JPH0739748A - Low temperature crosslinked type gel agent - Google Patents
Low temperature crosslinked type gel agentInfo
- Publication number
- JPH0739748A JPH0739748A JP19055093A JP19055093A JPH0739748A JP H0739748 A JPH0739748 A JP H0739748A JP 19055093 A JP19055093 A JP 19055093A JP 19055093 A JP19055093 A JP 19055093A JP H0739748 A JPH0739748 A JP H0739748A
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- Japan
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- weight
- parts
- agent
- acid
- gel
- Prior art date
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- Medicinal Preparation (AREA)
- Cosmetics (AREA)
Abstract
Description
【０００１】[0001]
【産業上の利用分野】本発明は、低温架橋型ゲル基剤及
び低温架橋型ゲル製剤に関する。さらに詳しくは、Ａ：
エタノール及び／又はイソプロパノール、ポリアクリル
酸及び／又はその塩類並びに難溶性多価金属化合物、
Ｂ：ヒドロキシ酸及び水のＡ，Ｂ両成分を３０℃以下で
混合し、ｐＨを４〜６とした低温架橋型ゲル基剤、及び
更にこの基剤に活性成分を含有せしめたゲル製剤に関す
る。TECHNICAL FIELD The present invention relates to a low temperature cross-linkable gel base and a low temperature cross-linkable gel preparation. More specifically, A:
Ethanol and / or isopropanol, polyacrylic acid and / or salts thereof, and sparingly soluble polyvalent metal compounds,
B: A low temperature cross-linking type gel base having a pH of 4 to 6 in which both A and B components of hydroxy acid and water are mixed at 30 ° C. or less, and a gel preparation in which an active ingredient is further contained in this base.
【０００２】[0002]
【従来の技術】従来、化粧用パック剤や、外用剤の基剤
として数多くのものが知られている。2. Description of the Related Art Conventionally, a large number of bases for cosmetic packs and external preparations have been known.
【０００３】例えば、パック剤用の基剤としてポリアク
リル酸ナトリウムと水酸化アルミニウムゲル、軽質無水
硅酸または含水硅酸及び水とからなるパック用基剤（特
開昭５９−９３０１２）が知られている。又パップ剤用
の基剤として、水溶性高分子物質を含有する膏体中に架
橋剤として水酸化アルミナマグネシウムを配合したパッ
プ剤用基剤（特公平４−５０２９１）や、ポリアクリル
酸ナトリウムなどの水溶性高分子物質、架橋剤としての
アルミニウムグリシネート又は水酸化アルミニウムゲ
ル、更にアルコール、ゼラチンを配合したアルコール含
有貼付剤基剤（特公平４−３４９６５）などが知られて
いる。[0003] For example, as a pack base, a pack base comprising sodium polyacrylate, aluminum hydroxide gel, light anhydrous silicic acid or hydrous silicic acid, and water is known (Japanese Patent Laid-Open No. 59-93012). ing. As a base for poultices, a base for poultices (Japanese Patent Publication No. 4-50291) in which magnesium hydroxide hydroxide is mixed as a crosslinking agent in a paste containing a water-soluble polymer substance, sodium polyacrylate, etc. Of water-soluble polymer, aluminum glycinate or aluminum hydroxide gel as a cross-linking agent, and an alcohol-containing patch base (Japanese Patent Publication No. 4-34965) containing alcohol and gelatin.
【０００４】[0004]
【発明が解決しようとする課題】上記パック用基剤は、
ポリアクリル酸ナトリウムと水酸化アルミニウムゲルに
よって高含水性ゲルを形成する。しかし、このゲルは多
量の水分を含有するため、経時的に水分がしみ出した
り、或いはゲルを形成する前に不織布より膏体がはみ出
したりする。そしてそのような点を抑えるために架橋剤
の水酸化アルミニウムゲルを増すと、硬くなって不織布
上に均一に展延出来なかったりする。また、パップ剤用
の基剤において、前者の特公平４−５０２９１号公報記
載の発明は従来のものの欠点がかなり改善されている
が、ゼラチンの使用が望ましく、その場合加温が必要で
あり、熱分解し易い薬物や揮散し易い薬物を使用する場
合は適切ではない。後者の特公平４−３４９６５号公報
記載の基剤においてはアルコール（エタノール）が用い
られており、難溶性かまたは油性の薬物を用いる場合に
適切であるとされているが、ゼラチンを用いるため、や
はり加温が必要である。そして実施例をみると４５℃位
に冷却してからアルコールを添加しているが、４５℃で
はエタノールはかなり揮散する。そして実際の製造現場
では大量に仕込む必要があり、この大量のものを４５℃
迄冷却するためにはかなりのコストがかかり経済的でな
い。本発明は、上記の問題点を解決した、活性成分、特
に熱分解し易い薬剤や、揮散し易い薬剤を含有せしめて
経皮投与製剤とした場合でも薬剤の熱分解や揮散が起こ
らない経皮投与用ゲル基剤、あるいは、同様の問題点を
解決した、活性成分として美肌成分などを含有せしめた
化粧用パック剤等のゲル製剤を提供することを目的とす
る。DISCLOSURE OF INVENTION Problems to be Solved by the Invention
A highly hydrous gel is formed by sodium polyacrylate and aluminum hydroxide gel. However, since this gel contains a large amount of water, the water may exude over time, or the plaster may exude from the nonwoven fabric before forming the gel. If aluminum hydroxide gel, which is a cross-linking agent, is added in order to suppress such a point, it becomes hard and cannot be spread uniformly on the nonwoven fabric. Further, in the base for poultices, the former invention of Japanese Examined Patent Publication No. 4-50291 has considerably improved the drawbacks of the conventional ones, but it is preferable to use gelatin, in which case heating is necessary, It is not appropriate when using a drug that is easily decomposed by heat or a compound that is easily volatilized. Alcohol (ethanol) is used in the base of the latter Japanese Patent Publication No. 4-34965, and it is said that it is suitable when using a poorly soluble or oily drug, but since gelatin is used, After all, heating is necessary. Then, looking at the examples, alcohol is added after cooling to about 45 ° C., but at 45 ° C., ethanol is considerably volatilized. And in the actual manufacturing site, it is necessary to prepare a large amount of this product, and this large amount of product is 45 ° C.
It takes a considerable cost and is not economical to cool down. The present invention has solved the above-mentioned problems, and even when a drug for transdermal administration is prepared by containing an active ingredient, particularly a drug which is easily decomposed by heat, or a drug which is easily evaporated, the drug is not thermally decomposed or evaporated. It is an object of the present invention to provide a gel base for administration, or a gel preparation such as a cosmetic pack containing the skin beautifying component as an active ingredient, which solves the same problems.
【０００５】[0005]
【課題を解決するための手段】このような技術状況に鑑
み、鋭意研究を重ねた結果、Ａ成分として、水溶性高分
子物質であるポリアクリル酸及び／又はその塩類を、架
橋剤である水酸化アルミナマグネシウムを用い、またエ
タノール及び／又はイソプロパノールを用い、またＢ成
分としてヒドロキシ酸及び水を用いることによって、難
溶性あるいは油性の活性成分を配合する場合に好都合
で、かつ貼付時の冷却効果がすぐれ、またゼラチンを用
いなくとも保形性が良好であると共にゼラチンの場合の
ような加温が不要のため種々の薬剤を含むゲル基剤が経
済的に製造できることを見出し、本発明を完成した。即
ち、本発明は（１）下記Ａ，Ｂ両成分を３０℃以下で混
合し、ｐＨを４〜６とした低温架橋型ゲル基剤： Ａ：エタノール及び／又はイソプロパノール、ポリアク
リル酸及び／又はその塩類並びに難溶性多価金属化合物 Ｂ：ヒドロキシ酸及び水、および（２）活性成分を含有
する又は含有しない上記（１）記載の低温架橋型ゲル基
剤からなる低温架橋型ゲル製剤、に関するものである。Means for Solving the Problems In view of the above technical situation, as a result of intensive studies, as a component A, polyacrylic acid and / or a salt thereof which is a water-soluble polymer substance, and a water which is a cross-linking agent are used. By using magnesium oxide alumina, ethanol and / or isopropanol, and by using hydroxy acid and water as the component B, it is convenient when a hardly soluble or oily active ingredient is blended, and the cooling effect at the time of application is good. The present invention has been completed by discovering that gel bases containing various agents can be produced economically because they have excellent shape retention properties without using gelatin and do not require heating unlike gelatin. . That is, the present invention is (1) a low temperature cross-linking type gel base having a pH of 4 to 6 by mixing both components A and B below at 30 ° C .: A: ethanol and / or isopropanol, polyacrylic acid and / or A salt thereof and a sparingly soluble polyvalent metal compound B: a low-temperature cross-linkable gel preparation comprising a hydroxy acid and water, and (2) a low-temperature cross-linkable gel base as described in (1) above, which does or does not contain an active ingredient. Is.
【０００６】本発明において、Ａ成分として水溶性高分
子であるポリアクリル酸及び／又はその塩類が用いられ
るが、これはゲルの主成分として用いられる。このポリ
アクリル酸塩としては、ポリアクリル酸ナトリウム、ポ
リアクリル酸カリウム等のポリアクリル酸の一価金属
塩、ポリアクリル酸モノエタノールアミン、ポリアクリ
ル酸ジエタノールアミン、ポリアクリル酸トリエタノー
ルアミン等のポリアクリル酸のアミン塩、ポリアクリル
酸のアンモニウム塩が挙げられるが、特に好的なものは
アクリル酸ナトリウムである。ポリアクリル酸及び／又
はその塩類の配合量は重量比で膏体全量の２〜１０％が
好適である。なお、ポリアクリル酸或はその塩類以外の
水溶性高分子物質、例えばポリビニールアルコール、ポ
リビニルピロリドン、メトキシエチレン無水マレイン酸
共重合体、メタクリル酸重合体或は多糖類系のアルギン
酸ナトリウム、アルギン酸アンモニウム、カルボキシメ
チルセルロース、カルボキシメチルセルロースナトリウ
ム、ヒドロキシメチルセルロース、ヒドロキシプロピル
セルロース、ヒドロキシプロピルエチルセルロース、メ
チルセルロース、可溶性デンプン、カルボキシメチルア
ミロース、デキストリン等、その他ペクチン、寒天末等
のヘミセルロース、アラビヤゴム、トラガカントゴム、
キサンタンガム等の植物ゴム、アクリル酸デンプン等の
高吸水性高分子等も勿論添加して差し支えない。水溶性
高分子物質全体の配合量は膏体全量に対し重量比で１〜
２０％が好ましい。In the present invention, polyacrylic acid which is a water-soluble polymer and / or a salt thereof is used as the component A, which is used as the main component of the gel. Examples of the polyacrylic acid salt include monovalent metal salts of polyacrylic acid such as sodium polyacrylate and potassium polyacrylate, polyacrylic acid monoethanolamine, polyacrylic acid diethanolamine, and polyacrylic acid triethanolamine. Examples include amine salts of acids and ammonium salts of polyacrylic acid, with sodium acrylate being particularly preferred. The blending amount of polyacrylic acid and / or its salts is preferably 2 to 10% by weight of the total amount of the plaster. Water-soluble polymer substances other than polyacrylic acid or salts thereof, such as polyvinyl alcohol, polyvinylpyrrolidone, methoxyethylene maleic anhydride copolymer, methacrylic acid polymer or polysaccharide-based sodium alginate, ammonium alginate, Carboxymethylcellulose, sodium carboxymethylcellulose, hydroxymethylcellulose, hydroxypropylcellulose, hydroxypropylethylcellulose, methylcellulose, soluble starch, carboxymethylamylose, dextrin, etc., other pectin, hemicelluloses such as agar powder, arabia gum, tragacanth gum,
Of course, vegetable gums such as xanthan gum and superabsorbent polymers such as starch acrylate may be added. The total amount of the water-soluble polymer substance is 1 to 1 by weight relative to the total amount of paste.
20% is preferable.
【０００７】Ａ成分の１つである難溶性多価金属化合物
としては、水酸化アルミナマグネシウム、水酸化アルミ
ニウム・炭酸水素ナトリウム共沈物、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使用できるが、
２価のマグネシウム、３価のアルミニウムの両方が共存
している水酸化アルミナマグネシウムが特に好適に使用
できる。これらは架橋剤として用いられ、その配合量
は、膏体全量に対し重量比で０．２〜３％が好適であ
る。又同じくＡ成分の１つ、エチルアルコール及び／又
はイソプロピルアルコールの配合量は、膏体全量に対し
重量比で２〜２０％が好適である。２％以下であると調
製時ゲル化の反応が早くなり、薄く塗布することができ
なかったり、厚さのむらを生じたりする。２０％以上で
あるとゲル化の反応が遅くなり、支持体からのしみ出し
や、はみ出しが生じる。As the sparingly soluble polyvalent metal compound which is one of the component A, alumina magnesium hydroxide, aluminum hydroxide / sodium hydrogen carbonate coprecipitate, aluminum glycinate, aluminum hydroxide gel and the like can be used.
Alumina magnesium hydroxide in which both divalent magnesium and trivalent aluminum coexist can be particularly preferably used. These are used as a cross-linking agent, and the blending amount thereof is preferably 0.2 to 3% by weight relative to the total amount of the plaster. Similarly, one of the component A, ethyl alcohol and / or isopropyl alcohol is preferably compounded in an amount of 2 to 20% by weight relative to the total amount of the paste. If it is 2% or less, the gelling reaction will be accelerated during preparation, thin coating cannot be performed, and uneven thickness may occur. If it is 20% or more, the gelling reaction becomes slow, and bleeding or bleeding out from the support occurs.
【０００８】Ｂ成分であるヒドロキシ酸は保形性を良好
に保持することができ、このヒドロキシ酸としては、酒
石酸、クエン酸、乳酸、リンゴ酸、グリコール酸、グル
コン酸、サリチル酸などが挙げられる。ヒドロキシ酸の
添加量は、膏体全量に対し重量比で０．５〜５％が好適
である。本発明ゲル基剤の調製において、多価アルコー
ル、例えばＤ−ソルビトール、グリセリン、１，３−ブ
タンジオール等を保湿剤として用いることができる。そ
の他、防腐剤や香料、着色料等も適宜配合して差し支え
ない。防腐剤としてはパラオキシ安息香酸メチル，パラ
オキシ安息香酸ブチル等のパラベン類，チモール，イソ
プロピルメチルフェノールなどが挙げられる。香料とし
てはペパーミント，スペアミントなどのミント系香料，
レモン，オレンジなどのシトラス系香料及びその他の各
種天然香料又は合成香料などが挙げられる。また，着色
料としては各種合成色素（タール色素），天然色素，ア
ルミニウムレーキ，顔料などが挙げられる。The hydroxy acid which is the component B can maintain good shape retention property, and examples of the hydroxy acid include tartaric acid, citric acid, lactic acid, malic acid, glycolic acid, gluconic acid and salicylic acid. The amount of hydroxy acid added is preferably 0.5 to 5% by weight relative to the total amount of the paste. In the preparation of the gel base of the present invention, a polyhydric alcohol such as D-sorbitol, glycerin, 1,3-butanediol can be used as a moisturizer. In addition, preservatives, fragrances, coloring agents and the like may be appropriately added. Examples of preservatives include parabens such as methyl paraoxybenzoate and butyl paraoxybenzoate, thymol and isopropylmethylphenol. As fragrances, mint flavors such as peppermint and spearmint,
Examples include citrus flavors such as lemon and orange, and various other natural flavors or synthetic flavors. Examples of colorants include various synthetic pigments (tar pigments), natural pigments, aluminum lakes and pigments.
【０００９】本発明のゲル基剤は活性成分を更に含有さ
せて低温架橋型ゲル製剤とすることができ、この活性成
分としてはパック剤等に用いられる美肌成分等の非薬剤
と、薬剤経皮吸収製剤として用いられる薬剤成分とがあ
る。本発明を例えばパック剤として用いる場合、配合す
る美肌成分としては特に制限されることはなく、従来の
パック剤で用いられているアスコルビン酸又はそのエス
テル，プラセンターエキス，コウジ酸，桑白皮，グルタ
チオン，感光素などの美白剤，ヒアルロン酸，コラーゲ
ン，ローヤルゼリー，アロエ，尿素などの保湿剤，イオ
ウ，サリチル酸，レゾルシンなどの角質軟化剤，トラネ
キサム酸，アラントイン，グリチルリチン酸などの抗炎
症剤，各種ビタミン剤等の各種の美肌用活性物質などを
適宜、単独或いは組合せて使用することができる。又、
本発明を薬剤経皮吸収製剤として用いる場合、配合する
薬剤としては、経皮吸収される薬剤であれば特に制限さ
れず、局所的に使用する薬剤及び全身的に適用する薬剤
いずれのものも使用される。例えば狭心症発作に対し、
血管拡張剤であるニトログリセリン、硝酸イソソルビ
ド、亜硝酸アミル等が挙げられ、気管支喘息に対し、鎮
咳、去痰の作用があるフマル酸フォルモテロール、リン
酸ジモルファン、クエン酸カルベタペンタン、塩酸プロ
カテロール等が挙げられる。更に、消炎鎮痛のためのサ
リチル酸メチル等のサリチル酸誘導体、ｌ−メントー
ル、ｄｌ−カンフル、ノニル酸ワニリルアミド等の他、
ジクロフェナクナトリウム、インドメタシン、ケトプロ
フェン、ピロキシカム、イブプロフェン等の非ステロイ
ド系薬剤、トリアムシノロンアセトニド、デキサメタゾ
ン、フルオロシノロンアセトニド等のステロイド系薬
剤、あるいはジフェンヒドラミン、マレイン酸クロルフ
ェニラミン等の抗ヒスタミン剤等が挙げられる。その
他，塩酸エペリゾン，ダントロレンナトリウム等の骨格
筋弛緩剤，塩酸モルヒネ，リン酸コディン等の麻薬等も
無論使用することができる。The gel base of the present invention can be made into a low temperature cross-linking type gel preparation by further containing an active ingredient. As this active ingredient, a non-drug such as a skin-care ingredient used in a pack or the like and a drug transdermal There are drug components used as absorption preparations. When the present invention is used, for example, as a pack agent, the skin beautifying ingredient to be blended is not particularly limited, and ascorbic acid or its ester, placenta extract, kojic acid, mulberry bark, which are used in conventional pack agents, Glutathione, whitening agents such as photosensitizers, hyaluronic acid, collagen, royal jelly, moisturizers such as aloe and urea, keratin softeners such as sulfur, salicylic acid and resorcin, anti-inflammatory agents such as tranexamic acid, allantoin and glycyrrhizinic acid, various vitamins Various active substances for skin beautification such as agents can be appropriately used alone or in combination. or,
When the present invention is used as a drug percutaneous absorption preparation, the drug to be blended is not particularly limited as long as it is a drug percutaneously absorbed, and both locally applied drugs and systemically applied drugs are used. To be done. For example, for an angina attack,
Examples include vasodilators nitroglycerin, isosorbide nitrate, amyl nitrite, etc., for bronchial asthma, antitussive, formoterol fumarate, dimorphan phosphate, carbetapentane citrate, procaterol hydrochloride, etc. which have an expectorant action. Can be mentioned. Further, other salicylic acid derivatives such as methyl salicylate for anti-inflammatory analgesia, l-menthol, dl-camphor, nonyl acid vanillylamide, etc.,
Examples thereof include non-steroidal drugs such as diclofenac sodium, indomethacin, ketoprofen, piroxicam, ibuprofen, steroidal drugs such as triamcinolone acetonide, dexamethasone and fluorocinolone acetonide, and antihistamines such as diphenhydramine and chlorpheniramine maleate. In addition, skeletal muscle relaxants such as eperisone hydrochloride and dantrolene sodium, and narcotics such as morphine hydrochloride and codin phosphate can of course be used.
【００１０】そして、本発明においては特に熱分解し易
い美肌成分や薬剤、例えばアスコルビン酸又はそのエス
テル，レチノール又はそのエステル，ビタミンＡ油，酢
酸ヒドロキソコバラミン，エルゴカルシフェノールなど
のビタミン類，硝酸イソソルビド，ニトログリセリン，
エナント酸テストステロン，酒石酸エルゴタミン，イン
スリンなどが挙げられる。揮発し易い美肌成分や薬物、
例えばユーカリ油，ニクズク油，チアミン油，ハッカ
油，メントール，カンフルなどのテルペン類，亜硝酸ア
ミル，トリメタジオン等が好適に用いられる。In the present invention, the components and agents for skin which are particularly susceptible to thermal decomposition, such as ascorbic acid or its ester, retinol or its ester, vitamin A oil, hydroxocobalamin acetate, ergocalciphenol and other vitamins, isosorbide nitrate, Nitroglycerin,
Examples include testosterone enanthate, ergotamine tartrate, and insulin. Volatile skin ingredients and drugs,
For example, terpenes such as eucalyptus oil, nutmeg oil, thiamine oil, peppermint oil, menthol and camphor, amyl nitrite and trimetadione are preferably used.
【００１１】又、本発明では美肌成分、薬用成分共に入
っていないゲル剤をそのまま、例えば不織布に塗布して
低温架橋型アイマスク等として用いることもできる。本
発明のゲル基剤の調製は例えば下記方法によって行われ
る。ヒドロキシ酸を必要量の精製水に溶解し、これに必
要により多価アルコールを加えてＢ成分とする。次にポ
リアクリル酸及び／又はその塩と水酸化アルミナマグネ
シウムを混合し、更に必要によりポりアクリル酸又はそ
の塩以外の水溶性高分子物質を加え、これにエタノール
及び／又はイソプロパノールを加え充分撹拌し均一の混
合物たるＡ成分とする。これに、先に調製したヒドロキ
シ酸の溶液Ｂを加え撹拌混合し、ゲル基剤とする。防腐
剤を使用する時は、エタノール及び／又はイソプロパノ
ールを加える際、それに混合溶解すればよい。Further, in the present invention, the gel agent containing neither the skin beautifying component nor the medicinal component can be applied as it is to, for example, a non-woven fabric to be used as a low temperature cross-linking type eye mask. The gel base of the present invention is prepared, for example, by the following method. The hydroxy acid is dissolved in a required amount of purified water, and if necessary, a polyhydric alcohol is added to obtain the component B. Next, polyacrylic acid and / or its salt and alumina magnesium hydroxide are mixed, and if necessary, a water-soluble polymer substance other than polyacrylic acid or its salt is added, and ethanol and / or isopropanol is added to this and stirred well. A component, which is a uniform mixture, is used. To this, the solution B of the hydroxy acid prepared above is added and mixed by stirring to form a gel base. When a preservative is used, it may be mixed and dissolved when adding ethanol and / or isopropanol.
【００１２】更に、本発明のゲル製剤は上記で得られた
ゲル基剤に適宜例えば美肌成分を加えてパック剤などに
するか、或いは局所作用薬又は全身作用薬を調製時、適
宜配合することによって得られる。この場合これらの美
肌成分あるいは薬用成分は精製水，エタノール，イソプ
ロパノール，多価アルコール又はその他の溶解剤に適
宜，溶解又は分散して配合する。本発明において、低温
架橋型ゲル基剤及び該製剤のｐＨを４〜６とするが、こ
れはＡ成分とＢ成分のｐＨがゲル強度や架橋速度並びに
美肌成分あるいは薬用成分の安定性に大きく影響するた
めである。例えばこれ以外の範囲ではｐＨが高いとゲル
形成が遅延されたり経時的にゲルから水が放出しやすく
なる。反対にｐＨが低いと架橋速度が速いため均一なゲ
ルが得られなかったり，貼付剤とする場合は展延出来な
かったりゲル強度が弱いため皮膚残りが生じたりする。Further, the gel preparation of the present invention may be prepared by adding, for example, a skin-beautifying component to the gel base obtained above to form a pack or the like, or a local or systemic agent may be appropriately added during preparation. Obtained by In this case, these skin beautifying ingredients or medicinal ingredients are appropriately dissolved or dispersed in purified water, ethanol, isopropanol, polyhydric alcohol or other solubilizers. In the present invention, the pH of the low temperature crosslinkable gel base and the formulation is set to 4 to 6, which means that the pH of the A component and the B component greatly influences the gel strength, the crosslinking rate and the stability of the skin beautifying component or the medicinal component. This is because For example, in a range other than this, when the pH is high, gel formation is delayed or water is easily released from the gel with time. On the other hand, if the pH is low, a uniform gel cannot be obtained because of a high crosslinking rate, and when it is used as a patch, it cannot be spread or the gel strength is weak, resulting in skin residue.
【００１３】[0013]
【発明の効果】本発明のゲル基剤は、上記の如くゼラチ
ンを使用しないため調製時加熱する必要がなく、又エタ
ノールやイソプロパノールを配合しているため、パック
剤やパップ剤として使用する場合、冷却効果が良好であ
るというすぐれた効果を有する。難溶性薬剤や油性の薬
剤、また熱分解し易い薬剤或いは揮散し易い薬剤を配合
する場合も好都合であり全く問題がない。The gel base of the present invention does not need to be heated at the time of preparation because it does not use gelatin as described above, and since it contains ethanol or isopropanol, when used as a pack or poultice, It has an excellent effect that the cooling effect is good. It is also convenient to mix a poorly soluble drug, an oily drug, a drug that is easily decomposed by heat or a drug that is easily volatilized, and there is no problem at all.
【００１４】[0014]
実施例１ エタノール５．０重量部にパラオキシ安息香酸メチル
０．１重量部を加え溶解させる。さらにポリアクリル酸
ナトリウム５．０重量部、水酸化アルミナマグネシウム
０．２５重量部、カルボキシメチルセルロースナトリウ
ム２．０重量部及び濃グリセリン１５．０重量部を加
え、混合分散し、Ａ液とする。別に精製水５６．１５重
量部に酒石酸１．５重量部及びＤ−ソルビトール液１
５．０重量部を加え完全溶解し、Ｂ液とする。Ａ，Ｂ両
液を２０℃で混合し、ｐＨ４．８の低温架橋型ゲル基剤
を得た。Example 1 To 5.0 parts by weight of ethanol, 0.1 part by weight of methyl paraoxybenzoate was added and dissolved. Further, 5.0 parts by weight of sodium polyacrylate, 0.25 parts by weight of magnesium alumina hydroxide, 2.0 parts by weight of sodium carboxymethyl cellulose and 15.0 parts by weight of concentrated glycerin are added, mixed and dispersed to prepare a liquid A. Separately, in 56.15 parts by weight of purified water, 1.5 parts by weight of tartaric acid and 1 part of D-sorbitol solution.
5.0 parts by weight is added and completely dissolved to prepare a solution B. Both liquids A and B were mixed at 20 ° C. to obtain a low temperature cross-linking type gel base having a pH of 4.8.
【００１５】実施例２ エタノール１０．０重量部にパラオキシ安息香酸メチル
０．１重量部及びポリアクリル酸１．０重量部を加え溶
解させる。さらにポリアクリル酸ナトリウム５．０重量
部、水酸化アルミナマグネシウム０．３重量部、アクリ
ル酸デンプン１．０重量部及び１，３−ブタンジオール
５．０重量部を加え、混合分散し、Ａ液とする。別に精
製水６６．６重量部に酒石酸１．０重量部及びＤ−ソル
ビトール液１０．０重量部を加え完全溶解し、Ｂ液とす
る。Ａ，Ｂ両液を５℃で混合し、ｐＨ４．２の低温架橋
型ゲル基剤を得た。Example 2 To 10.0 parts by weight of ethanol, 0.1 part by weight of methyl paraoxybenzoate and 1.0 part by weight of polyacrylic acid were added and dissolved. Further, 5.0 parts by weight of sodium polyacrylate, 0.3 parts by weight of magnesium hydroxide alumina, 1.0 part by weight of starch acrylate and 5.0 parts by weight of 1,3-butanediol are added, mixed and dispersed, and liquid A And Separately, 1.0 part by weight of tartaric acid and 10.0 parts by weight of D-sorbitol solution are added to 66.6 parts by weight of purified water and completely dissolved to prepare a solution B. Both liquids A and B were mixed at 5 ° C. to obtain a low temperature cross-linking type gel base having pH 4.2.
【００１６】実施例３ イソプロパノール５．０重量部にパラオキシ安息香酸メ
チル０．１重量部及びポリアクリル酸１．０重量部を加
え溶解させる。さらにポリアクリル酸ナトリウム３．０
重量部、水酸化アルミナマグネシウム０．１５重量部、
カルボキシメチルセルロースナトリウム３．０重量部及
び濃グリセリン１５．０重量部を加え、混合分散し、Ａ
液とする。別に精製水６６．７５重量部に乳酸１．０重
量部及び濃グリセリン５．０重量部を加え完全溶解し、
Ｂ液とする。Ａ，Ｂ両液を２０℃で混合し、ｐＨ４．１
の低温架橋型ゲル基剤を得た。Example 3 To 5.0 parts by weight of isopropanol, 0.1 parts by weight of methyl paraoxybenzoate and 1.0 part by weight of polyacrylic acid were added and dissolved. Furthermore, sodium polyacrylate 3.0
Parts by weight, 0.15 parts by weight of magnesium alumina hydroxide,
Add 3.0 parts by weight of sodium carboxymethyl cellulose and 15.0 parts by weight of concentrated glycerin, mix and disperse, and
Use as liquid. Separately, 1.0 part by weight of lactic acid and 5.0 parts by weight of concentrated glycerin were added to 66.75 parts by weight of purified water and completely dissolved,
Use liquid B. Both liquids A and B were mixed at 20 ° C., and the pH was 4.1.
A low temperature cross-linking type gel base of was obtained.
【００１７】実施例４ エタノール３．０重量部にパラオキシ安息香酸メチル
０．１重量部を加え溶解させる。さらにポリアクリル酸
ナトリウム６．０重量部、水酸化アルミナマグネシウム
０．２重量部、カルボキシメチルセルロースナトリウム
１．０重量部、１，３−ブタンジオール５．０重量部及
び濃グリセリン１０．０重量部を加え、混合分散し、Ａ
液とする。別に精製水６３．７重量部にリンゴ酸１．０
重量部及びＤ−ソルビトール液１０．０重量部を加え完
全溶解し、Ｂ液とする。Ａ，Ｂ両液を２０℃で混合し、
ｐＨ５．４の低温架橋型ゲル基剤を得た。Example 4 To 3.0 parts by weight of ethanol, 0.1 part by weight of methyl paraoxybenzoate was added and dissolved. Further, 6.0 parts by weight of sodium polyacrylate, 0.2 parts by weight of alumina magnesium hydroxide, 1.0 part by weight of sodium carboxymethyl cellulose, 5.0 parts by weight of 1,3-butanediol and 10.0 parts by weight of concentrated glycerin were added. In addition, mix and disperse, A
Use as liquid. Separately, malic acid 1.0 was added to 63.7 parts by weight of purified water.
Parts by weight and 10.0 parts by weight of D-sorbitol solution are added and completely dissolved to prepare a solution B. Mix both A and B solutions at 20 ℃,
A low temperature crosslinkable gel base having a pH of 5.4 was obtained.
【００１８】実施例５ エタノール５．０重量部にパラオキシ安息香酸メチル
０．１重量部を加え溶解させる。さらにポリアクリル酸
ナトリウム４．０重量部、水酸化アルミナマグネシウム
０．２重量部、カルボキシメチルセルロースナトリウム
２．０重量部及び濃グリセリン１５．０重量部を加え、
混合分散し、Ａ液とする。別に精製水５７．２重量部に
酒石酸１．５重量部及びＤ−ソルビトール１５．０重量
部を加え完全溶解し、Ｂ液とする。Ａ，Ｂ両液を２０℃
で混合し、不織布上に塗付量が２，０００ｃｍ2／１０
０ｇになるように塗付、裁断し、ｐＨ４．６の低温架橋
型アイマスクシートを得た。Example 5 To 5.0 parts by weight of ethanol, 0.1 part by weight of methyl paraoxybenzoate was added and dissolved. Further, 4.0 parts by weight of sodium polyacrylate, 0.2 parts by weight of alumina magnesium hydroxide, 2.0 parts by weight of sodium carboxymethyl cellulose and 15.0 parts by weight of concentrated glycerin were added,
Mix and disperse to prepare a liquid A. Separately, 1.5 parts by weight of tartaric acid and 15.0 parts by weight of D-sorbitol are added to 57.2 parts by weight of purified water and completely dissolved to prepare a solution B. Both A and B solutions at 20 ℃
In mixed, coated with the amount on the non-woven fabric 2,000 cm 2/10
It was applied and cut to 0 g to obtain a low temperature cross-linking type eye mask sheet having a pH of 4.6.
【００１９】実施例６ エタノール５．０重量部にパラオキシ安息香酸メチル
０．１重量部を加え溶解させる。さらにポリアクリル酸
ナトリウム４．０重量部、水酸化アルミナマグネシウム
０．３重量部、アクリル酸デンプン２．０重量部、１，
３−ブタンジオール５．０重量部及び濃グリセリン１
０．０重量部を加え、混合分散し、Ａ液とする。別に精
製水７１．６重量部に酒石酸１．５重量部及びアスコル
ビン酸リン酸マグネシウム０．５重量部を加え完全溶解
し、Ｂ液とする。Ａ，Ｂ両液を２０℃で混合し、不織布
上に塗付量が２，０００ｃｍ2／１００ｇになるように
塗付、裁断し、ｐＨ５．５の低温架橋型フェイスマスク
シートを得た。Example 6 To 5.0 parts by weight of ethanol, 0.1 part by weight of methyl paraoxybenzoate was added and dissolved. Furthermore, 4.0 parts by weight of sodium polyacrylate, 0.3 parts by weight of alumina magnesium hydroxide, 2.0 parts by weight of starch acrylate, 1,
5.0 parts by weight of 3-butanediol and concentrated glycerin 1
Add 0.0 parts by weight, mix and disperse to prepare a liquid A. Separately, 1.5 parts by weight of tartaric acid and 0.5 parts by weight of magnesium ascorbyl phosphate are added to 71.6 parts by weight of purified water and completely dissolved to prepare a solution B. A, were mixed B both liquids at 20 ° C., coat-like coat-weight on the nonwoven fabric is 2,000 cm 2/100 g, was cut to obtain a low-temperature crosslinking type face mask sheet pH 5.5.
【００２０】実施例７ エタノール５．０重量部にビタミンＡ油１．０重量部、
酢酸トコフェロール０．５重量部及びパラオキシ安息香
酸メチル０．１重量部を加え溶解させる。さらにポリア
クリル酸ナトリウム５．０重量部、水酸化アルミナマグ
ネシウム０．３重量部、カルボキシメチルセルロースナ
トリウム２．０重量部及び濃グリセリン１５．０重量部
を加え、混合分散し、Ａ液とする。別に精製水６０．１
重量部に酒石酸１．０重量部及びＤ−ソルビトール液１
０．０重量部を加え完全溶解し、Ｂ液とする。Ａ，Ｂ両
液を１５℃で混合し、不織布上に塗付量が２，０００ｃ
ｍ2／１００ｇになるように塗付、裁断し、ｐＨ５．２
の低温架橋型アイパックシートを得た。Example 7 5.0 parts by weight of ethanol and 1.0 part by weight of vitamin A oil,
0.5 part by weight of tocopherol acetate and 0.1 part by weight of methyl paraoxybenzoate are added and dissolved. Further, 5.0 parts by weight of sodium polyacrylate, 0.3 parts by weight of magnesium alumina hydroxide, 2.0 parts by weight of sodium carboxymethyl cellulose and 15.0 parts by weight of concentrated glycerin are added, mixed and dispersed to prepare a liquid A. Separately purified water 60.1
1.0 part by weight of tartaric acid and 1 part of D-sorbitol solution
Add 0.0 parts by weight to completely dissolve and prepare a solution B. Both A and B liquids are mixed at 15 ° C, and the coating amount is 2,000c on the non-woven fabric.
m 2 / coating with so as to 100g, cut, pH5.2
A low temperature crosslinkable eye pack sheet was obtained.
【００２１】実施例８ エタノール５．０重量部にユーカリ油０．５重量部、ニ
クズク油０．５重量部、ｌ−メントール０．７重量部、
ｄｌ−カンフル１．０重量部及びパラオキシ安息香酸メ
チル０．１重量部を加え溶解させる。さらにポリアクリ
ル酸ナトリウム５．０重量部、水酸化アルミナマグネシ
ウム０．２５重量部、カルボキシメチルセルロースナト
リウム２．０重量部及び濃グリセリン１５．０重量部を
加え、混合分散し、Ａ液とする。別に精製水５３．１５
重量部に酒石酸１．５重量部及びＤ−ソルビトール液１
５．０重量部を加え完全溶解し、Ｂ液とする。Ａ，Ｂ両
液を１０℃で混合し、不織布上に塗付量が９００ｃｍ2
／１００ｇになるように塗付、裁断し、ｐＨ５．２の低
温架橋型かぜ用パップ剤を得た。Example 8 5.0 parts by weight of ethanol, 0.5 parts by weight of eucalyptus oil, 0.5 parts by weight of nutmeg oil, 0.7 parts by weight of 1-menthol,
1.0 part by weight of dl-camphor and 0.1 part by weight of methyl paraoxybenzoate are added and dissolved. Further, 5.0 parts by weight of sodium polyacrylate, 0.25 parts by weight of magnesium alumina hydroxide, 2.0 parts by weight of sodium carboxymethyl cellulose and 15.0 parts by weight of concentrated glycerin are added, mixed and dispersed to prepare a liquid A. Separately purified water 53.15
1.5 parts by weight of tartaric acid and 1 part of D-sorbitol solution
5.0 parts by weight is added and completely dissolved to prepare a solution B. Mix both liquids A and B at 10 ° C, and apply a coating amount of 900cm 2 on the non-woven fabric.
The mixture was applied and cut to give 100 g / 100 g to obtain a low-temperature cross-linking cold poultice having a pH of 5.2.
【００２２】実施例９ イソプロパノール１０．０重量部に硝酸イソソルビド
５．０重量部及びパラオキシ安息香酸メチル０．１重量
部を均一分散させる。さらにポリアクリル酸ナトリウム
５．０重量部、水酸化アルミナマグネシウム０．４重量
部、アクリル酸デンプン２．０重量部、１，３−ブタン
ジオール１０．０重量部及び濃グリセリン１０．０重量
部を加え、混合分散し、Ａ液とする。別に精製水２６．
５重量部に酒石酸１．０重量部及びＤ−ソルビトール液
３０．０重量部を加え完全溶解し、Ｂ液とする。Ａ，Ｂ
両液を２０℃で混合し、不織布上に塗付量が２，０００
ｃｍ2／１００ｇになるように塗付、裁断し、ｐＨ５．
２の低温架橋型経皮吸収貼付剤を得た。Example 9 5.0 parts by weight of isosorbide dinitrate and 0.1 part by weight of methyl paraoxybenzoate are uniformly dispersed in 10.0 parts by weight of isopropanol. Furthermore, 5.0 parts by weight of sodium polyacrylate, 0.4 parts by weight of magnesium hydroxide hydroxide, 2.0 parts by weight of starch acrylate, 10.0 parts by weight of 1,3-butanediol and 10.0 parts by weight of concentrated glycerin were added. In addition, they are mixed and dispersed to prepare a liquid A. Separately purified water 26.
To 5 parts by weight, 1.0 part by weight of tartaric acid and 30.0 parts by weight of D-sorbitol solution are added and completely dissolved to prepare a solution B. A, B
Both solutions are mixed at 20 ° C, and the coating amount is 2,000 on the non-woven fabric.
cm 2 / coated with such that 100 g, and cut, pH 5.
A low temperature cross-linking type transdermal absorption patch of 2 was obtained.
【００２３】実施例１０ エタノール５．０重量部にインドメタシン０．５重量
部、ｌ−メントール１．０重量部及びパラオキシ安息香
酸メチル０．１重量部を加え溶解させる。さらにポリア
クリル酸ナトリウム５．０重量部、水酸化アルミナマグ
ネシウム０．３重量部、アクリル酸デンプン２．０重量
部及び１，３−ブタンジオルール５．０重量部を加え、
混合分散し、Ａ液とする。別に精製水６０．１重量部に
酒石酸１．０重量部及びＤ−ソルビトール液３０．０重
量部を加え完全溶解し、Ｂ液とする。Ａ，Ｂ両液を２０
℃で混合し、不織布上に塗付量が１，０００ｃｍ2／１
００ｇになるように塗付、裁断し、ｐＨ５．３の低温架
橋型消炎鎮痛外用貼付剤を得た。実施例における配合割
合を次の表にまとめて示す。Example 10 To 5.0 parts by weight of ethanol, 0.5 parts by weight of indomethacin, 1.0 part by weight of 1-menthol and 0.1 part by weight of methyl paraoxybenzoate were added and dissolved. Furthermore, 5.0 parts by weight of sodium polyacrylate, 0.3 parts by weight of magnesium alumina hydroxide, 2.0 parts by weight of starch acrylate and 5.0 parts by weight of 1,3-butanediolol are added,
Mix and disperse to prepare a liquid A. Separately, 1.0 part by weight of tartaric acid and 30.0 parts by weight of D-sorbitol solution are added to 60.1 parts by weight of purified water and completely dissolved to prepare a solution B. 20 A and B liquids
It was mixed at ° C., coated with the amount on the non-woven fabric 1,000 cm 2/1
It was applied and cut to give 00 g to obtain a low-temperature cross-linking type anti-inflammatory analgesic external patch having a pH of 5.3. The mixing ratios in the examples are summarized in the following table.
【００２４】[0024]
【表１】 [Table 1]
───────────────────────────────────────────────────── フロントページの続き (51)Int.Cl.6 識別記号 庁内整理番号 ＦＩ 技術表示箇所 Ａ６１Ｋ 9/70 ３２４ 47/02 Ｚ 47/32 Ｆ (72)発明者 沢井 義弘 富山県射水郡小杉町戸破後宝1203−１ 救 急薬品工業株式会社内─────────────────────────────────────────────────── ─── Continuation of the front page (51) Int.Cl. 6 Identification number Reference number within the agency FI Technical indication location A61K 9/70 324 47/02 Z 47/32 F (72) Inventor Yoshihiro Sawai Kosugi, Imizu-gun, Toyama Prefecture 1203-1 Machito Hagogo Takashi Pharmaceutical Co., Ltd.
Claims (9)
ｐＨを４〜６とした低温架橋型ゲル基剤： Ａ：エタノール及び／又はイソプロパノール、ポリアク
リル酸及び／又はその塩類並びに難溶性多価金属化合物 Ｂ：ヒドロキシ酸及び水。1. The following components A and B are mixed at 30 ° C. or lower,
Low temperature cross-linking type gel base having a pH of 4 to 6: A: ethanol and / or isopropanol, polyacrylic acid and / or salts thereof and sparingly soluble polyvalent metal compound B: hydroxy acid and water.
アクリル酸ナトリウムである請求項１記載のゲル基剤。2. The gel base according to claim 1, wherein the polyacrylic acid and / or its salt is sodium polyacrylate.
グネシウムである請求項１記載のゲル基剤。3. The gel base according to claim 1, wherein the sparingly soluble polyvalent metal compound is magnesium alumina hydroxide.
酸である請求項１記載のゲル基剤。4. The gel base according to claim 1, wherein the hydroxy acid is tartaric acid, lactic acid or malic acid.
ｐＨを４〜６とした活性成分含有又は非含有の低温架橋
型ゲル製剤： Ａ：エタノール及び／又はイソプロパノール、ポリアク
リル酸及び／又はその塩類並びに難溶性多価金属化合物 Ｂ：ヒドロキシ酸及び水。5. The following components A and B are mixed at 30 ° C. or lower,
Low-temperature cross-linking type gel preparation containing or not containing active ingredient having pH of 4 to 6: A: ethanol and / or isopropanol, polyacrylic acid and / or salts thereof and sparingly soluble polyvalent metal compound B: hydroxy acid and water.
アクリル酸ナトリウムである請求項５記載のゲル製剤。6. The gel preparation according to claim 5, wherein the polyacrylic acid and / or its salt is sodium polyacrylate.
グネシウムである請求項５記載のゲル製剤。7. The gel preparation according to claim 5, wherein the sparingly soluble polyvalent metal compound is magnesium alumina hydroxide.
ゴ酸である請求項５記載のゲル製剤。8. The gel preparation according to claim 5, wherein the hydroxy acid is tartaric acid, lactic acid or malic acid.
５、６、７または８記載のゲル製剤。9. The gel preparation according to claim 5, 6, 7 or 8, wherein the active ingredient is a drug or a skin beautifying ingredient.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP19055093A JP3739100B2 (en) | 1993-07-30 | 1993-07-30 | Low temperature crosslinking gel |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP19055093A JP3739100B2 (en) | 1993-07-30 | 1993-07-30 | Low temperature crosslinking gel |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH0739748A true JPH0739748A (en) | 1995-02-10 |
| JP3739100B2 JP3739100B2 (en) | 2006-01-25 |
Family
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP19055093A Expired - Fee Related JP3739100B2 (en) | 1993-07-30 | 1993-07-30 | Low temperature crosslinking gel |
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| JP (1) | JP3739100B2 (en) |
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