gum, karaya gum, agar, starch, carrageenan, alginic acid, alginate, propylene glycol alginate, dextran, dextrin, amylose, gelatin, collagen, and purulan. , Pectin, amyropectin, amyropectin sodium semiglycolate, chitin, albumin, casein, polyglutamic acid and other natural polymers, methylcellulose, ethylcellulose, propylcellulose, ethylmethylcellulose, hydroxycellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, hydroxypropylstarch, carbokimethyl Semi-synthetic polymers such as sisterch, alkali metal carboxymethyl cellulose, alkali metal cellulose sulfate, cellulose acetate phthalate, starch-acrylic acid graft copolymer, cross-linked gelatin, phthalic acid-modified gelatin anhydride, succinic acid-modified gelatin, polyvinyl alcohol, polyvinyl Pyrrolidone, polyvinyl methyl ether, methyl vinyl ester, polyacrylate (eg, sodium polyacrylic acid), carboxyvinyl polymer, vinyl pyrrolidone-ethyl acrylate copolymer, vinyl pyrrolidone-styrene copolymer, vinyl pyrrolidone-vinyl acetate Polymers, vinyl acetate- (meth) acrylic acid copolymers, vinyl acetate-crotonic acid copolymers, polyvinyl sulfonic acid, polyitaconic acid, polyhydroxyethyl acrylates, polyacrylamides, styrene-maleic acid anhydride copolymers, Examples thereof include synthetic polymers such as an ethylene-maleic acid anhydride copolymer and an acrylamide-acrylic acid copolymer.

パップ型製剤に含まれる水の量は、水の含有量が少ないと薬物の吸収が遅くなり、パップ型製剤を皮膚に貼付した際に水の蒸発による冷感効果が低下する傾向があり、逆に多くなると、水溶性ポリマーの流動性が大きくなり、製剤の形状を保持するのが困難になる傾向があるので、一般に１～９０質量％であり、好ましくは５～８５質量％である。 As for the amount of water contained in the pap-type preparation, if the water content is low, the absorption of the drug is delayed, and when the pap-type preparation is applied to the skin, the cooling effect due to the evaporation of water tends to decrease, and vice versa. When the amount is too large, the fluidity of the water-soluble polymer tends to increase, and it tends to be difficult to maintain the shape of the pharmaceutical product. Therefore, it is generally 1 to 90% by mass, preferably 5 to 85% by mass.

上記パップ型製剤には、必要に応じて、アクリル系樹脂、ゴム、シリコーン系樹脂などの樹脂、多価アルコール（例えば、グリセリン、ポリプロピレングリコール）などの保湿剤、カオリン、ベントナイト、亜鉛華、二酸化チタンなどの無機充填剤、粘度調節剤、老化防止剤等が添加されてもよい。 The above-mentioned pap-type preparations include, if necessary, resins such as acrylic resins, rubbers and silicone resins, moisturizers such as polyhydric alcohols (eg, glycerin and polypropylene glycol), kaolin, bentonite, zinc flower and titanium dioxide. Inorganic fillers such as, viscosity modifiers, antiaging agents and the like may be added.

上記基剤には経皮吸収促進剤が添加されてもよい。経皮吸収促進剤としては、例えば、メンソール、カンフル、セチルアルコール等のアルコール類；パルミチン酸イソプロピル、ミリスチン酸イソプロピル等の脂肪酸エステル；モノラウリン酸グリセリン、モノオレイン酸グリセリン、モノカプリン酸グリセリン等のグリセリンエステル；ラウリン酸ジエタノールアミド等の酸アミド；ポリエチレングリコールジラウリルエーテル、ドデシル硫酸ナトリウム等の中性界面活性剤などが挙げられる。
経皮吸収促進剤の添加量は、少なすぎると経皮吸収効果が向上せず、多すぎると粘着性が低下するので、基剤１００質量部に対して３～４０質量部が好ましい。 A transdermal absorption promoter may be added to the base. Examples of the transdermal absorption promoter include alcohols such as menthol, camphor and cetyl alcohol; fatty acid esters such as isopropyl palmitate and isopropyl myristate; glycerin esters such as glycerin monolaurate, glycerin monooleate and glycerin monocaprate. Acid amides such as lauric acid diethanolamide; neutral surfactants such as polyethylene glycol dilauryl ether and sodium dodecyl sulfate can be mentioned.
If the amount of the percutaneous absorption accelerator added is too small, the percutaneous absorption effect is not improved, and if it is too large, the adhesiveness is lowered. Therefore, 3 to 40 parts by mass is preferable with respect to 100 parts by mass of the base.

本発明の外用剤又は化粧料は、有価物として、脂肪分解剤、脂肪溶解剤又は脂肪代謝促進剤のいずれか１種以上を含有する。有価物は、脂肪減少に働く成分であり、製剤中に０．１質量％以上含まれる。有価物の含有量は、皮下脂肪の分解、溶解又は代謝促進のためには、０．１～５０質量％が好ましく、０．２～３０質量％がより好ましい。さらに平方ｃｍ当たりの有価成分の量は１μｇ～１００ｍｇが好ましい。
本発明の外用剤又は化粧料には脂肪分解・溶解、脂肪代謝促進作用を有する有価物に加えて、脂肪燃焼の促進成分、脂肪細胞からの脂肪分解排出を促す成分、肌引き締め成分などを併用することにより脂肪分解・溶解効果を高めることができる。 The external preparation or cosmetic of the present invention contains at least one of a lipolytic agent, a fat dissolving agent and a fat metabolism promoting agent as a valuable resource. Valuables are components that act to reduce fat and are contained in the pharmaceutical product in an amount of 0.1% by mass or more. The content of valuables is preferably 0.1 to 50% by mass, more preferably 0.2 to 30% by mass, for the purpose of decomposing, dissolving or promoting metabolism of subcutaneous fat. Further, the amount of the valuable component per square cm is preferably 1 μg to 100 mg.
In addition to valuable resources having lipolysis / dissolution and lipolysis promoting effects, the external preparation or cosmetic of the present invention is used in combination with a component that promotes fat burning, a component that promotes lipolysis and excretion from adipocytes, a skin tightening component, and the like. By doing so, the lipolysis / dissolving effect can be enhanced.

脂肪分解剤としては、リパーゼのような脂肪分解酵素、グルカゴン、アドレナリン、ノルアドレナリン、グレリン、成長ホルモン、テストステロン、コルチゾール、のようなホルモンがある。またケア部位および目的に合わせて、タンパク質分解酵素としてプロテアーゼ、コラーゲン分解酵素としてコラゲナーゼ、ヒアルロン酸分解酵素としてヒアルロニダーゼ、さらに野菜・果物・海藻より発酵抽出した酵素発酵植物エキス等を併用することも有効である。
脂肪分解剤はリパーゼが好ましい。リパーゼを用いる場合、リパーゼの安定化剤を共存させてもよい。例えば、グリセロール、グリシン、メルカプトエタノール、トリトンＸ－１００、トリトンＮ－１０１、デオキシコール酸又はその塩、Ｍｇ２＋イオン、Ｃａ２＋イオン、ＢＳＡ、塩類などが挙げられる。Ｍｇ２＋イオン及びＣａ２＋イオンは塩として共存していてもよい。 Lipolytic agents include lipolytic enzymes such as lipase, hormones such as glucagon, adrenaline, noradrenaline, ghrelin, growth hormone, testosterone, cortisol, and the like. It is also effective to use protease as a proteolytic enzyme, collagenase as a collagen degrading enzyme, hyaluronidase as a hyaluronidase degrading enzyme, and an enzyme fermented plant extract fermented and extracted from vegetables, fruits and seaweed according to the care site and purpose. be.
Lipase is the preferred lipolytic agent. When lipase is used, a lipase stabilizer may coexist. For example, glycerol, glycine, mercaptoethanol, triton X-100, triton N-101, deoxycholic acid or a salt thereof, Mg 2+ ion, Ca 2+ ion, BSA, salts and the like can be mentioned. Mg 2+ ions and Ca 2+ ions may coexist as salts.

脂肪溶解剤としては、ホスファチジルコリン、ヒバマタ抽出物、チロシン、アデノシン三リン酸及びそのナトリウム塩、セイヨウトチノキ、ペルシャグルミ、メチルプロパンジオール、マンヌロン酸メチルシラノール、オキナグサ、カラクサケマン、デオキシコール酸又はその塩、ケノデオキシコール酸、等があげられる。さらにキサンチン誘導体(カフェイン、テオフィリン、テオブロミン、キサンチン、アミノフィリン、コリンテオフィリン、ジプロフィリン、プロキシフィリン及びオクストリフィリン等)、アオツヅラフジ(木防巳)エキス、アザミエキス、オオツヅラフジ(防己)エキス、ガジュツ(莪朮)エキス、カラクサケマンエキス、キキョウ(桔梗、桔梗根)エキス、キヅタエキス、コショウ(胡椒)エキス、サラシナヨウマ根エキス、ツポクサエキス、グチナシ果実エキス、フマリア・オィキナスエキス、イチゴ葉エキス、等が挙げられる。
脂肪溶解剤は、ホスファチジルコリン、アデノシン三リン酸及びそのナトリウム塩ならびにデオキシコール酸又はその塩からなる群より選ばれる１種以上が好ましい。
また、ホスファチジルコリンの安定化剤としてはアスタキサンチン、酢酸トコフェロール、トコフェロール、パルミチン酸アスコルビル、ジエタノールアミンなどが好ましい。デオキシコール酸の塩を添加する場合、皮膚内への浸透を促進するために酸性物質、例えば、クエン酸、乳酸、オレイン酸、酒石酸、等を共存させることが望ましい。 Examples of the fat dissolving agent include phosphatidylcholine, hibamata extract, tyrosine, adenosine triphosphate and its sodium salt, horse chestnut, persian glumi, methylpropanediol, methylsilanol mannuronate, okinagusa, fumitory man, deoxycholic acid or its salt, and chenodeoxycholic acid. Acid, etc. can be mentioned. Furthermore, xanthin derivatives (caffeine, theophylline, theobromine, xanthin, aminophyllin, cholineteophylline, diprophylline, proxiphyllin, oxtriphyllin, etc.), Aotsuzurafuji (Kibomi) extract, Azami extract, Otsuzurafuji (self-defense) extract, Gajutsu (莪朮) ) Extract, Karakusakeman extract, Kyoko (kikyo, Kikyo root) extract, Kizuta extract, pepper (kosho) extract, Sarashinayouma root extract, Tupokusa extract, Guchinashi fruit extract, Fumaria okinus extract, strawberry leaf extract, and the like.
The fat-dissolving agent is preferably one or more selected from the group consisting of phosphatidylcholine, adenosine triphosphate and sodium salts thereof, and deoxycholic acid or salts thereof.
Further, as the stabilizer of phosphatidylcholine, astaxanthin, tocopherol acetate, tocopherol, ascorbyl palmitate, diethanolamine and the like are preferable. When a salt of deoxycholic acid is added, it is desirable to coexist with an acidic substance such as citric acid, lactic acid, oleic acid, tartaric acid, etc. in order to promote penetration into the skin.

脂肪代謝促進剤として、チロシン、セリン、トレオニン、フェニルアラニン、トリプトファン、イソロイシン、リジン、アルギニン、ベタイン、ヒスチジン、グルタミン、グリシン、システイン、などのアミノ酸、脂肪燃焼の促進成分として、Ｌ－カルニチン、イノシトール、カプサイシン、カフェイン、コエンザイムＱ１０、カテキン、等が挙げられる。
脂肪代謝促進剤は、アミノ酸、Ｌ－カルニチン、イノシトール、カプサイシン及びカフェインからなる群より選ばれる１種以上が好ましく、アミノ酸も上記の中から１種以上用いることが好ましい。 Amino acids such as tyrosine, serine, threonine, phenylalanine, tryptophan, isoleucine, lysine, arginine, betaine, histidine, glutamine, glycine, and cysteine as fat metabolism promoters, and L-carnitine, inositol, and capsaicin as fat burning promoters. , Caffeine, coenzyme Q10, catechin, etc.
The fat metabolism promoter is preferably one or more selected from the group consisting of amino acids, L-carnitine, inositol, capsaicin and caffeine, and it is preferable to use one or more amino acids from the above.

上記の有価物と基剤は本発明における必須成分であるが、その他の皮膚有価物の添加が限定されるものではない。例えば、色素沈着抑制剤、保湿剤、代謝活性化剤、抗酸化剤、活性酸素消去剤・ラジカル消去剤、等が挙げられる。 The above valuables and bases are essential ingredients in the present invention, but the addition of other skin valuables is not limited. For example, a pigmentation inhibitor, a moisturizer, a metabolism activator, an antioxidant, an active oxygen scavenger / radical scavenger, and the like can be mentioned.

色素沈着抑制剤
本発明には色素沈着抑制剤を添加することができる。色素沈着抑制剤の具体例として、p-アミノ安息香酸誘導体、サルチル酸誘導体、ベンゼンスルホンアミド誘導体、イミダゾール誘導体、ナフタレン誘導体、ヒドロキシアントラニル酸又はその塩並びにそれらの誘導体、アントラニル酸誘導体、クマリン誘導体、アラントイン誘導体、ニコチン酸誘導体、アスコルビン酸又はその塩並びにそれらの誘導体、トコフェロール又はその塩並びにそれらの誘導体、トコトリエノール又はその塩並びにそれらの誘導体、コウジ酸又はその誘導体、オキシベンゾン、ベンゾフェノン、グアイアズレン、シコニン、バイカリン又はその塩並びにそれらの誘導体、バイカレイン又はその塩並びにそれらの誘導体、ベルベリン又はその塩並びにそれらの誘導体、アピゲニン又はその塩並びにそれらの誘導体、ルテオリン又はその塩並びにそれらの誘導体、ケンフェロール又はその塩並びにそれらの誘導体、クエルセチン又はその塩並びにそれらの誘導体、クエルシトリン又はその塩並びにそれらの誘導体、イソクエルシトリン又はその塩並びにそれらの誘導体、ルチン又はその塩並びにそれらの誘導体、ミリセチン又はその塩並びにそれらの誘導体、ナリンゲニン又はその塩並びにそれらの誘導体、ヘスペリジン又はその塩並びにそれらの誘導体、グルタチオン又はその塩並びにそれらの誘導体、エラグ酸又はその塩並びにそれらの誘導体、等が挙げられる。 Pigmentation inhibitor A pigmentation inhibitor can be added to the present invention. Specific examples of the pigmentation inhibitor include p-aminobenzoic acid derivative, sulcylic acid derivative, benzenesulfonamide derivative, imidazole derivative, naphthalene derivative, hydroxyanthranic acid or a salt thereof, and their derivatives, anthranic acid derivative, coumarin derivative, and allantin. Derivatives, nicotinic acid derivatives, ascorbic acid or salts thereof and derivatives thereof, tocopherols or salts thereof and derivatives thereof, tocotrienol or salts thereof and derivatives thereof, kodiic acid or derivatives thereof, oxybenzone, benzophenone, guaiazulene, ciconin, bicarin or Its salts and their derivatives, baicalene or its salts and their derivatives, velverin or its salts and their derivatives, apigenin or its salts and their derivatives, luteolin or its salts and their derivatives, kenferol or its salts and theirs. Derivatives of quercetin or salts thereof and derivatives thereof, quercitrin or salts thereof and derivatives thereof, isoquercitrin or salts thereof and derivatives thereof, rutin or salts thereof and derivatives thereof, mylicetin or salts thereof and derivatives thereof. , Naringenin or salts thereof and derivatives thereof, hesperidin or salts thereof and derivatives thereof, glutathione or salts thereof and derivatives thereof, ellagic acid or salts thereof and derivatives thereof, and the like.

保湿剤
本発明には保湿剤を添加することができる。保湿剤の具体例として、クインスシード、寒天またはその誘導体、カゼイン、グルコース、ガラクトース、マンノース、キシロース、フルクトース、マルトース、イソマルトース、セロビオース、ゲンチオビオース、トレハロース、ピラロース、1,3-ブチレングリコール、グリセリン、プロピレングリコール、ポリエチレングリコール、ジプロピレングリコール、1,2-ペンタンジオール、1,5-ペンタンジオール、1,2-ヘキサンジオール、1,6-ヘキサンジオール、マンニトール及びソルビトール、1,2-プロパンジオール、1,3-プロパンジオール、ポリプロピレングリコール、1,2-ブタンジオール、1,3-ブタンジオール、1,4-ブタンジオール、ペンチレングリコール、ヘキシレングリコール、1,3-ペンタンジオール、1,4-ペンタンジオール、エリスリトール、ペンタエリスリトール、ジペンタエリスリトール、キシリトール、マルチトール、イノシトール、パンテノール又はその誘導体、デキストリン、ゼラチン、ペクチン、デンプン、カラギーナン、カルボキシメチルキチン又はキトサン、キトサン塩、硫酸化キチン又はキトサン、リン酸化キチン又はキトサン、アルギン酸又はその塩、ヒアルロン酸又はその塩、コンドロイチン硫酸又はその塩、β-1,3-グルカン、β-1,4-グルカン、β-1,6-グルカン、グルコサミン、ヘパリン、エチルセルロース、メチルセルロース、カルボキシメチルセルロース、カルボキシエチルセルロース、カルボキシエチルセルロースナトリウム、ヒドロキシエチルセルロース、ヒドロキシプロピルセルロース、ニトロセルロース、結晶セルロース、ヒドロキシプロピルメチルセルロース、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、ポリアクリル酸塩、カルボキシビニルポリマー、デルマタン硫酸、ケラタン硫酸等の水溶性高分子類、ピロリドンカルボン酸又はその塩、ポリグルタミン酸又はその塩、天然保湿因子に含有されるピロリドンカルボン酸、尿素、ウロカニン酸、ベタイン、乳酸ナトリウム、アスパラギン酸、グルタミン酸、イソロイシン、ヒスチジン、フェニルアラニン、トレオニン、セリン、バリン、プロリン、グリシン、アラニン、リシン、アルギニン、セラミド１、セラミド２、セラミド３、セラミド４、セラミド５、セラミド６II、セラミド９などのセラミド類、等が挙げられる。 Moisturizer A moisturizer can be added to the present invention. Specific examples of moisturizers include quince seeds, agar or derivatives thereof, casein, glucose, galactose, mannose, xylose, fructose, maltose, isomartose, cellobiose, gentiobiose, trehalose, pyralose, 1,3-butylene glycol, glycerin, propylene. Glycol, polyethylene glycol, dipropylene glycol, 1,2-pentanediol, 1,5-pentanediol, 1,2-hexanediol, 1,6-hexanediol, mannitol and sorbitol, 1,2-propanediol, 1, 3-Propanediol, Polypropylene Glycol, 1,2-Butanediol, 1,3-Butanediol, 1,4-Butanediol, Pentylene Glycol, Hexylene Glycol, 1,3-Pentanediol, 1,4-Pentanediol , Erythritol, pentaerythritol, dipentaerythritol, xylitol, martitol, inositol, pantenol or derivatives thereof, dextrin, gelatin, pectin, starch, carrageenan, carboxymethyl chitin or chitosan, chitosan salt, sulfated chitin or chitosan, phosphorylation. Chitin or chitosan, alginic acid or its salt, hyaluronic acid or its salt, chondroitin sulfate or its salt, β-1,3-glucan, β-1,4-glucan, β-1,6-glucan, glucosamine, heparin, ethylcellulose , Methyl cellulose, carboxymethyl cellulose, carboxyethyl cellulose, sodium carboxyethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, nitrocellulose, crystalline cellulose, hydroxypropylmethylcellulose, polyvinyl alcohol, polyvinylmethyl ether, polyvinylpyrrolidone, polyacrylic acid salt, carboxyvinyl polymer, dermatane Water-soluble polymers such as sulfuric acid and keratane sulfate, pyrrolidone carboxylic acid or a salt thereof, polyglutamic acid or a salt thereof, pyrrolidone carboxylic acid contained in a natural moisturizing factor, urea, urocanic acid, betaine, sodium lactate, aspartic acid, glutamate. , Isoleucine, histidine, phenylalanine, threonine, serine, valine, proline, glycine, alanine, lysine, arginine, ceramide 1, ceramide 2, ceramide 3, ceramide 4, ceramide 5, ceramide 6II, ceramides such as ceramide 9, etc. Can be mentioned.

代謝活性化剤
本発明には代謝活性化剤を添加することができる。代謝活性化剤の具体例として、ビタミンＡ群：レチノール又はその塩並びにそれらの誘導体、レチナール又はその塩並びにそれらの誘導体、デヒドロレチナール又はその塩並びにそれらの誘導体、レチノイン酸又はその塩並びにそれらの誘導体、カロチン又はその塩並びにそれらの誘導体、リコピン又はその塩並びにそれらの誘導体、
ビタミンＢ群：チアミン又はその塩並びにそれらの誘導体、リボフラビン又はその塩並びにそれらの誘導体、ピリドキシン又はその塩並びにそれらの誘導体、ピリドキサール又はその塩並びにそれらの誘導体、シアノコバラミン又はその塩並びにそれらの誘導体、葉酸又はその塩並びにそれらの誘導体、ニコチン酸又はその塩並びにそれらの誘導体、パントテン酸又はその塩並びにそれらの誘導体、ビオチン又はその塩並びにそれらの誘導体、コリン又はその塩並びにそれらの誘導体、イノシトール又はその塩並びにそれらの誘導体、
ビタミンＣ群：アスコルビン酸又はその塩並びにそれらの誘導体、
ビタミンＤ群：エルゴカルシフェロール又はその塩並びにそれらの誘導体、コレカルシフェロール及びその塩並びにそれらの誘導体、
ビタミンＥ群等：トコフェロール又はその塩並びにそれらの誘導体、トコトリエノール又はその塩並びにそれらの誘導体、ユビキノン又はその塩並びにそれらの誘導体、リノール酸又はその塩並びにそれらの誘導体、リノレン酸又はその塩並びにそれらの誘導体、アラキドン酸又はその塩並びにそれらの誘導体等、カルニチン又はその塩並びにそれらの誘導体、フェルラ酸又はその塩並びにそれらの誘導体、γ-オリザノール又はその塩並びにそれらの誘導体、
ビタミンＰ群：ルチン又はその塩並びにそれらの誘導体、ヘスペリジン又はその塩並びにそれらの誘導体、アミノ酸類その他：バリン、ロイシン、イソロイシン、トレオニン、メチオニン、フェニルアラニン、トリプトファン、リジン、グリシン、アラニン、アスパラギン、グルタミン、セリン、システイン、シスチン、チロシン、プロリン、ヒドロキシプロリン、アスパラギン酸、グルタミン酸、ヒドロキシリジン、アルギニン、オルニチン、ヒスチジン又はその誘導体等や、それらの硫酸塩、リン酸塩、硝酸塩、クエン酸塩、あるいはピロリドンカルボン酸等のアミノ酸誘導体等のアミノ酸類、グリコール酸、クエン酸、リンゴ酸、酒石酸、乳酸、コハク酸等のα-ヒドロキシ酸類、2-ヒドロキシカルボン酸類、ポリヒドロキシカルボン酸又はヒドロキシポリカルボン酸類、ラクトビオン酸、感光素３０１号、ヒノキチオール、パントテン酸又はその誘導体、アラントイン、トリメチルグリシン、プロテオグリカン、等が挙げられる。 Metabolite Activator A metabolism activator can be added to the present invention. Specific examples of the metabolic activator include vitamin A group: retinol or a salt thereof and a derivative thereof, retinal or a salt thereof and a derivative thereof, dehydroretinal or a salt thereof and a derivative thereof, retinoic acid or a salt thereof and a derivative thereof. , Carotene or its salts and their derivatives, lycopene or its salts and their derivatives,
B vitamins: thiamine or a salt thereof and a derivative thereof, riboflavin or a salt thereof and a derivative thereof, pyridoxine or a salt thereof and a derivative thereof, pyridoxal or a salt thereof and a derivative thereof, cyanocobalamine or a salt thereof and a derivative thereof, folic acid. Or salts thereof and derivatives thereof, nicotinic acid or salts thereof and derivatives thereof, pantothenic acid or salts thereof and derivatives thereof, biotin or salts thereof and derivatives thereof, choline or salts thereof and derivatives thereof, inositol or salts thereof. And their derivatives,
Vitamin C group: ascorbic acid or its salts and their derivatives,
Vitamin D group: ergocalciferol or its salt and its derivatives, choleciferol and its salts and their derivatives,
Vitamin E group, etc .: tocopherol or a salt thereof and a derivative thereof, tocotrienol or a salt thereof and a derivative thereof, ubiquinone or a salt thereof and a derivative thereof, linoleic acid or a salt thereof and a derivative thereof, linolenic acid or a salt thereof and their salts. Derivatives, arachidonic acid or salts thereof and derivatives thereof, carnitine or salts thereof and derivatives thereof, ferulic acid or salts thereof and derivatives thereof, γ-orizanol or salts thereof and derivatives thereof,
Vitamin P group: rutin or its salt and its derivatives, hesperidin or its salts and their derivatives, amino acids, etc .: valine, leucine, isoleucine, treonine, methionine, phenylalanine, tryptophan, lysine, glycine, alanine, asparagine, glutamine, Serine, cysteine, cystine, tyrosine, proline, hydroxyproline, aspartic acid, glutamic acid, hydroxylysine, arginine, ornithine, histidine or derivatives thereof, and their sulfates, phosphates, nitrates, citrates, or pyrrolidone carboxylics. Amino acids such as amino acid derivatives such as acids, α-hydroxy acids such as glycolic acid, citric acid, malic acid, tartaric acid, lactic acid and succinic acid, 2-hydroxycarboxylic acids, polyhydroxycarboxylic acids or hydroxypolycarboxylic acids, lactobionic acid. , Photosensitizer No. 301, hinokithiol, pantothenic acid or a derivative thereof, allantin, trimethylglycine, proteoglycan, and the like.

抗酸化剤
本発明には抗酸化剤を添加することができる。抗酸化剤の具体例として、アスコルビン酸又はその塩並びにそれらの誘導体、トコフェロール又はその塩並びにそれらの誘導体、トコトリエノール又はその塩並びにそれらの誘導体、ブチルヒドロキシトルエン(BHT)、ブチルヒドロキシアニソール(BHA)、コエンザイムＱn(n＝7～10)、ピロロキノリンキノン、没食子酸プロピル、セサモール、カロテノイド類等が挙げられる。ホスファチジルコリンは酸化されやすいため、アスタキサンチン、酢酸トコフェロール、トコフェロール、パルミチン酸アスコルビルなどの抗酸化剤を共存させることが望ましい。その添加量は、ホスファチジルコリン１質量部に対し０.００１質量部以上が好ましい。さらにジエタノールアミン、塩化アンモニウム、アンモニア等を共存させると、より安定性を向上させる。その添加量は、０．００１質量部以上が好ましい。 Antioxidants Antioxidants can be added to the present invention. Specific examples of antioxidants include ascorbic acid or a salt thereof and a derivative thereof, tocopherol or a salt thereof and a derivative thereof, tocotrienol or a salt thereof and a derivative thereof, butylated hydroxytoluene (BHT), butylated hydroxyanisole (BHA), and the like. Examples thereof include coenzyme Qn (n = 7 to 10), pyroquinolinquinone, propyl ascorbic acid, sesamol, carotenoids and the like. Since phosphatidylcholine is easily oxidized, it is desirable to coexist with an antioxidant such as astaxanthin, tocopherol acetate, tocopherol, and ascorbyl palmitate. The amount added is preferably 0.001 part by mass or more with respect to 1 part by mass of phosphatidylcholine. Further, when diethanolamine, ammonium chloride, ammonia and the like coexist, the stability is further improved. The addition amount is preferably 0.001 part by mass or more.

活性酸素消去剤・ラジカル消去剤
本発明には活性酸素消去剤・ラジカル消去剤を添加することができる。活性酸素消去剤・ラジカル消去剤の具体例として、スーパーオキシドディスムターゼ、カタラーゼ、グルタチオンペルオキシダーゼ、ビリルビン、クエルセチン、クエルシトリン、カテキン、カテキン誘導体、ルチン又はその誘導体、没食子酸又はその塩並びにそれらの誘導体、クルクミン又はその塩並びにそれらの誘導体、トランスフェリン、セルロプラスミン、コエンザイムＱn(n＝7～10)、尿酸、ビリルビン、メタロチオネイン、等が挙げられる。 Active oxygen scavenger / radical scavenger An active oxygen scavenger / radical scavenger can be added to the present invention. Specific examples of active oxygen scavengers / radical scavengers include superoxide dismutase, catalase, glutathione peroxidase, birylbin, quercetin, quercitrin, catechin, catechin derivatives, rutin or derivatives thereof, gallic acid or salts thereof, and derivatives thereof, curcumin. Alternatively, salts thereof and derivatives thereof, transferase, celluloplasmin, coenzyme Qn (n = 7 to 10), uric acid, gallic acid, metallothioneine, and the like can be mentioned.

本発明には上記した構成成分の他に、通常化粧品や医薬品等の皮膚外用剤に用いられる成分を添加しても良い。水性成分、油性成分、植物抽出物、動物抽出物、粉末、界面活性剤、油剤、アルコール、ｐＨ調整剤、防腐剤、増粘剤、色素、香料等からなる1以上の成分からなり、これらは基剤の一部でありかつその皮膚への効果（例えば、肌引き締め作用）により有価物としても働くことも有りうる。 In addition to the above-mentioned constituent components, components usually used for external skin preparations such as cosmetics and pharmaceuticals may be added to the present invention. It consists of one or more components consisting of aqueous components, oily components, plant extracts, animal extracts, powders, surfactants, oils, alcohols, pH regulators, preservatives, thickeners, pigments, fragrances, etc. It may also act as a valuable resource due to its effect on the skin (eg, skin tightening action) as a part of the base.

本発明の外用剤又は化粧料は、貼付シートであってもよい。
貼付シートである外用剤及び化粧料がパッチ剤の場合、パッチの大きさは０.５～３００平方ｃｍである。０.５平方ｃｍ未満であっては効果が限定され有効性が発揮しにくい。３００平方ｃｍを超えると、体表面を覆うには密着性に問題が生じやすい。広い体表面を覆うには３００平方ｃｍ以下のパッチを複数個用いればよい。テープ剤及びパップ剤もパッチ剤と同様の大きさである。
別途、貼付シートをロール状シートとし、使用部位に合わせてカットして適当なサイズとし使用しても良い。その場合、シート幅は１ｃｍ以上３０ｃｍ以内で携帯可能なサイズでよい。 The external preparation or cosmetic of the present invention may be a sticking sheet.
When the external preparation and the cosmetic used as the patch sheet are patch agents, the size of the patch is 0.5 to 300 square cm. If it is less than 0.5 square cm, the effect is limited and the effectiveness is difficult to be exhibited. If it exceeds 300 square cm, there is a tendency for problems in adhesion to cover the body surface. To cover a wide body surface, a plurality of patches of 300 square cm or less may be used. The tape agent and the poultice agent have the same size as the patch agent.
Separately, the pasted sheet may be made into a roll-shaped sheet, cut according to the part to be used, and used in an appropriate size. In that case, the seat width may be 1 cm or more and 30 cm or less and a portable size.

貼付シートである外用剤及び化粧料を皮膚に安定して適用し皮膚に保持するためには、粘着性基剤の背面に支持体シートがあることが、必須ではないが、より好ましい。
支持体シートは、柔軟性を考慮し、不織布、編み布、織布、ポリウレタンフィルム、ポリウレタンフォーム、ポリエチレンフィルム、ＰＰ（ポリプロピレン）、ＥＶＡ（エチレンビニルアセテート）などが適当である。フィルムにおいては、３～７０μｍの厚みが適当である。特に厚みが３～５０μｍのポリウレタンフィルムが好ましい。皮膚蒸れなく長時間貼付可能な厚みが５～１５μｍのポリウレタンフィルムが支持体シートとしてはより好ましい。 In order to stably apply the external preparation and cosmetics, which are adhesive sheets, to the skin and hold them on the skin, it is not essential, but more preferable, to have a support sheet on the back surface of the adhesive base.
As the support sheet, non-woven fabric, knitted cloth, woven cloth, polyurethane film, polyurethane foam, polyethylene film, PP (polypropylene), EVA (ethylene vinyl acetate) and the like are suitable in consideration of flexibility. For films, a thickness of 3 to 70 μm is suitable. In particular, a polyurethane film having a thickness of 3 to 50 μm is preferable. A polyurethane film having a thickness of 5 to 15 μm that can be applied for a long time without stuffiness on the skin is more preferable as the support sheet.

本発明の外用剤・化粧料を製造するには、粘着性基剤によって異なる製造法となる。溶液型粘着剤を基剤とする場合（実施例における粘着性組成物Ａ）、粘着性組成物、各種有価物、及びその他添加剤を均一に混合し、得られた粘着剤溶液を離型シート上に塗布し溶媒を乾燥させて、必要に応じて、乾燥させた粘着剤層を支持体シートに積層し、適当なサイズに裁断して製品とする。ホットメルト型粘着剤を基剤とする場合（実施例における粘着性組成物Ｂ）、粘着性組成物、各種有価物、及びその他添加剤を高温で均一混錬した後、得られた粘着剤混合物を離型シートあるいは支持体シートに塗布する。基剤がパップ基剤の場合（実施例における粘着性組成物Ｃ）、粘着性組成物、各種有価物、及びその他添加剤を均一混錬した後、得られた水溶性樹脂組成物を離型シートあるいは支持体シートに塗布する。 In order to produce the external preparation / cosmetic of the present invention, the production method differs depending on the adhesive base. When a solution-type adhesive is used as a base (adhesive composition A in Examples), the adhesive composition, various valuable resources, and other additives are uniformly mixed, and the obtained adhesive solution is used as a release sheet. It is applied on top and the solvent is dried, and if necessary, a dried pressure-sensitive adhesive layer is laminated on a support sheet and cut into an appropriate size to obtain a product. When the hot melt type adhesive is used as a base (adhesive composition B in Examples), the adhesive composition, various valuable resources, and other additives are uniformly kneaded at a high temperature, and then the obtained adhesive mixture is obtained. Is applied to the release sheet or the support sheet. When the base is a pap base (tacky composition C in Examples), the sticky composition, various valuable resources, and other additives are uniformly kneaded, and then the obtained water-soluble resin composition is released from the mold. Apply to sheet or support sheet.

本発明の外用剤及び化粧料を脂肪を除去したい部位の皮膚に適用する。適用箇所は皮膚全般であり、特に限定されない。脂肪を除去したい面積に応じて、外用剤及び化粧料の適用枚数を設定する。１回の適用時間は、０．５時間～４８時間程度であり、複数回の適用の場合は、０～７日の間隔で適用することが効果的である。 The external preparation and cosmetics of the present invention are applied to the skin of the site where fat is desired to be removed. The application site is the entire skin and is not particularly limited. Set the number of external agents and cosmetics to be applied according to the area where you want to remove fat. The application time for one time is about 0.5 hours to 48 hours, and in the case of multiple applications, it is effective to apply at intervals of 0 to 7 days.

本発明により、体の所望する部位の部分痩せが可能である。特に、顔への適用は効果が発揮されやすい。例えば、瞼下に適用した場合、瞼下のふくらみ（目袋）の縮小効果が得られる。 According to the present invention, it is possible to partially thin a desired part of the body. In particular, application to the face is likely to be effective. For example, when applied under the eyelids, the effect of reducing the bulge (eyelids) under the eyelids can be obtained.

以下、本発明を下記実施例によりさらに詳しく説明する。これら実施例は、単に本発明を具体的に説明するための例であり、本発明の範囲がこれら実施例に限定されるものではない。 Hereinafter, the present invention will be described in more detail with reference to the following examples. These examples are merely examples for specifically explaining the present invention, and the scope of the present invention is not limited to these examples.

実施例１～７
表１に示すように、HiPAS（登録商標）粘着剤（アクリルエステル、コスメディ製薬（株）製）等の３種の粘着剤組成物１００質量部に、エタノールに溶解させたホスファチジルコリン（和光純薬）とデオキシコール酸（和光純薬）、ならびにその他の成分を添加し均一な溶液とし、厚さ２６μｍのＰＥＴシートに塗布し、乾燥させて厚さ５０μｍの粘着剤層が積層されたテープ型製剤を得た。 Examples 1-7
As shown in Table 1, phosphatidylcholine (Wako Pure Chemical Industries, Ltd.) dissolved in ethanol in 100 parts by mass of three kinds of pressure-sensitive adhesive compositions such as HiPAS (registered trademark) pressure-sensitive adhesive (acrylic ester, manufactured by Cosmed Pharmaceutical Industries, Ltd.) ), Deoxycholic acid (Wako Pure Chemical Industries, Ltd.), and other ingredients to make a uniform solution, which is applied to a PET sheet with a thickness of 26 μm, dried, and a tape-type preparation in which a pressure-sensitive adhesive layer with a thickness of 50 μm is laminated. Got

Figure 2022020578000001
Figure 2022020578000001

粘着剤組成物A：HiPAS（登録商標）粘着剤100質量部にミリスチン酸イソプロピル（IPM）10質量部を含む組成物
粘着剤組成物B：SIS、流動パラフィン、アルコンP100（粘着付与剤）を30：40：30質量部の割合にて150℃加温しながら混合した組成物
粘着剤組成物C：ポリアクリル酸ナトリウム、濃グリセリン、水、クエン酸、アルミニウムグリシネートを8：30：50：1：0.1質量部の割合にて混合した組成物
安定化剤：１．アスタキサンチン、２．酢酸トコフェロール、３．ジエタノールアミン Adhesive composition A: Composition containing 10 parts by mass of isopropyl myristate (IPM) in 100 parts by mass of HiPAS (registered trademark) Adhesive composition B: SIS, liquid paraffin, 30 parts of Archon P100 (adhesive imparting agent) : 40: 30 parts by mass of composition mixed while heating at 150 ° C. Adhesive composition C: Sodium polyacrylate, concentrated glycerin, water, citric acid, aluminum glycinate 8:30:50: 1 : Composition stabilizer mixed at a ratio of 0.1 parts by mass: 1. Astaxanthin, 2. Tocopherol acetate, 3. Diethanolamine

実施例８ パッチ剤の製造
粘着剤溶液に乾燥後の質量部割合が表２記載となるように各種成分をエタノールに溶解させ添加し、均一な溶液とし、厚さ４０μｍの離型ＰＥＴシートに塗布し乾燥させて後、ウレタンフィルム（厚さ１０μｍ）に転写し、厚さ５０μｍの粘着剤層が積層されたシート状製剤を得た。得られたシートを図１のようなテープに打ち抜いて、７０×９５ｍｍの脂肪燃焼パッチ剤を得た。 Example 8 Production of patch agent Various components are dissolved in ethanol and added to the adhesive solution so that the parts by mass after drying are shown in Table 2, and the solution is made uniform and applied to a release PET sheet having a thickness of 40 μm. After drying, the product was transferred to a urethane film (thickness 10 μm) to obtain a sheet-like preparation having an adhesive layer having a thickness of 50 μm laminated. The obtained sheet was punched into a tape as shown in FIG. 1 to obtain a fat burning patch having a size of 70 × 95 mm.

Figure 2022020578000002
Figure 2022020578000002

皮下脂肪厚さの評価
〈被験者数〉 ９名
〈測定期間〉 前半２週間 ＋ 後半２週間
※使用前、使用２週間目、使用４週間目に皮下脂肪厚を測定した。
〈適用方法〉 二の腕：上腕外側の肘から８ｃｍのところから貼り付けた。
腹部：おへそをはさんで左右に縦に貼り付けた。
〈貼付時間〉 最長入浴後から翌日入浴前まで。毎日貼り換えた。
〈測定方法〉
腹部: 皮下脂肪の厚み測定：タニタ皮下脂肪厚計SR803を用いて測定した。
おへそから５ｃｍ程度横に、本人から見て右側縦向きに測定した。
二の腕: 皮下脂肪の厚み測定：タニタ皮下脂肪厚計SR803を用いて測定した。
上腕外側の肘から１０ｃｍのところを測定した。
〈結果〉
使用前測定データを１００％とし、使用後の数値を算出した。結果を表３、４及び図２、３に示す。 Evaluation of subcutaneous fat thickness <Number of subjects> 9 subjects <Measurement period> First half 2 weeks + Second half 2 weeks * Subcutaneous fat thickness was measured before use, 2 weeks after use, and 4 weeks after use.
<Application method> Upper arm: Attached from 8 cm from the elbow on the outside of the upper arm.
Abdomen: Attached vertically to the left and right with the navel in between.
<Attachment time> From the longest bathing period to the next day before bathing. I replaced it every day.
<Measuring method>
Abdomen: Subcutaneous fat thickness measurement: Measured using Tanita Subcutaneous Fat Thickness Gauge SR803.
The measurement was performed about 5 cm from the navel and vertically to the right of the person.
Upper arm: Subcutaneous fat thickness measurement: Measured using Tanita Subcutaneous Fat Thickness Gauge SR803.
A measurement was made 10 cm from the elbow on the outside of the upper arm.
<result>
The measurement data before use was set to 100%, and the numerical value after use was calculated. The results are shown in Tables 3 and 4 and FIGS. 2 and 3.

Figure 2022020578000003
Figure 2022020578000003

Figure 2022020578000004
Figure 2022020578000004

腹部、及び二の腕に貼付した本発明のパッチ剤により４週間で明瞭な皮下脂肪の減少が観察された。

A clear decrease in subcutaneous fat was observed in 4 weeks by the patch of the present invention applied to the abdomen and upper arm.

Claims (15)

脂肪分解剤、脂肪溶解剤又は脂肪代謝促進剤のいずれか１種以上を含有し、脂肪低減又は/及び部分痩せ又は/及び肌引き締めを目的とする外用剤又は化粧料。 An external preparation or cosmetic containing one or more of a lipolytic agent, a fat dissolving agent or a fat metabolism promoting agent, for the purpose of reducing fat and / and partially thinning or / and tightening the skin. 脂肪分解剤、脂肪溶解剤及び脂肪代謝促進剤からなる群から選ばれる１種以上の脂肪減少に働く成分を０．１質量％以上含有する脂肪低減又は/及び部分痩せ又は/及び肌引き締めを目的とする外用剤又は化粧料。 For the purpose of fat reduction and / and partial thinning or / and skin tightening containing 0.1% by mass or more of one or more components acting on fat reduction selected from the group consisting of lipolytic agents, fat dissolving agents and fat metabolism promoters. External preparations or cosmetics. 脂肪分解剤がリパーゼである、請求項１又は２に記載の外用剤又は化粧料。 The external preparation or cosmetic according to claim 1 or 2, wherein the lipolytic agent is lipase. リパーゼとＭｇ塩及びＣａ塩とが含まれている、請求項３に記載の外用剤又は化粧料。 The external preparation or cosmetic according to claim 3, which contains a lipase, an Mg salt and a Ca salt. 脂肪溶解剤がホスファチジルコリン、アデノシン三リン酸及びそのナトリウム塩ならびにデオキシコール酸及びその塩からなる群より選ばれる１種以上である、請求項１又は２に記載の外用剤又は化粧料。 The external preparation or cosmetic according to claim 1 or 2, wherein the fat-dissolving agent is at least one selected from the group consisting of phosphatidylcholine, adenosine triphosphate and sodium salts thereof, and deoxycholic acid and salts thereof. 脂肪代謝促進剤がアミノ酸、Ｌ－カルニチン、イノシトール、カプサイシン及びカフェインからなる群より選ばれる１種以上である、請求項１又は２に記載の外用剤又は化粧料。 The external preparation or cosmetic according to claim 1 or 2, wherein the fat metabolism promoter is at least one selected from the group consisting of amino acids, L-carnitine, inositol, capsaicin and caffeine. アミノ酸がチロシン、セリン、トレオニン、フェニルアラニン、トリプトファン、イソロイシン、リジン、アルギニン、ベタイン、ヒスチジン、グルタミン、グリシン及びシステインからなる群より選ばれる１種以上である、請求項６に記載の外用剤又は化粧料。 The external preparation or cosmetic according to claim 6, wherein the amino acid is at least one selected from the group consisting of tyrosine, serine, threonine, phenylalanine, tryptophan, isoleucine, lysine, arginine, betaine, histidine, glutamine, glycine and cysteine. .. 外用剤又は化粧料が貼付シートである、請求項１～７のいずれか１項に記載の外用剤又は化粧料。 The external preparation or cosmetic according to any one of claims 1 to 7, wherein the external preparation or cosmetic is a sticking sheet. アクリル系、ゴム系又はシリコーン系粘着剤を基剤とする、請求項８に記載の外用剤又は化粧料。 The external preparation or cosmetic according to claim 8, which is based on an acrylic, rubber-based or silicone-based adhesive. 水溶性樹脂を基剤とする、請求項８に記載の外用剤又は化粧料。 The external preparation or cosmetic according to claim 8, which is based on a water-soluble resin. ホスファチジルコリンと、アスタキサンチン、酢酸トコフェロール、トコフェロール、パルミチン酸アスコルビル及びジエタノールアミンからなる群より選ばれる1種以上とが共存する外用剤又は化粧料。 An external preparation or cosmetic in which phosphatidylcholine coexists with at least one selected from the group consisting of astaxanthin, tocopherol acetate, tocopherol, ascorbyl palmitate and diethanolamine. デオキシコール酸ナトリウムと酸性物質とが共存する外用剤又は化粧料。 An external preparation or cosmetic in which sodium deoxycholate and an acidic substance coexist. 膏体と支持体シートとから構成され、該膏体がアクリル系、ゴム系又はシリコーン系粘着剤中に脂肪分解剤、脂肪溶解剤又は脂肪代謝促進剤のいずれか１種以上を含有し、該支持体シートが不織布、織布、編み布又はポリウレタンフィルムであり、該膏体厚みが５～２００μｍである、請求項１～９のいずれか１項に記載の外用剤又は化粧料。 It is composed of a plaster body and a support sheet, and the plaster body contains one or more of a lipolytic agent, a lipolytic agent or a fat metabolism promoter in an acrylic, rubber or silicone adhesive, and the said. The external preparation or cosmetic according to any one of claims 1 to 9, wherein the support sheet is a non-woven fabric, a woven cloth, a knitted cloth or a polyurethane film, and the thickness of the plaster is 5 to 200 μm. 前記支持体シートが厚み３～５０μｍのポリウレタンフィルムであり、前記膏体がロール状シートであり、該膏体厚みが５～１００μｍである、請求項１３に記載の外用剤又は化粧料。 The external preparation or cosmetic according to claim 13, wherein the support sheet is a polyurethane film having a thickness of 3 to 50 μm, the plaster is a roll-shaped sheet, and the plaster has a thickness of 5 to 100 μm. 請求項８～１０のいずれか１項に記載の外用剤又は化粧料の製造方法であって、下記（a）、（b）、又は（c）の工程を含む製造方法：
（a）基剤が溶液型粘着剤の場合、
粘着剤溶液、並びに、脂肪分解剤、脂肪溶解剤及び脂肪代謝促進剤からなる群より選ばれる少なくとも１種の有価物を均一に混合する工程、
得られた粘着剤溶液を離型シート上に塗布し、溶媒を乾燥させる工程、並びに
乾燥させた粘着剤層を必要に応じ支持体シートに積層する工程；
（b）基剤がホットメルト型粘着剤の場合、
粘着性組成物、並びに、脂肪分解剤、脂肪溶解剤及び脂肪代謝促進剤からなる群より選ばれる少なくとも１種の有価物を高温で均一混錬する工程、並びに
得られた粘着剤混合物を離型シートあるいは支持体シートに塗布する工程；
（c）基剤がパップ基剤の場合、
水溶性樹脂、脂肪分解剤、脂肪溶解剤及び脂肪代謝促進剤からなる群より選ばれる少なくとも１種の有価物、並びに、水を均一混錬する工程、並びに
得られた水溶性樹脂組成物を離型シートあるいは支持体シートに塗布する工程。

The method for producing an external preparation or cosmetic according to any one of claims 8 to 10, which comprises the following steps (a), (b), or (c):
(A) When the base is a solution type adhesive
A step of uniformly mixing a pressure-sensitive adhesive solution and at least one valuable resource selected from the group consisting of a lipolytic agent, a lipolytic agent and a fat metabolism promoter.
A step of applying the obtained pressure-sensitive adhesive solution on a release sheet and drying the solvent, and a step of laminating the dried pressure-sensitive adhesive layer on the support sheet as needed;
(B) When the base is a hot melt type adhesive
A step of uniformly kneading the tacky composition and at least one valuable material selected from the group consisting of a lipolytic agent, a lipolytic agent and a fat metabolism promoter at a high temperature, and a release of the obtained pressure-sensitive adhesive mixture. The process of applying to a sheet or support sheet;
(C) If the base is a pap base,
Release at least one valuable resource selected from the group consisting of a water-soluble resin, a lipolytic agent, a lipolytic agent and a fat metabolism promoter, a step of uniformly kneading water, and the obtained water-soluble resin composition. The process of applying to a mold sheet or support sheet.
JP2021116514A 2020-07-20 2021-07-14 Cosmetic external preparation and cosmetic Pending JP2022020578A (en)

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JP3907872B2 (en) * 1999-07-06 2007-04-18 株式会社カネボウ化粧品 Sheet-shaped pack cosmetic for body
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US20070071706A1 (en) * 2005-09-28 2007-03-29 Filiberto Zadini Lipodissolving dermatological topical preparation
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