JPS6351330A - External plaster containing steroidal agent - Google Patents
External plaster containing steroidal agentInfo
- Publication number
- JPS6351330A JPS6351330A JP61195935A JP19593586A JPS6351330A JP S6351330 A JPS6351330 A JP S6351330A JP 61195935 A JP61195935 A JP 61195935A JP 19593586 A JP19593586 A JP 19593586A JP S6351330 A JPS6351330 A JP S6351330A
- Authority
- JP
- Japan
- Prior art keywords
- water
- agent
- plaster
- parts
- steroid
- 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.)
- Pending
Links
- 239000011505 plaster Substances 0.000 title abstract 5
- 230000003637 steroidlike Effects 0.000 title 1
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 18
- 150000003431 steroids Chemical class 0.000 claims abstract description 17
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 13
- 229920003169 water-soluble polymer Polymers 0.000 claims abstract description 8
- 239000000853 adhesive Substances 0.000 claims description 9
- 230000001070 adhesive effect Effects 0.000 claims description 9
- 239000004615 ingredient Substances 0.000 claims description 5
- DRSFVGQMPYTGJY-GNSLJVCWSA-N Deprodone propionate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)CC)[C@@]1(C)C[C@@H]2O DRSFVGQMPYTGJY-GNSLJVCWSA-N 0.000 claims 1
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 abstract description 11
- 239000000499 gel Substances 0.000 abstract description 11
- 230000000694 effects Effects 0.000 abstract description 10
- -1 etc.) Substances 0.000 abstract description 6
- 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 abstract description 4
- 239000000600 sorbitol Substances 0.000 abstract description 4
- 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 abstract description 3
- 108010010803 Gelatin Proteins 0.000 abstract description 3
- 239000002202 Polyethylene glycol Substances 0.000 abstract description 3
- 238000010521 absorption reaction Methods 0.000 abstract description 3
- 229960001347 fluocinolone acetonide Drugs 0.000 abstract description 3
- FEBLZLNTKCEFIT-VSXGLTOVSA-N fluocinolone acetonide Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O FEBLZLNTKCEFIT-VSXGLTOVSA-N 0.000 abstract description 3
- 239000008273 gelatin Substances 0.000 abstract description 3
- 229920000159 gelatin Polymers 0.000 abstract description 3
- 235000019322 gelatine Nutrition 0.000 abstract description 3
- 235000011852 gelatine desserts Nutrition 0.000 abstract description 3
- 238000000034 method Methods 0.000 abstract description 3
- 229920001223 polyethylene glycol Polymers 0.000 abstract description 3
- 229920001817 Agar Polymers 0.000 abstract description 2
- 208000024780 Urticaria Diseases 0.000 abstract description 2
- 239000008272 agar Substances 0.000 abstract description 2
- 206010061218 Inflammation Diseases 0.000 abstract 2
- 239000004820 Pressure-sensitive adhesive Substances 0.000 abstract 2
- 230000004054 inflammatory process Effects 0.000 abstract 2
- 239000000758 substrate Substances 0.000 abstract 2
- BMFMQGXDDJALKQ-BYPYZUCNSA-N Argininic acid Chemical compound NC(N)=NCCC[C@H](O)C(O)=O BMFMQGXDDJALKQ-BYPYZUCNSA-N 0.000 abstract 1
- 238000013329 compounding Methods 0.000 abstract 1
- 230000032798 delamination Effects 0.000 abstract 1
- 229960002117 triamcinolone acetonide Drugs 0.000 abstract 1
- YNDXUCZADRHECN-JNQJZLCISA-N triamcinolone acetonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O YNDXUCZADRHECN-JNQJZLCISA-N 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 description 12
- 210000003491 skin Anatomy 0.000 description 9
- 230000000699 topical effect Effects 0.000 description 7
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 6
- 229940079593 drug Drugs 0.000 description 5
- 239000003814 drug Substances 0.000 description 5
- 208000017520 skin disease Diseases 0.000 description 5
- 201000004624 Dermatitis Diseases 0.000 description 4
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 4
- 235000011187 glycerol Nutrition 0.000 description 4
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- QWOJMRHUQHTCJG-UHFFFAOYSA-N CC([CH2-])=O Chemical compound CC([CH2-])=O QWOJMRHUQHTCJG-UHFFFAOYSA-N 0.000 description 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 229920002125 Sokalan® Polymers 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 238000004299 exfoliation Methods 0.000 description 3
- 241000411851 herbal medicine Species 0.000 description 3
- 239000004584 polyacrylic acid Substances 0.000 description 3
- 230000000638 stimulation Effects 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
- 206010033546 Pallor Diseases 0.000 description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 description 2
- NIXOWILDQLNWCW-UHFFFAOYSA-N acrylic acid group Chemical group C(C=C)(=O)O NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 2
- 208000010668 atopic eczema Diseases 0.000 description 2
- 239000001913 cellulose Substances 0.000 description 2
- 229920002678 cellulose Polymers 0.000 description 2
- DNTGGZPQPQTDQF-XBXARRHUSA-N crotamiton Chemical compound C/C=C/C(=O)N(CC)C1=CC=CC=C1C DNTGGZPQPQTDQF-XBXARRHUSA-N 0.000 description 2
- 229960003338 crotamiton Drugs 0.000 description 2
- 229960000890 hydrocortisone Drugs 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 239000004745 nonwoven fabric Substances 0.000 description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 description 2
- 229960005205 prednisolone Drugs 0.000 description 2
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 208000024891 symptom Diseases 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 229940070710 valerate Drugs 0.000 description 2
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 2
- FUFLCEKSBBHCMO-UHFFFAOYSA-N 11-dehydrocorticosterone Natural products O=C1CCC2(C)C3C(=O)CC(C)(C(CC4)C(=O)CO)C4C3CCC2=C1 FUFLCEKSBBHCMO-UHFFFAOYSA-N 0.000 description 1
- 229920002126 Acrylic acid copolymer Polymers 0.000 description 1
- 241000894006 Bacteria Species 0.000 description 1
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- MFYSYFVPBJMHGN-ZPOLXVRWSA-N Cortisone Chemical compound O=C1CC[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 MFYSYFVPBJMHGN-ZPOLXVRWSA-N 0.000 description 1
- MFYSYFVPBJMHGN-UHFFFAOYSA-N Cortisone Natural products O=C1CCC2(C)C3C(=O)CC(C)(C(CC4)(O)C(=O)CO)C4C3CCC2=C1 MFYSYFVPBJMHGN-UHFFFAOYSA-N 0.000 description 1
- ITRJWOMZKQRYTA-RFZYENFJSA-N Cortisone acetate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)C)(O)[C@@]1(C)CC2=O ITRJWOMZKQRYTA-RFZYENFJSA-N 0.000 description 1
- 206010012442 Dermatitis contact Diseases 0.000 description 1
- 206010015150 Erythema Diseases 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 206010016936 Folliculitis Diseases 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- 206010062717 Increased upper airway secretion Diseases 0.000 description 1
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical group CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 1
- 229920000057 Mannan Polymers 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- 229920000297 Rayon Polymers 0.000 description 1
- 241000978776 Senegalia senegal Species 0.000 description 1
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 229940022663 acetate Drugs 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical class [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 239000003522 acrylic cement Substances 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 235000010419 agar Nutrition 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 229960001126 alginic acid Drugs 0.000 description 1
- 150000004781 alginic acids Chemical class 0.000 description 1
- 230000000172 allergic effect Effects 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- NBMKJKDGKREAPL-DVTGEIKXSA-N beclomethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O NBMKJKDGKREAPL-DVTGEIKXSA-N 0.000 description 1
- 229940092705 beclomethasone Drugs 0.000 description 1
- RUJUQAPQALJUPC-UHFFFAOYSA-K bis[(2-aminoacetyl)oxy]alumanyl 2-aminoacetate Chemical compound [Al+3].NCC([O-])=O.NCC([O-])=O.NCC([O-])=O RUJUQAPQALJUPC-UHFFFAOYSA-K 0.000 description 1
- DQXBYHZEEUGOBF-UHFFFAOYSA-N but-3-enoic acid;ethene Chemical compound C=C.OC(=O)CC=C DQXBYHZEEUGOBF-UHFFFAOYSA-N 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 229920003123 carboxymethyl cellulose sodium Polymers 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 229940105329 carboxymethylcellulose Drugs 0.000 description 1
- 229940063834 carboxymethylcellulose sodium Drugs 0.000 description 1
- CBGUOGMQLZIXBE-XGQKBEPLSA-N clobetasol propionate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CCl)(OC(=O)CC)[C@@]1(C)C[C@@H]2O CBGUOGMQLZIXBE-XGQKBEPLSA-N 0.000 description 1
- 229960004703 clobetasol propionate Drugs 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 208000010247 contact dermatitis Diseases 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
- BMCQMVFGOVHVNG-TUFAYURCSA-N cortisol 17-butyrate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)CO)(OC(=O)CCC)[C@@]1(C)C[C@@H]2O BMCQMVFGOVHVNG-TUFAYURCSA-N 0.000 description 1
- 229960004544 cortisone Drugs 0.000 description 1
- 229960003290 cortisone acetate Drugs 0.000 description 1
- 239000003431 cross linking reagent Substances 0.000 description 1
- 229960003957 dexamethasone Drugs 0.000 description 1
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 description 1
- 125000004386 diacrylate group Chemical group 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 229920001971 elastomer Polymers 0.000 description 1
- 231100000321 erythema Toxicity 0.000 description 1
- 239000005038 ethylene vinyl acetate Substances 0.000 description 1
- 229960001048 fluorometholone Drugs 0.000 description 1
- FAOZLTXFLGPHNG-KNAQIMQKSA-N fluorometholone Chemical compound C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@]2(F)[C@@H](O)C[C@]2(C)[C@@](O)(C(C)=O)CC[C@H]21 FAOZLTXFLGPHNG-KNAQIMQKSA-N 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 239000000321 herbal drug Substances 0.000 description 1
- 229960001524 hydrocortisone butyrate Drugs 0.000 description 1
- 239000011256 inorganic filler Substances 0.000 description 1
- 229910003475 inorganic filler Inorganic materials 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 230000007721 medicinal effect Effects 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 1
- 208000026435 phlegm Diseases 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 229950010765 pivalate Drugs 0.000 description 1
- IUGYQRQAERSCNH-UHFFFAOYSA-N pivalic acid Chemical compound CC(C)(C)C(O)=O IUGYQRQAERSCNH-UHFFFAOYSA-N 0.000 description 1
- 229920001200 poly(ethylene-vinyl acetate) Polymers 0.000 description 1
- 229920000058 polyacrylate Polymers 0.000 description 1
- 229920002239 polyacrylonitrile Polymers 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 229920002635 polyurethane Polymers 0.000 description 1
- 239000004814 polyurethane Substances 0.000 description 1
- 229920000915 polyvinyl chloride Polymers 0.000 description 1
- 239000004800 polyvinyl chloride Substances 0.000 description 1
- GRLPQNLYRHEGIJ-UHFFFAOYSA-J potassium aluminium sulfate Chemical compound [Al+3].[K+].[O-]S([O-])(=O)=O.[O-]S([O-])(=O)=O GRLPQNLYRHEGIJ-UHFFFAOYSA-J 0.000 description 1
- 238000009101 premedication Methods 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 239000002964 rayon Substances 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 229910000162 sodium phosphate Inorganic materials 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 210000000434 stratum corneum Anatomy 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 210000000106 sweat gland Anatomy 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 239000002759 woven fabric Substances 0.000 description 1
- 235000014692 zinc oxide Nutrition 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
【発明の詳細な説明】
産業上の利用分野
本発明は、ステロイド剤を配合した、外用貼付剤に関す
る。さらに詳しくは、水溶性高分子、水、保水剤を必須
成分とする粘着性ゲル基剤中に皮膚疾患治療用ステロイ
ド剤(デブロドンブロビオネートを除く)を配合させた
ものを柔軟な支持体上に塗布し、この製剤を皮膚疾患部
に対して直接貼付適用することにより、含有するステロ
イド剤を皮膚に投与し治療するためのステロイド剤含有
貼付剤に関する。DETAILED DESCRIPTION OF THE INVENTION Field of the Invention The present invention relates to an external patch containing a steroid agent. More specifically, a flexible support is prepared by blending a steroid agent for treating skin diseases (excluding debrodonbrobionate) into an adhesive gel base whose essential components are a water-soluble polymer, water, and a water-retaining agent. The present invention relates to a steroid-containing patch for administering the contained steroid to the skin and treating the skin by applying the preparation directly to a skin disease area.
従来の技術
従来、湿疹、しん麻疹、小児ストロフルス、外形しん出
仕紅斑、ヘーチェノト症1ffin、指掌山皮症、乾せ
ん等のアレルギー性皮膚疾害、の治療にはコルチゾン等
を生薬とする経口剤、注射剤、外用剤などが用いられて
いる。Conventional technology Conventionally, oral preparations containing herbal medicines such as cortisone have been used to treat allergic skin diseases such as eczema, hives, infantile strophulus, erythema exfoliation, Hechenotism 1ffin, digital palmar dermatitis, and psoriasis. Injections and external preparations are used.
しかしこれらの製剤はなんらかの副作用や使用上の不便
さを有しており、例えば経口剤では飲み忘れや過剰投与
の危険性があり、注射剤では投与時に於ける苦痛やスト
レスが大きくまた個人での投与が困難である。軟膏剤や
ローション剤なとの外用剤では衣服なとを、・θ染ずろ
ばかりてなく定量投与か困難である。また多くの皮膚痰
中ばほとんどの場合そうよう感を伴うため、物理的な刺
激を与えろ衝動にかられ、この刺激のために症状を悪化
さUoることかある等、適切な乙のであるとは言い稚い
。以上のような欠点の改良を目的に、大公ゴムあるいは
アクリル酸エステル−アクリル酸共重合体からなる感圧
性帖?予剤にある杯のステロイド剤を含有さ什たテープ
剤が開発されている。これらのテープ剤は、小;歪に貼
付することにより密封包::シ法の効果が期待でさ、ま
た治療時の作業性に優れている等、従来の外用剤に比べ
優れた点が多い。しかしながら、これらのテープ剤を患
部に貼付した場合、粘着剤自体に起因する接触皮膚炎や
皮表細菌等に基づく毛色炎や汗腺の刺激による皮膚炎症
などの発生も希ではない。また、これらのテープ剤は、
剥離時に於ける患部の損傷や角質の剥離等により連用し
て貼付するのが困難であるばかりでなく、症状を悪化さ
せるなどいまだ不充分なものであると言わざるを得ない
。However, these preparations have some side effects and are inconvenient to use.For example, oral preparations pose a risk of forgetting to take doses or overdosing, while injection preparations cause great pain and stress during administration, and may be difficult for individuals to administer. Difficult to administer. With external preparations such as ointments and lotions, it is difficult to administer a fixed amount to clothing, as well as to θ dyes. In addition, many cases of skin phlegm are accompanied by a similar feeling, so it is possible that you have an urge to give physical stimulation, and this stimulation may worsen the symptoms. That's a childish thing to say. In order to improve the above-mentioned drawbacks, a pressure-sensitive sheet made of Daigong rubber or an acrylic ester-acrylic acid copolymer has been developed. A tape preparation containing a steroid agent as a premedication has been developed. These tapes have many advantages over conventional topical preparations, such as the effectiveness of the hermetically sealed package that can be applied to a small and distorted area, as well as superior workability during treatment. . However, when these tapes are applied to the affected area, it is not uncommon for contact dermatitis caused by the adhesive itself, folliculitis caused by bacteria on the skin surface, and skin inflammation due to stimulation of sweat glands to occur. In addition, these tape agents are
It must be said that it is still unsatisfactory, as it is not only difficult to apply continuously due to damage to the affected area and exfoliation of the dead skin during peeling, but also worsens the symptoms.
発明の目的
そこで本発明者等は、これらのテープ剤等が有する欠点
を改良する為に鋭意研究の結果、水溶性高分子、水、保
水剤を必須成分とする粘着性基剤に、生薬成分としてス
テロイド剤(デブロドンプロピオネートを除く)を配合
させ、この基剤を柔軟な支持体上に展延塗布することに
より、従来のテープ剤におけるような欠点のない優れた
貼付剤が得られることを見い出し、本発明を完成するに
至った。すなわち、本発明は、水溶性高分子、水、保水
剤を必須成分とずろ粘着性ゲル基剤中にステロイド剤(
デブロドンブロピオネートを除く)を配合した外用貼付
剤を提供するものである。Purpose of the Invention Therefore, in order to improve the drawbacks of these tape preparations, the present inventors have conducted extensive research and have found that the present inventors have added herbal drug ingredients to an adhesive base containing a water-soluble polymer, water, and a water-retaining agent as essential ingredients. By incorporating a steroid agent (excluding debrodone propionate) as a base and spreading and coating this base on a flexible support, an excellent patch without the drawbacks of conventional tapes can be obtained. This discovery led to the completion of the present invention. That is, the present invention contains a water-soluble polymer, water, and a water-retaining agent as essential ingredients, and a steroid agent (
The present invention provides an external patch containing a combination of debrodone propionate (excluding debrodone propionate).
発明の+l14成よ5よび効果
本発明の外用貼付剤に用いられる水溶性高分子としては
、ゼラチン、寒天、アルギン酸、マンナン、カルボキシ
メヂルセルロース、メヂルセルロース、ポリビニルアル
コール、ポリアクリル酸、アラビアガム等が挙げられ、
またこれらの金属塩及び、有機、無機の架橋剤により架
橋させたしの等が用いられる。これらの水溶性高分子は
、本粘着性ゲル基剤中に使用される他の原料の物性によ
り、一種または二種以上を組み合わせて用いられ、本ゲ
ル基剤中の配合量は0.1〜30w/w%、好ましくは
0.5〜+5w/w%である。+l14 Aspects and Effects of the Invention Water-soluble polymers used in the topical patch of the present invention include gelatin, agar, alginic acid, mannan, carboxymethyl cellulose, medyl cellulose, polyvinyl alcohol, polyacrylic acid, and gum arabic. etc. are mentioned,
In addition, metal salts of these and materials crosslinked with organic or inorganic crosslinking agents are used. These water-soluble polymers may be used singly or in combination of two or more depending on the physical properties of other raw materials used in the present adhesive gel base, and the blending amount in the present gel base may range from 0.1 to 30 w/w%, preferably 0.5 to +5 w/w%.
つぎに保水剤としては、ポリエチレングリコール、グリ
セリン、ソルビトール、マルヂトール、プロピレングリ
コール、1.3−ブタンジオール等の多価アルコールが
挙げられ、その一種または二種以上を組み合わせて用い
られ、本ゲル基剤中の配合量は5〜60w/w%、好ま
しくはIO〜5Ow/w%である。また、デンプン−ア
クリロニトリルグラフト体、デンプン−アクリル酸グラ
フト体、デンプン−スチレンスルホン酸グラフト体、デ
ンプン−ビニルスルホン酸グラフト体、セルロース−ア
クリロニトリルグラフト体、セルロースースチレンスル
ホン酸グラフト体、カルホキジメチルセルロース架橋体
、ボリヒニルアルコール架橋体、アクリル酸−酢酸ヒニ
ルケン化物、ポリアクリル酸塩架橋体、ポリアクリロニ
トリル系重合体ケン化物、ポリエチレングリコールジア
クリレート架橋体等の高吸水性高分子を用いることらで
き、これらの場合は、0.01−10.0w/w%、好
ましくは005〜7.Ow/w%の範囲て用いられろ。Next, examples of water retention agents include polyhydric alcohols such as polyethylene glycol, glycerin, sorbitol, marditol, propylene glycol, and 1,3-butanediol, which may be used alone or in combination of two or more. The blending amount is 5 to 60 w/w%, preferably IO to 5Ow/w%. In addition, starch-acrylonitrile graft, starch-acrylic acid graft, starch-styrene sulfonic acid graft, starch-vinyl sulfonic acid graft, cellulose-acrylonitrile graft, cellulose-styrene sulfonic acid graft, carboxydimethyl cellulose cross-linked It is possible to use super water-absorbing polymers such as polyhinyl alcohol crosslinked products, saponified acrylic acid-hinyl acetate products, polyacrylate crosslinked products, saponified polyacrylonitrile polymers, and polyethylene glycol diacrylate crosslinked products, In these cases, the content is 0.01-10.0 w/w%, preferably 0.05-7. It should be used within the range of Ow/w%.
本発明で用いられる粘着性ゲル基剤は水分を含むことが
特徴の−ってあり、それによって活性成分であるステロ
イド剤の吸収を向上させることかでさる。その水分の含
有量は、lO〜70w/w%、好ましくは20〜50w
/w%である。The adhesive gel base used in the present invention is characterized by containing water, which improves the absorption of the active ingredient, the steroid. Its moisture content is lO~70w/w%, preferably 20~50w
/w%.
次に、本外用貼付剤の生薬成分である。ステロイド剤と
しては、例えばフルオロメロンアでトニド、トリアムン
ノロンアセトニド、デキザメタゾン、メヂルブレドニゾ
ロン、ブレドニソ殆ン、ヒドロコルデシン、バラメタシ
ン、ベタメタシン、りん酸ベタメタシンナトリウム、酢
酸デキサメタシン、酢酸コルチゾン、酢酸ヒドロコルチ
ゾン、酢酸メヂルプレドニゾロン、プロピオン酸クロベ
タゾール、酪酸ヒドロコルチゾン、フルオシノニト、フ
ルオロメトロン、フルドロキンコルチド、ピバル酸フル
メタシン1.プロピオン酸ベクロメタゾン、吉草酸ベタ
メタシン、酢酸メチルブレドニン等が挙げられ、これら
のステロイド剤の粘着性ゲル基剤中の配合量は0.00
1〜IW/W%、好ましくは0.005〜0.5w/w
%、更に好ましくは0.01〜0.25w/w%である
。Next is the herbal medicine ingredient of this topical patch. Examples of steroids include fluoromelonatonide, triamnolone acetonide, dexamethasone, medilbrednisolone, bredonisoline, hydrocordesin, valamethacin, betamethacin, betamethacin sodium phosphate, dexamethacin acetate, cortisone acetate, and acetic acid. Hydrocortisone, medylprednisolone acetate, clobetasol propionate, hydrocortisone butyrate, fluocinonite, fluorometholone, fludroquincortide, flumethacin pivalate 1. Examples include beclomethasone propionate, betamethacin valerate, methylbredonin acetate, and the amount of these steroids in the adhesive gel base is 0.00.
1 to IW/W%, preferably 0.005 to 0.5 w/w
%, more preferably 0.01 to 0.25 w/w%.
また、上記ステロイド剤の水に対する溶解性や分散性を
上げる為、クロタミトン、ベンノルアルコール、ミリス
チン酸イソプロピル、エチレングリコール、セパノル酸
ジエチルー2−エチル−5−ピロリドン等のオイル成分
や界面活性剤等を配合することらできる。In order to increase the solubility and dispersibility of the steroids in water, oil components such as crotamiton, bennoral alcohol, isopropyl myristate, ethylene glycol, diethyl-2-ethyl-5-pyrrolidone sepanolate, and surfactants are added. It can be done by blending.
更に従来公知の安定化剤、酸化防止剤、pI−(Q整剤
、無機充填剤等を所望により添加することもできる。Furthermore, conventionally known stabilizers, antioxidants, pI-(Q adjusters, inorganic fillers, etc.) may be added as desired.
次に、本発明に使用される支持体としては人体の動作に
追随するような柔軟な支持体が望ましく、各種の織布、
不織布、ネル等を挙げることができる。また、本発明の
外用貼付剤は、粘着性ゲル基剤層が連続相であるため、
密封包帯法の効果を期待することができるが、より強力
な密封包帯法の効果を所望の場合には前記の支持体に、
エヂレンビニルアセテート、ポリエチレン、ポリ塩化ビ
ニル、ポリウレタン等をラミネートした支持体を用いる
ことらできる。Next, the support used in the present invention is preferably a flexible support that follows the movements of the human body, such as various woven fabrics,
Examples include non-woven fabrics and flannel. In addition, in the external patch of the present invention, since the adhesive gel base layer is a continuous phase,
The effect of the occlusive bandage method can be expected, but if a stronger effect of the occlusive bandage method is desired, the above-mentioned support may be
A support laminated with ethylene vinyl acetate, polyethylene, polyvinyl chloride, polyurethane, etc. can be used.
本発明は、従来公知のテープ剤に比べ皮膚炎症などの副
作用の発生が少ないばかりでなく、剥離時に於ける患部
の損傷や角質の剥離などが少ないため、連用して貼付す
ることが可能である。また本外用貼付剤を皮膚疾患部に
適用した場合、従来のテープ剤と同様に密封包帯法の効
果を期待できるばかりでなく、本外用貼付剤に含まれる
水分により角質層の積極的な水和か起こり、その結里生
薬成分であるステロイド剤の吸収が向上し、より優れた
治療効果を現わすことができる。The present invention not only causes less side effects such as skin inflammation than conventionally known tape preparations, but also causes less damage to the affected area and less exfoliation of dead skin when peeling off, so it can be applied repeatedly. . In addition, when this topical patch is applied to a skin disease area, it can not only be expected to have the same occlusive dressing effect as conventional tapes, but also actively hydrate the stratum corneum due to the water contained in this topical patch. As a result, the absorption of the steroid drug, which is a component of the medicinal herbal medicine, is improved, and better therapeutic effects can be achieved.
さらに、外用貼付剤を皮膚疾患部に適用したときに薬効
が発現するためには、薬剤が基剤から遊離し、皮膚へ移
行することが必要になるが、これには薬剤と基剤の間の
親和性が関与し、薬効に影響を及ぼすと考えられる。こ
の親和性に影響を及ぼす要因としては基剤あるいは基剤
成分中の薬剤の溶解度、拡散係数、熱力学的活性等が挙
げられるが、本外用貼付剤は基剤成分の組み合わせ等に
よりこれらの要因の制御が可能であるので、それぞれの
薬剤の至適濃度の設定が可能となり、他の製剤に比べて
優れた治療効果を得ることができる。Furthermore, in order for a topical patch to exert its medicinal effect when applied to a skin disease area, it is necessary for the drug to be released from the base and migrate to the skin; This is thought to be related to the affinity of Factors that affect this affinity include the solubility, diffusion coefficient, and thermodynamic activity of the drug in the base or base components, but this topical patch has a combination of base components that can affect these factors. Since it is possible to control the concentration of each drug, it is possible to set the optimal concentration of each drug, and it is possible to obtain superior therapeutic effects compared to other preparations.
以下に実施例、および実験例を挙げて本発明をさらに詳
しく説明する。実施例中の「部」は重量部を意味する。The present invention will be explained in more detail by giving examples and experimental examples below. "Parts" in the examples mean parts by weight.
実施例I
水31部、ゼラチン5.0部、パラオキシ安い、香酸メ
チル0.1部、クエン酸0.2部、トリアムンノロンア
セトニド0.1部、クロタミトン10部、ソルビトール
20部、グリセリン30部およびポリアクリル酸4.0
部をニーダ−中で加温しながら攪拌して溶解した後、こ
れに水8部に硫酸アルミニウムカリウム0.5部を溶解
した溶液を加え、充分に攪拌して粘着性ゲル基剤を得ろ
。この粘着性ゲル基剤を常法により剥離紙上に200g
/m’になるように展延塗布し、更にポリウレタンをラ
ミネートしたレーヨン製の不織布に転写し、所望の大き
さに裁断してトリアムンノロンアセトニドを20部g/
cm’含有する外用貼付剤を得る。Example I 31 parts of water, 5.0 parts of gelatin, paraoxyl, 0.1 part of methyl fragrant, 0.2 parts of citric acid, 0.1 part of triamunolone acetonide, 10 parts of crotamiton, 20 parts of sorbitol, glycerin 30 parts and polyacrylic acid 4.0
After stirring and dissolving a portion while heating in a kneader, a solution of 0.5 part of potassium aluminum sulfate dissolved in 8 parts of water was added to this, and the mixture was sufficiently stirred to obtain a sticky gel base. Apply 200g of this adhesive gel base onto release paper using a conventional method.
/m', then transferred to a polyurethane-laminated nonwoven fabric made of rayon, cut to desired size, and applied 20 parts g/m' of triamunolone acetonide.
An external patch containing cm' is obtained.
実施例2
水25部、ポリアクリル酸10部、亜鉛華5部、ポリビ
ニルアルコール6部、ベンンルアルコール3.0部、ヒ
ドロコルデシン10部、バラオキシ安息香酸プロピル0
.1部、カルボキシメチルセルロースナトリウム塩8.
0部、グリセリン20部およびソルビトール20部を実
施例Iと同様にしてニーグー中で溶解後、水2部5部に
ジヒドロキンアルミニウムアミノアセテート0.2部を
溶解した溶液を加え、充分に攪拌して粘着性ゲル基剤を
得る。この基剤から、実施例Iと同様にして、ヒドロコ
ルチゾンを200μg/cm’含有する外用貼付剤を得
る。Example 2 25 parts of water, 10 parts of polyacrylic acid, 5 parts of zinc white, 6 parts of polyvinyl alcohol, 3.0 parts of benzyl alcohol, 10 parts of hydrocordesin, 0 parts of propyl roseoxybenzoate
.. 1 part, carboxymethylcellulose sodium salt8.
After dissolving 0 parts of glycerin, 20 parts of glycerin, and 20 parts of sorbitol in Nigu in the same manner as in Example I, a solution of 0.2 parts of dihydroquine aluminum aminoacetate dissolved in 2 parts and 5 parts of water was added, and the mixture was thoroughly stirred. to obtain a sticky gel base. From this base, an external patch containing 200 μg/cm' of hydrocortisone is obtained in the same manner as in Example I.
四員各立
酢酸デキサメタシンを0.1部用いる以外は実施例1と
同様にして、酢酸デキサメタシンを20部g/cm2含
何する外用貼付剤を得る。An external patch containing 20 parts g/cm2 of dexamethacin acetate is obtained in the same manner as in Example 1 except that 0.1 part of each four-membered dexamethacin acetate is used.
犬鬼桝エ
メヂルブレドニゾロンを0.25部用いる以外は実施例
1と同様にして、メヂルブレトニゾロンを50部g/c
m2含汀する外用貼付剤を得る。50 parts g/c of medylbretonisolone was prepared in the same manner as in Example 1 except that 0.25 parts of medylbretonisolone was used.
An external patch containing m2 is obtained.
実施例5
プレドニゾロンを05部用いる以外は、実施例1と同様
にして、プレドニゾロンを100μg/cm’含有する
外用貼付剤を得る。Example 5 An external patch containing 100 μg/cm' of prednisolone is obtained in the same manner as in Example 1, except that 0.5 parts of prednisolone is used.
実施例(
フルオシノロンアセトニドをo 、 o =i部用いる
以外は実施例1と同様にして、フルオノノ〔7ンアセト
ニドを8μg/cm”含有する外用貼付剤を得る。Example (An external patch containing 8 μg/cm” of fluoronono[7-acetonide] is obtained in the same manner as in Example 1 except that o , o = i parts of fluocinolone acetonide are used.
火験仮↓
皮膚蒼白化試験により、前記実施例1〜6の貼付剤、な
らびにフルドキンコルチド4μg/am’、フルオシノ
ロンアセトニド8μg/cm”および吉草酸ベタメタシ
ン6μg/am’をそれぞれ含有するアクリル系帖着剤
の市販テープ剤の効力を比較した。Fire Test Temporary ↓ According to the skin pallor test, the patches of Examples 1 to 6, and each containing fludoquincortide 4 μg/am', fluocinolone acetonide 8 μg/cm", and betamethacin valerate 6 μg/am' The effectiveness of commercially available acrylic adhesive tapes was compared.
これらのステロイド類含行貼付剤及び市販テープ剤をそ
れぞれ直径10mmの円状に打ち抜いて供試試料とし、
これらの試料を健康成人男子10名の中背部に無作為に
割り付け、貼付した。貼付時間は、30分、1時間、2
時間、4時間とし、剥離して2時間および4時間後に皮
膚蒼白化を判定した。Each of these steroid-containing patches and commercially available tapes was punched out into a circular shape with a diameter of 10 mm and used as a test sample.
These samples were randomly assigned and applied to the middle backs of 10 healthy male adults. Pasting time is 30 minutes, 1 hour, 2
The skin pallor was determined at 2 and 4 hours after peeling.
結果を第1表〜第4表に示す。第1表および第2表は剥
離2時間後に測定した結果を示し、第1表は試験を行な
った10名のうち陽性を示した人数を、第2表は凝陽性
または陽性を示した人数を表わす。第3表および第4表
は剥離4時間後に測定した結果を示し、第3表は10名
中、陽性を示した人数を、第4表は凝陽性または陽性を
示した人数を表わす。The results are shown in Tables 1 to 4. Tables 1 and 2 show the results measured 2 hours after the peeling.Table 1 shows the number of people who tested positive out of the 10 people who tested, and Table 2 shows the number of people who tested positive or who tested positive. represent Tables 3 and 4 show the results of measurements taken 4 hours after stripping, Table 3 shows the number of people who tested positive out of 10, and Table 4 shows the number of people who tested positive or clotted.
(以下余白)(Margin below)
Claims (1)
性ゲル基剤中にステロイド剤(デプロドンプロピオネー
トを除く)を配合した外用貼付剤。(1) An external patch containing a steroid agent (excluding deprodone propionate) in an adhesive gel base containing a water-soluble polymer, water, and a water-retaining agent as essential ingredients.
Priority Applications (8)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP61195935A JPS6351330A (en) | 1986-08-20 | 1986-08-20 | External plaster containing steroidal agent |
US07/639,758 US5082663A (en) | 1986-08-20 | 1987-08-20 | External adhesive preparation containing steroids |
DE8787905474T DE3775208D1 (en) | 1986-08-20 | 1987-08-20 | PREPARATION OF STEROIDS FOR EXTERNAL USE. |
EP87905474A EP0280737B1 (en) | 1986-08-20 | 1987-08-20 | Steroidal drug-containing preparation for external use |
PCT/JP1987/000618 WO1988001170A1 (en) | 1986-08-20 | 1987-08-20 | Steroidal drug-containing preparation for external use |
KR1019880700403A KR950013750B1 (en) | 1986-08-20 | 1987-08-20 | External adhesive preparation containing steroids |
SG29994A SG29994G (en) | 1986-08-20 | 1994-02-24 | Steroidal drug-containing preparation for external use |
HK77194A HK77194A (en) | 1986-08-20 | 1994-08-04 | Steroidal drug-containing preparation for external use |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP61195935A JPS6351330A (en) | 1986-08-20 | 1986-08-20 | External plaster containing steroidal agent |
Publications (1)
Publication Number | Publication Date |
---|---|
JPS6351330A true JPS6351330A (en) | 1988-03-04 |
Family
ID=16349418
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP61195935A Pending JPS6351330A (en) | 1986-08-20 | 1986-08-20 | External plaster containing steroidal agent |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS6351330A (en) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2000002563A1 (en) * | 1998-07-10 | 2000-01-20 | Hisamitsu Pharmaceutical Co., Inc. | Steroid-containing cataplasms and process for producing the same |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS6066710A (en) * | 1983-09-21 | 1985-04-16 | 前田 孝憲 | Furniture-like bar refregarator |
-
1986
- 1986-08-20 JP JP61195935A patent/JPS6351330A/en active Pending
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS6066710A (en) * | 1983-09-21 | 1985-04-16 | 前田 孝憲 | Furniture-like bar refregarator |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2000002563A1 (en) * | 1998-07-10 | 2000-01-20 | Hisamitsu Pharmaceutical Co., Inc. | Steroid-containing cataplasms and process for producing the same |
US6432431B1 (en) | 1998-07-10 | 2002-08-13 | Hisamitsu Pharmaceutical Co., Inc. | Steroid-containing cataplasms and process for producing the same |
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