JPS6158446B2 - - Google Patents
Info
- Publication number
- JPS6158446B2 JPS6158446B2 JP15270681A JP15270681A JPS6158446B2 JP S6158446 B2 JPS6158446 B2 JP S6158446B2 JP 15270681 A JP15270681 A JP 15270681A JP 15270681 A JP15270681 A JP 15270681A JP S6158446 B2 JPS6158446 B2 JP S6158446B2
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- thiourea
- urea
- tocopherol
- present
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 33
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 claims description 22
- 239000008194 pharmaceutical composition Substances 0.000 claims description 13
- 239000004202 carbamide Substances 0.000 claims description 11
- LVYLCBNXHHHPSB-UHFFFAOYSA-N 2-hydroxyethyl salicylate Chemical compound OCCOC(=O)C1=CC=CC=C1O LVYLCBNXHHHPSB-UHFFFAOYSA-N 0.000 claims description 7
- RGOVYLWUIBMPGK-UHFFFAOYSA-N nonivamide Chemical compound CCCCCCCCC(=O)NCC1=CC=C(O)C(OC)=C1 RGOVYLWUIBMPGK-UHFFFAOYSA-N 0.000 claims description 6
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 claims description 4
- 229960000520 diphenhydramine Drugs 0.000 claims description 4
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims description 3
- 229960001295 tocopherol Drugs 0.000 claims description 3
- 229930003799 tocopherol Natural products 0.000 claims description 3
- 235000010384 tocopherol Nutrition 0.000 claims description 3
- 239000011732 tocopherol Substances 0.000 claims description 3
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 claims description 3
- 239000004480 active ingredient Substances 0.000 description 10
- 239000000203 mixture Substances 0.000 description 10
- 239000000853 adhesive Substances 0.000 description 6
- 230000001070 adhesive effect Effects 0.000 description 6
- 239000011627 DL-alpha-tocopherol Substances 0.000 description 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 238000009472 formulation Methods 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- -1 vaseline Chemical compound 0.000 description 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 230000000052 comparative effect Effects 0.000 description 3
- 229920001971 elastomer Polymers 0.000 description 3
- 239000004745 nonwoven fabric Substances 0.000 description 3
- 238000002360 preparation method Methods 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-N 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 2
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 2
- 230000001760 anti-analgesic effect Effects 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- 235000011187 glycerol Nutrition 0.000 description 2
- 238000004898 kneading Methods 0.000 description 2
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 2
- 239000000454 talc Substances 0.000 description 2
- 229910052623 talc Inorganic materials 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 description 1
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 description 1
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 1
- RZRNAYUHWVFMIP-KTKRTIGZSA-N 1-oleoylglycerol Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-KTKRTIGZSA-N 0.000 description 1
- UHKPXKGJFOKCGG-UHFFFAOYSA-N 2-methylprop-1-ene;styrene Chemical compound CC(C)=C.C=CC1=CC=CC=C1.C=CC1=CC=CC=C1 UHKPXKGJFOKCGG-UHFFFAOYSA-N 0.000 description 1
- TZZAKSLHHIJRLL-UHFFFAOYSA-N 4-hydroxy-3-methoxybenzamide Chemical compound COC1=CC(C(N)=O)=CC=C1O TZZAKSLHHIJRLL-UHFFFAOYSA-N 0.000 description 1
- 244000215068 Acacia senegal Species 0.000 description 1
- 239000004925 Acrylic resin Substances 0.000 description 1
- 239000005995 Aluminium silicate Substances 0.000 description 1
- 241000416162 Astragalus gummifer Species 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 235000001815 DL-alpha-tocopherol Nutrition 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 229920002367 Polyisobutene Polymers 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 1
- 229920001615 Tragacanth Polymers 0.000 description 1
- YKTSYUJCYHOUJP-UHFFFAOYSA-N [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] Chemical compound [O--].[Al+3].[Al+3].[O-][Si]([O-])([O-])[O-] YKTSYUJCYHOUJP-UHFFFAOYSA-N 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- HDYRYUINDGQKMC-UHFFFAOYSA-M acetyloxyaluminum;dihydrate Chemical compound O.O.CC(=O)O[Al] HDYRYUINDGQKMC-UHFFFAOYSA-M 0.000 description 1
- 229920006243 acrylic copolymer Polymers 0.000 description 1
- 235000012211 aluminium silicate Nutrition 0.000 description 1
- 229940009827 aluminum acetate Drugs 0.000 description 1
- 239000010775 animal oil Substances 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- 235000013871 bee wax Nutrition 0.000 description 1
- 239000012166 beeswax Substances 0.000 description 1
- 239000000440 bentonite Substances 0.000 description 1
- 229910000278 bentonite Inorganic materials 0.000 description 1
- SVPXDRXYRYOSEX-UHFFFAOYSA-N bentoquatam Chemical compound O.O=[Si]=O.O=[Al]O[Al]=O SVPXDRXYRYOSEX-UHFFFAOYSA-N 0.000 description 1
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 description 1
- 239000004327 boric acid Substances 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 229960002504 capsaicin Drugs 0.000 description 1
- 235000017663 capsaicin Nutrition 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- RZRNAYUHWVFMIP-HXUWFJFHSA-N glycerol monolinoleate Natural products CCCCCCCCC=CCCCCCCCC(=O)OC[C@H](O)CO RZRNAYUHWVFMIP-HXUWFJFHSA-N 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- JEIPFZHSYJVQDO-UHFFFAOYSA-N iron(III) oxide Inorganic materials O=[Fe]O[Fe]=O JEIPFZHSYJVQDO-UHFFFAOYSA-N 0.000 description 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
- 229940057995 liquid paraffin Drugs 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 229960001047 methyl salicylate Drugs 0.000 description 1
- 230000003020 moisturizing effect Effects 0.000 description 1
- 229940074096 monoolein Drugs 0.000 description 1
- FBUKVWPVBMHYJY-UHFFFAOYSA-M nonanoate Chemical compound CCCCCCCCC([O-])=O FBUKVWPVBMHYJY-UHFFFAOYSA-M 0.000 description 1
- 230000009965 odorless effect Effects 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 239000000123 paper Substances 0.000 description 1
- 239000003208 petroleum Substances 0.000 description 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N phenol group Chemical group C1(=CC=CC=C1)O ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 description 1
- 239000002985 plastic film Substances 0.000 description 1
- 229920006255 plastic film Polymers 0.000 description 1
- 229920001083 polybutene Polymers 0.000 description 1
- 229920006267 polyester film Polymers 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- 229920002379 silicone rubber Polymers 0.000 description 1
- 239000004945 silicone rubber Substances 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 229920006132 styrene block copolymer Polymers 0.000 description 1
- 229920003002 synthetic resin Polymers 0.000 description 1
- 239000000057 synthetic resin Substances 0.000 description 1
- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 229940099259 vaseline Drugs 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- 239000002759 woven fabric Substances 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Description
【発明の詳細な説明】
本発明は外皮適用医薬組成物、特に湿布用及び
貼付用医薬組成物の改良に関する。
外皮適用製剤、特に消炎鎮痛湿布剤、貼付剤中
には一般にカプサイシン、ノニル酸バニリルアミ
ド、サリチル酸メチル、サリチル酸モノエチレン
グリコール、トコフエロール、ジフエンヒドラミ
ンなどの有効成分が配合される。
これら有効成分はフエノール性水酸基、エステ
ル結合及び/又はアミド結合などを有していると
ころから不安定であり、市販の消炎鎮痛外用製剤
の多くは2〜3年程度の保存により、当初の薬効
が得られないことがしばしばである。また上記有
効成分中には強い薬品臭を有するものがあり、そ
のため患者にその使用が忌壁されることも見聞さ
れる。
本発明者らは、上記有効成分の経日安定性の改
善及び無臭化を図るべく研究を重ねた結果、上記
有効成分の配合された外皮適用医薬組成物中にチ
オ尿素及び尿素を添加するとこれら問題点が一挙
に解決されることを見出した。
本発明はかかる知見に基づいて完成されたもの
であり、ノニル酸バニリルアミド、サリチル酸モ
ノエチレングリコール、トコフエロール、ジフエ
ンヒドラミンから選ばれた少なくとも一種及び製
剤上許容される基剤を含有する外皮適用医薬組成
物において、チオ尿素および尿素を配合すること
による外皮適用医薬組成物に関する。
本発明医薬組成物はチオ尿素及び尿素の両者を
配合することが必須であるが、両者の配合比は使
用される薬物によつて異なるが、概してチオ尿素
1重量部に対して尿素0.1〜10、好ましくは0.3〜
5重量部である。
本発明医薬組成物中に配合されるチオ尿素と尿
素の総量は、薬物により異なるが、0.0005〜50重
量%である。
本発明にて用いられる製薬上許容される基剤
は、外皮適用剤の製造上用いられる基剤であれば
いずれでもよく、たとえば次の如きものが好まし
いものとして列挙される。
湿布用基剤(たとえばカリオン、ベントナイ
ト、酸化チタン、酸化亜鉛、タルク、ロウ、ワ
セリン、ホウ酸、珪酸アルミニウムなど)。
粘着含水系貼付基剤(たとえば、アルギン酸
ソーダー、ポリアクリル酸系樹脂、ポリビニル
ピロリドン、ポリビニルアルコール、トラガン
トガム、アラビアゴム、カルボキシメチルセル
ロース、ゼラチンなど)。
粘着無水系貼付基剤〔たとえばゴム及び/又
は合成樹脂を主体とするもの(例えば、シリコ
ーンゴム、ポリイソブチレンゴム、アクリル系
共重合物、ポリビニルアルキルエーテル化合物
など)など〕
本発明医薬組成物中には、さらに流動パラフイ
ン、動物油、植物油、ポリブテンなどの軟化剤、
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、ソルビトール、酢酸アルミニウム
などの保湿剤、ベンガラ、炭酸カルシウムなどの
充填剤、抗酸化剤などを添加してもよい。
本発明の医薬組成物は、各成分をたとえば撹拌
擂潰機、二軸混練機、アジホモミキサー、高トル
ク撹拌機、練合機を用いて混練することによつて
調製され、一般に湿布剤、粘着貼付剤として使用
に供される。練合時の温度は5℃〜130℃、好ま
しくは湿布剤では10℃〜30℃、粘着貼付剤の場合
は60℃〜120℃である。
かくして得られる製剤は、そのまま患部に適用
してもよく、また公知の担持体(紙、織布、不織
布、発泡シート、ゴムシート、プラスチツクフイ
ルムなど)上に展延して適用してもよい。
次に本発明の実施例を示すが文中%とは重量%
を意味する。
実施例 1
有効成分組成物 2.5%
内訳100%として
サリチル酸モノエチレングリコール 30%
l−メントール 30%
dl−カンフル 35%
α−dl−トコフエロール 5%
尿 素 8.0%
チオ尿素 4.0%
カオリン 10.0%
タルク 35.5%
水 33.0%
グリセリン 7.0%
以上諸剤を撹拌機に投入し、40分撹拌してペー
スト状になつたところでこれを取り出し湿布用医
薬組成物を得た。
かくして得られた湿布用医薬組成物は薬品臭が
ほとんどなく、また当該湿布剤をビン詰めして40
℃、湿度60%にて3ケ月保存した後の有効成分の
含量低下はサリチル酸モノエチレングリコールが
6.5%、α−dl−トコフエロールが3.4%であつ
た。一方、上記処方から尿素、チオ尿素を除いて
得た湿布剤は強い薬品臭を有し、これを上記と同
一条件にて保存した後の有効成分の含量低下はサ
リチル酸モノエチレングリコールが17.9%、α−
dl−トコフエロールが15.6%であつた。
実施例 2
1 有効成分組成物 8.5%
内訳100%として
サリチル酸モノエチレングリコール 63.6%
l−メントール 26.4%
α−dl−トコフエロール 1.3%
ジフエンヒドラミン 1.7%
ノニル酸バニリルアミド 0.2%
オウバクエキス 6.8%
2 尿素、チオ尿素混合物 11.5%
内訳100%として
尿 素 55%
チオ尿素 45%
3 スチレン−イソブチレン−スチレンブロツク
共重合体 30%
4 ミツロウ 3%
5 オリーブ油 4%
6 石油樹脂 38%
7 水 4.5%
8 ソルビタンモノオレイン 0.5%
配合番号3、4、5を120℃で二軸ニーダーで
溶解混練する。次に2、6、8を加え、同温で20
分混練し、温度を70℃まで落とした後1を加え5
分混練し、7を加えて20分練合して粘着性医薬組
成物を得る。この貼着性組成物を75℃で不織布の
上に厚さ0.2mmに展延塗付した。この薬剤面にポ
リエステルフイルムを被覆した。一方実施例2の
処方から尿素及びチオ尿素を除いた粘着性医薬組
成物を得、同様に不織布上に展延してポリエチレ
ンフイルムで被覆した(比較例)
各々の製剤をポリエステルフイルムをはがして
患部に貼付したところ、実施例2の製剤はほとん
ど臭気がなく、8〜10時間治療効果が認められた
のに対して比較例の製剤は薬品臭が強く、治療効
果は4〜5時間しか認められなかつた。
また実施例2及び比較例の膏体をビン詰して40
℃、湿度60%にて3ケ月保存した後の各有効成分
の含量低下は第1表に示した通りである。
【表】DETAILED DESCRIPTION OF THE INVENTION The present invention relates to improvements in pharmaceutical compositions for external use, particularly for poultices and patches. External preparations, particularly anti-inflammatory and analgesic poultices and patches, generally contain active ingredients such as capsaicin, nonylic acid vanillylamide, methyl salicylate, monoethylene glycol salicylate, tocopherol, and diphenhydramine. These active ingredients are unstable because they contain phenolic hydroxyl groups, ester bonds, and/or amide bonds, and many commercially available anti-inflammatory and analgesic topical preparations lose their original efficacy after being stored for about 2 to 3 years. It is often not possible to obtain it. Furthermore, some of the above-mentioned active ingredients have a strong chemical odor, and it has been reported that patients are reluctant to use them. As a result of repeated research aimed at improving the stability of the above-mentioned active ingredients over time and making them odorless, the present inventors have found that when thiourea and urea are added to a pharmaceutical composition for skin application containing the above-mentioned active ingredients, We found that the problems were solved all at once. The present invention was completed based on this knowledge, and provides a dermatologically applied drug containing at least one selected from vanillylamide nonylate, monoethylene glycol salicylate, tocopherol, and diphenhydramine and a pharmaceutically acceptable base. The present invention relates to a pharmaceutical composition for external application by incorporating thiourea and urea in the composition. It is essential that the pharmaceutical composition of the present invention contains both thiourea and urea, and the mixing ratio of the two varies depending on the drug used, but in general, 0.1 to 10 parts by weight of urea to 1 part by weight of thiourea. , preferably 0.3~
It is 5 parts by weight. The total amount of thiourea and urea blended into the pharmaceutical composition of the present invention varies depending on the drug, but is 0.0005 to 50% by weight. The pharmaceutically acceptable base used in the present invention may be any base used in the production of skin-applying agents, and the following are listed as preferred examples. Poultice bases (eg carrion, bentonite, titanium oxide, zinc oxide, talc, wax, vaseline, boric acid, aluminum silicate, etc.). Adhesive water-containing patch base (for example, sodium alginate, polyacrylic resin, polyvinylpyrrolidone, polyvinyl alcohol, gum tragacanth, gum arabic, carboxymethyl cellulose, gelatin, etc.). Adhesive anhydrous patch base (for example, one mainly composed of rubber and/or synthetic resin (for example, silicone rubber, polyisobutylene rubber, acrylic copolymer, polyvinyl alkyl ether compound, etc.)) In the pharmaceutical composition of the present invention In addition, softeners such as liquid paraffin, animal oil, vegetable oil, and polybutene,
Moisturizing agents such as glycerin, propylene glycol, polyethylene glycol, sorbitol, and aluminum acetate, fillers such as red iron oxide and calcium carbonate, antioxidants, and the like may be added. The pharmaceutical composition of the present invention is prepared by kneading each component using, for example, a stirrer and crusher, a twin-screw kneader, an Ajihomo mixer, a high-torque stirrer, or a kneader, and is generally a poultice, Used as an adhesive patch. The temperature during kneading is 5°C to 130°C, preferably 10°C to 30°C for poultices, and 60°C to 120°C for adhesive patches. The preparation thus obtained may be applied to the affected area as it is, or may be spread on a known carrier (paper, woven fabric, nonwoven fabric, foamed sheet, rubber sheet, plastic film, etc.) and applied. Next, examples of the present invention will be shown, and % in the text refers to % by weight.
means. Example 1 Active ingredient composition 2.5% Monoethylene glycol salicylate 30% l-menthol 30% dl-camphor 35% α-dl-tocopherol 5% urea 8.0% thiourea 4.0% kaolin 10.0% talc 35.5% Water: 33.0% Glycerin: 7.0% The above ingredients were put into a stirrer and stirred for 40 minutes to form a paste, which was then taken out and a pharmaceutical composition for compresses was obtained. The thus obtained pharmaceutical composition for poultice has almost no chemical odor, and the poultice can be bottled for 40 minutes.
After storage for 3 months at ℃ and 60% humidity, the content of active ingredients decreased due to monoethylene glycol salicylate.
6.5%, and α-dl-tocopherol was 3.4%. On the other hand, the poultice obtained by removing urea and thiourea from the above formulation has a strong chemical odor, and after storing it under the same conditions as above, the content of active ingredients decreases by 17.9% for monoethylene glycol salicylate, α−
dl-tocopherol was 15.6%. Example 2 1 Active ingredient composition 8.5% Monoethylene glycol salicylate 63.6% l-menthol 26.4% α-dl-tocopherol 1.3% diphenhydramine 1.7% nonylic acid vanillylamide 0.2% Auronicum extract 6.8% 2 Urea, Thiourea mixture 11.5% Urea 55% Thiourea 45% 3 Styrene-isobutylene-styrene block copolymer 30% 4 Beeswax 3% 5 Olive oil 4% 6 Petroleum resin 38% 7 Water 4.5% 8 Sorbitan monoolein 0.5% Mixture numbers 3, 4, and 5 are melted and kneaded in a twin-screw kneader at 120°C. Next, add 2, 6, and 8 and keep at the same temperature for 20 minutes.
Knead for minutes, lower the temperature to 70℃, then add 1 and 5.
Add 7 and knead for 20 minutes to obtain a sticky pharmaceutical composition. This adhesive composition was spread and applied to a thickness of 0.2 mm on a nonwoven fabric at 75°C. This drug surface was covered with a polyester film. On the other hand, an adhesive pharmaceutical composition was obtained by removing urea and thiourea from the formulation of Example 2, and similarly spread on a nonwoven fabric and covered with a polyethylene film (comparative example). When applied to the skin, the formulation of Example 2 had almost no odor and its therapeutic effect was observed for 8 to 10 hours, whereas the formulation of Comparative Example had a strong chemical odor and its therapeutic effect was observed for only 4 to 5 hours. Nakatsuta. In addition, the plasters of Example 2 and Comparative Example were bottled for 40
Table 1 shows the decrease in the content of each active ingredient after storage for 3 months at ℃ and 60% humidity. 【table】
Claims (1)
チレングリコール、トコフエロール、ジフエンヒ
ドラミンから選ばれた少なくとも一種及び製薬上
許容される基剤を含有する外皮適用医薬組成物に
おいて、チオ尿素および尿素を配合することを特
徴とする外皮適用医薬組成物。1. A pharmaceutical composition for skin application containing at least one selected from nonylic acid vanillylamide, monoethylene glycol salicylate, tocopherol, and diphenhydramine and a pharmaceutically acceptable base, characterized in that thiourea and urea are blended. A pharmaceutical composition for external skin application.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP15270681A JPS5855417A (en) | 1981-09-27 | 1981-09-27 | Medicinal composition |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP15270681A JPS5855417A (en) | 1981-09-27 | 1981-09-27 | Medicinal composition |
Publications (2)
Publication Number | Publication Date |
---|---|
JPS5855417A JPS5855417A (en) | 1983-04-01 |
JPS6158446B2 true JPS6158446B2 (en) | 1986-12-11 |
Family
ID=15546364
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP15270681A Granted JPS5855417A (en) | 1981-09-27 | 1981-09-27 | Medicinal composition |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS5855417A (en) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4681897A (en) * | 1984-01-16 | 1987-07-21 | The Procter & Gamble Company | Pharmaceutical products providing enhanced analgesia |
JP2671248B2 (en) * | 1991-10-23 | 1997-10-29 | ブロック・ドラッグ・カンパニー・インコーポレイテッド | Method for enhancing the penetration of medicinal or cosmetic ingredients |
IT1256170B (en) * | 1992-11-03 | 1995-11-29 | DRESSING FOR SKIN PATHOLOGIES | |
JPH06234628A (en) * | 1993-02-09 | 1994-08-23 | Kao Corp | External agent for skin |
JPH0812568A (en) * | 1994-06-30 | 1996-01-16 | Shiseido Co Ltd | Cosmetic |
ATE328868T1 (en) * | 2000-08-21 | 2006-06-15 | Pacific Corp | NEW (THIO)UREA COMPOUNDS AND MEDICINAL COMPOSITIONS CONTAINING THEM |
WO2002016317A1 (en) * | 2000-08-21 | 2002-02-28 | Pacific Corporation | Novel thiocarbamic acid derivatives and the pharmaceutical compositions containing the same |
ATE393141T1 (en) * | 2000-08-21 | 2008-05-15 | Pacific Corp | NEW THIOUREA DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME |
WO2005027642A1 (en) * | 2003-09-25 | 2005-03-31 | Darren Wayne Eade | Repellent preparations |
JP2006001908A (en) * | 2004-06-21 | 2006-01-05 | Daikyo Yakuhin Kogyo Kk | Plaster compounded with beeswax and method for producing the same |
EP2065705B1 (en) * | 2007-11-30 | 2011-07-27 | Roche Diagnostics GmbH | Stabilization of conjugates comprising a thiourea linker |
KR102077954B1 (en) * | 2016-02-25 | 2020-02-14 | 히사미쓰 세이야꾸 가부시키가이샤 | Patch |
-
1981
- 1981-09-27 JP JP15270681A patent/JPS5855417A/en active Granted
Also Published As
Publication number | Publication date |
---|---|
JPS5855417A (en) | 1983-04-01 |
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