JPH01299218A - Drug preparation for transcutaneous administration - Google Patents
Drug preparation for transcutaneous administrationInfo
- Publication number
- JPH01299218A JPH01299218A JP13103988A JP13103988A JPH01299218A JP H01299218 A JPH01299218 A JP H01299218A JP 13103988 A JP13103988 A JP 13103988A JP 13103988 A JP13103988 A JP 13103988A JP H01299218 A JPH01299218 A JP H01299218A
- Authority
- JP
- Japan
- Prior art keywords
- steroidal anti
- preparation
- inflammatory agent
- drug
- transcutaneous administration
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 238000002360 preparation method Methods 0.000 title claims abstract description 18
- 229940079593 drug Drugs 0.000 title abstract description 11
- 239000003814 drug Substances 0.000 title abstract description 11
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims abstract description 16
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims abstract description 15
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 9
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 abstract description 7
- 229960000991 ketoprofen Drugs 0.000 abstract description 7
- 239000000853 adhesive Substances 0.000 abstract description 5
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 abstract description 2
- 238000010521 absorption reaction Methods 0.000 abstract description 2
- LPEPZBJOKDYZAD-UHFFFAOYSA-N flufenamic acid Chemical compound OC(=O)C1=CC=CC=C1NC1=CC=CC(C(F)(F)F)=C1 LPEPZBJOKDYZAD-UHFFFAOYSA-N 0.000 abstract description 2
- 229960004369 flufenamic acid Drugs 0.000 abstract description 2
- 229960001680 ibuprofen Drugs 0.000 abstract description 2
- 238000013329 compounding Methods 0.000 abstract 1
- 206010040880 Skin irritation Diseases 0.000 description 6
- 230000036556 skin irritation Effects 0.000 description 6
- 231100000475 skin irritation Toxicity 0.000 description 6
- -1 antispasmodics Substances 0.000 description 5
- 229920005989 resin Polymers 0.000 description 5
- 239000011347 resin Substances 0.000 description 5
- 230000001070 adhesive effect Effects 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 229920001577 copolymer Polymers 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- 239000004744 fabric Substances 0.000 description 3
- 239000002480 mineral oil Substances 0.000 description 3
- 235000010446 mineral oil Nutrition 0.000 description 3
- 239000003208 petroleum Substances 0.000 description 3
- VSKJLJHPAFKHBX-UHFFFAOYSA-N 2-methylbuta-1,3-diene;styrene Chemical compound CC(=C)C=C.C=CC1=CC=CC=C1.C=CC1=CC=CC=C1 VSKJLJHPAFKHBX-UHFFFAOYSA-N 0.000 description 2
- RSWGJHLUYNHPMX-UHFFFAOYSA-N Abietic-Saeure Natural products C12CCC(C(C)C)=CC2=CCC2C1(C)CCCC2(C)C(O)=O RSWGJHLUYNHPMX-UHFFFAOYSA-N 0.000 description 2
- 244000043261 Hevea brasiliensis Species 0.000 description 2
- 239000004698 Polyethylene Substances 0.000 description 2
- KHPCPRHQVVSZAH-HUOMCSJISA-N Rosin Natural products O(C/C=C/c1ccccc1)[C@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 KHPCPRHQVVSZAH-HUOMCSJISA-N 0.000 description 2
- BZHJMEDXRYGGRV-UHFFFAOYSA-N Vinyl chloride Chemical compound ClC=C BZHJMEDXRYGGRV-UHFFFAOYSA-N 0.000 description 2
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 2
- NIXOWILDQLNWCW-UHFFFAOYSA-N acrylic acid group Chemical group C(C=C)(=O)O NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 2
- 238000011156 evaluation Methods 0.000 description 2
- 229960002390 flurbiprofen Drugs 0.000 description 2
- SYTBZMRGLBWNTM-UHFFFAOYSA-N flurbiprofen Chemical compound FC1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC=C1 SYTBZMRGLBWNTM-UHFFFAOYSA-N 0.000 description 2
- CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 description 2
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 229920003052 natural elastomer Polymers 0.000 description 2
- 229920001194 natural rubber Polymers 0.000 description 2
- 239000004745 nonwoven fabric Substances 0.000 description 2
- 239000003921 oil Substances 0.000 description 2
- 239000000123 paper Substances 0.000 description 2
- 229920006267 polyester film Polymers 0.000 description 2
- 229920000573 polyethylene Polymers 0.000 description 2
- 229920000346 polystyrene-polyisoprene block-polystyrene Polymers 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 2
- 229940125723 sedative agent Drugs 0.000 description 2
- 239000000932 sedative agent Substances 0.000 description 2
- 230000035807 sensation Effects 0.000 description 2
- 239000000021 stimulant Substances 0.000 description 2
- KHPCPRHQVVSZAH-UHFFFAOYSA-N trans-cinnamyl beta-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OCC=CC1=CC=CC=C1 KHPCPRHQVVSZAH-UHFFFAOYSA-N 0.000 description 2
- NOOLISFMXDJSKH-KXUCPTDWSA-N (-)-Menthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@H]1O NOOLISFMXDJSKH-KXUCPTDWSA-N 0.000 description 1
- RDJGLLICXDHJDY-NSHDSACASA-N (2s)-2-(3-phenoxyphenyl)propanoic acid Chemical compound OC(=O)[C@@H](C)C1=CC=CC(OC=2C=CC=CC=2)=C1 RDJGLLICXDHJDY-NSHDSACASA-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
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 description 1
- GOXQRTZXKQZDDN-UHFFFAOYSA-N 2-Ethylhexyl acrylate Chemical compound CCCCC(CC)COC(=O)C=C GOXQRTZXKQZDDN-UHFFFAOYSA-N 0.000 description 1
- 229930000680 A04AD01 - Scopolamine Natural products 0.000 description 1
- 241000723346 Cinnamomum camphora Species 0.000 description 1
- GJSURZIOUXUGAL-UHFFFAOYSA-N Clonidine Chemical compound ClC1=CC=CC(Cl)=C1NC1=NCCN1 GJSURZIOUXUGAL-UHFFFAOYSA-N 0.000 description 1
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 1
- JOYRKODLDBILNP-UHFFFAOYSA-N Ethyl urethane Chemical compound CCOC(N)=O JOYRKODLDBILNP-UHFFFAOYSA-N 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- STECJAGHUSJQJN-GAUPFVANSA-N Hyoscine Natural products C1([C@H](CO)C(=O)OC2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-GAUPFVANSA-N 0.000 description 1
- ZCVMWBYGMWKGHF-UHFFFAOYSA-N Ketotifene Chemical compound C1CN(C)CCC1=C1C2=CC=CC=C2CC(=O)C2=C1C=CS2 ZCVMWBYGMWKGHF-UHFFFAOYSA-N 0.000 description 1
- STECJAGHUSJQJN-UHFFFAOYSA-N N-Methyl-scopolamin Natural products C1C(C2C3O2)N(C)C3CC1OC(=O)C(CO)C1=CC=CC=C1 STECJAGHUSJQJN-UHFFFAOYSA-N 0.000 description 1
- CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 description 1
- 239000004677 Nylon Substances 0.000 description 1
- 239000005062 Polybutadiene Substances 0.000 description 1
- 229920002367 Polyisobutene Polymers 0.000 description 1
- 239000004743 Polypropylene Substances 0.000 description 1
- TVQZAMVBTVNYLA-UHFFFAOYSA-N Pranoprofen Chemical compound C1=CC=C2CC3=CC(C(C(O)=O)C)=CC=C3OC2=N1 TVQZAMVBTVNYLA-UHFFFAOYSA-N 0.000 description 1
- QYKIQEUNHZKYBP-UHFFFAOYSA-N Vinyl ether Chemical compound C=COC=C QYKIQEUNHZKYBP-UHFFFAOYSA-N 0.000 description 1
- 239000002998 adhesive polymer Substances 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 229940124599 anti-inflammatory drug Drugs 0.000 description 1
- 230000002921 anti-spasmodic effect Effects 0.000 description 1
- 239000001961 anticonvulsive agent Substances 0.000 description 1
- 229940125715 antihistaminic agent Drugs 0.000 description 1
- 239000000739 antihistaminic agent Substances 0.000 description 1
- 229940030600 antihypertensive agent Drugs 0.000 description 1
- 239000002220 antihypertensive agent Substances 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 239000003907 antipyretic analgesic agent Substances 0.000 description 1
- 229940124575 antispasmodic agent Drugs 0.000 description 1
- 239000003434 antitussive agent Substances 0.000 description 1
- 229940124584 antitussives Drugs 0.000 description 1
- 230000006793 arrhythmia Effects 0.000 description 1
- 206010003119 arrhythmia Diseases 0.000 description 1
- 244000309464 bull Species 0.000 description 1
- 229960000846 camphor Drugs 0.000 description 1
- 229930008380 camphor Natural products 0.000 description 1
- 230000000747 cardiac effect Effects 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000012829 chemotherapy agent Substances 0.000 description 1
- 229960002896 clonidine Drugs 0.000 description 1
- 239000002131 composite material Substances 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 230000001054 cortical effect Effects 0.000 description 1
- 239000002934 diuretic Substances 0.000 description 1
- 229940030606 diuretics Drugs 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 239000005038 ethylene vinyl acetate Substances 0.000 description 1
- 229960001419 fenoprofen Drugs 0.000 description 1
- 239000006260 foam 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
- 229940125697 hormonal agent Drugs 0.000 description 1
- 230000000147 hypnotic effect Effects 0.000 description 1
- 229960000905 indomethacin Drugs 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 229960004958 ketotifen Drugs 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 229960001047 methyl salicylate Drugs 0.000 description 1
- 229960002009 naproxen Drugs 0.000 description 1
- CMWTZPSULFXXJA-VIFPVBQESA-N naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 description 1
- 229920001778 nylon Polymers 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 230000001766 physiological effect Effects 0.000 description 1
- 239000002985 plastic film Substances 0.000 description 1
- 229920006255 plastic film Polymers 0.000 description 1
- 229920001200 poly(ethylene-vinyl acetate) Polymers 0.000 description 1
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 description 1
- 229920002857 polybutadiene Polymers 0.000 description 1
- 229920001083 polybutene Polymers 0.000 description 1
- 229920000728 polyester Polymers 0.000 description 1
- 229920001155 polypropylene Polymers 0.000 description 1
- 229920001296 polysiloxane 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
- 229960003101 pranoprofen Drugs 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- STECJAGHUSJQJN-FWXGHANASA-N scopolamine Chemical compound C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-FWXGHANASA-N 0.000 description 1
- 229960002646 scopolamine Drugs 0.000 description 1
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 description 1
- 230000003637 steroidlike Effects 0.000 description 1
- 229920006132 styrene block copolymer Polymers 0.000 description 1
- 230000035900 sweating Effects 0.000 description 1
- 229940124549 vasodilator Drugs 0.000 description 1
- 239000003071 vasodilator agent Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
Abstract
Description
【発明の詳細な説明】
〔産業上の利用分野〕
本発明は、経皮投与製剤において少量の非ステロイド抗
炎症剤を配合することにより、気触れを防止することに
ある。DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The purpose of the present invention is to prevent skin irritation by incorporating a small amount of a non-steroidal anti-inflammatory agent into a transdermal preparation.
従来、経皮より薬物を投与する手段として、粘着性高分
子に薬物を含有させ柔軟性のある布、不織布、各種プラ
スチックフィルムなどの担持体上に直接あるいは間接的
に展延したプラスター剤、パップ剤、テープ剤等が用い
られてきたが、剥離時の毛の引張り、角質の剥離等の物
理的作用、長時間貼付によるムレ、発汗等の生理的作用
による発赤、気触れ等の副作用の発現が問題とされてい
た。Traditionally, as a means of transdermally administering drugs, plasters and poultices have been used, which are adhesive polymers containing drugs and spread directly or indirectly onto carriers such as flexible cloth, nonwoven fabrics, and various plastic films. Agents, tapes, etc. have been used, but they can cause side effects such as physical effects such as pulling hair and exfoliating dead skin when peeling, stuffiness due to long-term application, and physiological effects such as sweating, such as redness and skin irritation. was considered a problem.
例えば、特開昭５８−４７２１号、特開昭６０−５１１
４号、特開昭６０−５６９１１号、特開昭６０−２３３
１２号等には気触れ防止あるいは、皮膚刺激低減のため
、薬物配合が示されている。For example, JP-A-58-4721, JP-A-60-511
No. 4, JP-A-60-56911, JP-A-60-233
No. 12 etc. contain drugs to prevent exposure or reduce skin irritation.
しかし、いずれの場合においても、実用性に問題があり
、又その効果も不充分なものであるため、更に改良が待
たれているのが現状である。However, in any case, there are problems in practicality and the effects are insufficient, so further improvements are currently awaited.
本発明者らは、上記技術状況に鑑み、従来技術における
問題点を解決した経皮用貼付剤の開発を目的として鋭意
研究を重ねた結果、経皮投与製剤において、その製剤中
に非ステロイド抗炎症剤を配合することにより、気触れ
を防止した経皮投与製剤を提供するにいたったものであ
る。In view of the above-mentioned technical situation, the present inventors have conducted intensive research with the aim of developing a transdermal patch that solves the problems in the conventional technology. By incorporating an inflammatory agent, we have now provided a transdermal preparation that prevents skin contact.
次に本発明の構成成分について説明する。Next, the constituent components of the present invention will be explained.
気触れ防止剤として配合される非ステロイド抗炎症剤と
しては、公知のものが広く使用でき、例えばイブプロフ
ェン、ケトプロフェン、フルルビプロフェン、フルフェ
ナミン酸、フェノプロフェン、ナプロキセン、フエンブ
フエン、及びそのエステル誘導体等であり、その配合量
としては、０、００１〜２■／−であり、好ましくは０
．００５〜１■／−であり、更に好ましくは０．Ｏ１〜
０．５■／ｃｄである。A wide variety of known non-steroidal anti-inflammatory drugs can be used as non-steroidal anti-inflammatory agents, such as ibuprofen, ketoprofen, flurbiprofen, flufenamic acid, fenoprofen, naproxen, fuenbufuene, and ester derivatives thereof. and its blending amount is 0,001 to 2/-, preferably 0.
．． 005 to 1■/-, more preferably 0. O1～
It is 0.5■/cd.
粘着剤としては、別に制約はなく、常温で粘着性を示す
ものであれば良い。例えばシリコーン系、スチレン−イ
ソプレン−スチレン系、アクリル系、天然ゴム系、ウレ
タン系、ポリイソブチレン系等の油性粘着剤、及びビニ
ルエーテル系、ゼラチン／ポリアクリル酸ソーダ系等の
水性粘着剤等から適時用いることができる。更に従来公
知の粘着付与剤、及び抗酸化剤等を必要に応じて使用で
きうろことはもちろんである。There are no particular restrictions on the adhesive, as long as it exhibits tackiness at room temperature. For example, oil-based adhesives such as silicone-based, styrene-isoprene-styrene-based, acrylic-based, natural rubber-based, urethane-based, polyisobutylene-based, etc., and water-based adhesives such as vinyl ether-based, gelatin/sodium polyacrylate, etc. are used as appropriate. be able to. Furthermore, it goes without saying that conventionally known tackifiers, antioxidants, etc. can be used as needed.
主薬としては、経皮吸収薬物（例えば催眠鎮静剤、抗て
んかん剤、解熱鎮痛消炎剤、興奮剤・覚醒剤、鎮量刑、
精神神経用剤、鎮痙剤、抗ヒスタミン剤、強心剤、不整
脈用剤、利尿剤、血圧降下剤、血管拡張剤、動脈硬化用
剤、鎮咳きょたん剤、ホルモン剤、化学療法剤、抗ガン
剤等）であれば特に限定はなく、これらを０．００１〜
３■／ｄの配合量で用いることができる。Main drugs include transdermal absorption drugs (e.g. hypnotic sedatives, anti-epileptic drugs, antipyretic analgesic anti-inflammatory drugs, stimulants/stimulants, sedatives,
Neuropsychiatric agents, antispasmodics, antihistamines, cardiac inotropes, arrhythmia agents, diuretics, antihypertensive agents, vasodilators, arteriosclerotic agents, antitussive agents, hormonal agents, chemotherapy agents, anticancer agents, etc.) If so, there is no particular limitation, and these can be from 0.001 to
It can be used in a blending amount of 3/d.
支持体としては、伸縮性及び非伸縮性のものが用いられ
、例えばポリエチレン、ポリプロピレン、ポリブタジェ
ン、エチレン酢酸ビニル共重合体、ポリ塩化ビニル、ポ
リエステル、ナイロン、ポリウレタン等のフィルム又は
シート、あるいはこれらの積層体、多孔質体、発泡体、
そして・紙、布、不織布等より選ばれる。Stretchable and non-stretchable supports are used, such as films or sheets of polyethylene, polypropylene, polybutadiene, ethylene vinyl acetate copolymer, polyvinyl chloride, polyester, nylon, polyurethane, or laminates thereof. body, porous body, foam,
-Choose from paper, cloth, non-woven fabric, etc.
以上の如くして得られた本発明の経皮投与製剤は、その
気触れ防止剤としての、非ステロイド抗炎症剤の配合に
より、従来経皮投与製剤に頻発していた気触れの一掃が
図られ、医療上非常に有用なものである。The transdermal preparation of the present invention obtained as described above can eliminate the unpleasant sensations that frequently occur in conventional transdermal preparations by incorporating a non-steroidal anti-inflammatory agent as an agent for preventing unpleasant sensations. It is very useful medically.
以下に、試験例、及び実施例を示し本発明を更に詳しく
説明する。The present invention will be explained in more detail by showing test examples and examples below.
実施例１
アクリル酸−２−エチルへキシル−アクリル酸よりなる
共重合物に、スコポラミンＯ６１■／Ｃ＋４゜非ステロ
イド抗炎症剤としてケトプロフェン０．０３■／ｄにな
るように配合し、アルミニウムが蒸着された塩化ビニル
フィルムに厚さ６０−で展延、本発明の経皮投与製剤と
した。Example 1 A copolymer of 2-ethylhexyl acrylate and acrylic acid was mixed with scopolamine O61/C+4° and ketoprofen as a nonsteroidal anti-inflammatory agent at a concentration of 0.03/d, and aluminum was vapor-deposited. The mixture was spread on a vinyl chloride film with a thickness of 60 mm to obtain a percutaneous administration preparation of the present invention.
実施例２
スチレン−イソプレン−スチレンブロック共重合体／水
添ロジン樹脂／鉱油、４．５ ／ ３ ／ ３の比のも
のに、サリチル酸メチル０．４■／ｃｄ、 ｌ−メント
ール０．５■／−になるように配合し、非ステロイド抗
炎症剤としてフルルビプロフェン０．Ｏ１■／ｃｊ添加
後、厚さ９０−で剥離紙に展延後、塩化ビニルシートで
覆い本発明の経皮投与製剤とした。Example 2 Styrene-isoprene-styrene block copolymer/hydrogenated rosin resin/mineral oil in a ratio of 4.5/3/3, methyl salicylate 0.4/cd, l-menthol 0.5/c. flurbiprofen as a non-steroidal anti-inflammatory agent. After adding O1/cj, the mixture was spread on release paper to a thickness of 90 mm, and then covered with a vinyl chloride sheet to obtain a transdermal preparation of the present invention.
実施例３
スチレン−イソプレン−スチレンブーロック共重合体／
石油系樹脂／鉱油、５／４／３の比のものに、ケトチフ
ェン０．１■／−１非ステロイド抗炎症剤としてケトプ
ロフェン０．０２■／−配合し、厚さ１００−でポリエ
ステルフィルムに展延し本発明の経皮投与製剤とした。Example 3 Styrene-isoprene-styrene bullock copolymer/
Petroleum resin/mineral oil in a ratio of 5/4/3 was mixed with 0.1/- of ketotifen and 0.02/- of ketoprofen as a non-steroidal anti-inflammatory agent, and spread on a polyester film with a thickness of 100 mm. This was then used to form a transdermal preparation of the present invention.
実施例４
天然ゴム／ロジン変性樹脂／ポリブテン／酸化亜鉛、７
７６／２／３の比のものにサリチル酸メ＋）Ｌｔｌ、６
Ｎ／ｄ、 １−／ ７ ）−１ｔｚ１．Ｏｗ／Ｊ、ａ−
カンフル０．３■／−１非ステロイド抗炎症剤としてプ
ラノプロフェン０．０４■／Ｃｌ１１になるように配合
し、厚さ２００μＩで布に展延し、本発明の経皮投与製
剤とした。Example 4 Natural rubber/rosin modified resin/polybutene/zinc oxide, 7
76/2/3 ratio of salicylic acid (meth+) Ltl, 6
N/d, 1-/7)-1tz1. Ow/J, a-
A mixture of camphor 0.3 .mu./-1 and pranoprofen as a non-steroidal anti-inflammatory agent was mixed at a ratio of 0.04 .mu.l/Cl and spread on cloth to a thickness of 200 .mu.I to prepare a transdermal preparation of the present invention.
実施例５
アクリル酸−２−エチルへキシル−酢酸ビニル共重合体
にインドメタシン０．０１■／−１非ステロイド抗炎症
剤としてケトプロフェン０．００６■／−になるように
配合し、厚さ６０μ皇でポリエチレンフィルムに展延し
本発明の経皮投与製剤とした。Example 5 A 2-ethylhexyl acrylate-vinyl acetate copolymer was blended with indomethacin at 0.01 µ/-1 and ketoprofen as a non-steroidal anti-inflammatory agent at 0.006 µ/- in a thickness of 60 μm. The mixture was spread on a polyethylene film to obtain a transdermal preparation of the present invention.
実施例６
スチレン−イソプレン−スチレンブロック共重合体／石
油系樹脂／に油、１１０．６／１の比のものに、クロニ
ジン０．７■／ ｃ４ 、非ステロイド抗炎症剤として
ケトプロフェン０．０２■／ｄ配合し、厚さ１００μ負
でポリエステル−塩化ビニル複合フィルムに展延し本発
明の経皮投与製剤とした。Example 6 Styrene-isoprene-styrene block copolymer/petroleum resin/oil in a ratio of 110.6/1, clonidine 0.7/c4, and ketoprofen 0.02/as a non-steroidal anti-inflammatory agent. /d and spread it on a polyester-vinyl chloride composite film to a thickness of 100 μm to obtain a percutaneous administration preparation of the present invention.
実施例７
スチレン−イソブレン−スチレンプロツク共重合体／石
油系樹脂／鉱油、１ ／ １．２ ／ １．８の比のも
のに、イソソルバイトジニトレート０．６■／ｃＩｉ、
非ステロイド抗炎症剤としてケトプロフェン０．０１５
■／ｃｄ配合し、厚さ１００ｎでポリエステルフィルム
に展延し本発明の経皮投与製剤とした。Example 7 Styrene-isobrene-styrene block copolymer/petroleum resin/mineral oil, ratio of 1/1.2/1.8, isosorbite dinitrate 0.6/cIi,
Ketoprofen 0.015 as a non-steroidal anti-inflammatory agent
(1)/cd was blended and spread on a polyester film to a thickness of 100 nm to obtain a percutaneous administration preparation of the present invention.
試験例１ （皮膚刺激試験）
本発明の実施例！、２，３，４１１．び５を用い、健康
成人男子３０名の背中に４８時間貼付し、剥離後１時間
及び２４時間後にそれぞれ判定し、皮膚刺激具合を観察
した。（参考例として、実施例より、非ステロイド抗炎
症剤をそれぞれ除いたものを用い、参考例１〜５は実施
例１〜５に準じる。Test Example 1 (Skin irritation test) Example of the present invention! , 2,3,411. 5 was applied to the backs of 30 healthy male adults for 48 hours, and evaluations were made 1 hour and 24 hours after removal to observe the degree of skin irritation. (As a reference example, the non-steroidal anti-inflammatory drug was removed from each example, and Reference Examples 1 to 5 were based on Examples 1 to 5.
各試料は直径２０■ｌで打ち抜き、パッチテスト用絆創
膏で押さえた。）結果を表１に示す。Each sample was punched out to a diameter of 20 μl and pressed with a patch test adhesive. ) The results are shown in Table 1.
尚、判定基準としては下記を用い、各点数の総和をボラ
ンティア数で除しＸ１００倍したものを、皮膚刺激指数
として表した。The following criteria were used for the evaluation, and the sum of each score was divided by the number of volunteers and multiplied by X100, which was expressed as a skin irritation index.
判 定 点数
変化なし Ｏ
微弱な変化 ± ０．５
明瞭な変化 ＋ １．０
重篤な気触れ 妊 ２．０
表１
以上の試験結果より、本発明は非ステロイド剤を少量含
有させることにより顕著な皮層刺激抑制作用を示した。Judgment No change in score O Slight change ± 0.5 Clear change + 1.0 Severe feeling Pregnancy 2.0 Table 1 From the above test results, the present invention shows that it is noticeable by containing a small amount of non-steroidal drug. It exhibited a significant inhibitory effect on cortical irritation.
手続補正書、。発、
１、事件の表示
昭和６３年 特許願第２３１０３９号
２、発明の名称 経皮投与製剤３、補正をする
者
４、補正命令の日付
５、補正の対象
明細書中、「３、発明の詳細な説明」の欄（１） 明
細書中、「３、発明の詳細な説明」の欄の第１真下から
第４行目の「気触れ」を「気触れ（カブレ）」と訂正す
る。Procedural Amendment,. 1. Indication of the case 1988 Patent Application No. 231039 2. Title of the invention Transdermal administration preparation 3. Person making the amendment 4. Date of the amendment order 5. In the specification subject to the amendment, "3. ``Detailed Description'' Column (1) In the specification, ``Feelings'' in the fourth line from the first bottom of the ``3. Detailed Description of the Invention'' column is corrected to ``Feelings''.
（２）同書中、第９真上から第３行目の「微弱な変化」
を「微弱な発赤」と訂正する。(2) “Slight change” in the third line from the top of No. 9 in the same book
was corrected to "slight redness."
（３）同書中、第９真上から第４行目の「明瞭な変化」
を「明瞭な発赤Ｊと訂正する。(3) “Clear change” in the fourth line from the top of No. 9 in the same book
is corrected as ``clear redness J.''
Claims (1)
た経皮投与製剤。 ２、気触れ防止剤として非ステロイド抗炎症剤が０．０
０１〜２ｍｇ／ｃｍ＾２配合された請求項１記載の経皮
投与製剤。[Scope of Claims] 1. A transdermal preparation containing a non-steroidal anti-inflammatory agent as a precautionary agent. 2. 0.0 non-steroidal anti-inflammatory agent as a precautionary agent
2. The transdermal preparation according to claim 1, which contains 01 to 2 mg/cm^2.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP63131039A JPH07106979B2 (en) | 1988-05-27 | 1988-05-27 | Transdermal formulation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP63131039A JPH07106979B2 (en) | 1988-05-27 | 1988-05-27 | Transdermal formulation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPH01299218A true JPH01299218A (en) | 1989-12-04 |
| JPH07106979B2 JPH07106979B2 (en) | 1995-11-15 |
Family
ID=15048592
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP63131039A Expired - Fee Related JPH07106979B2 (en) | 1988-05-27 | 1988-05-27 | Transdermal formulation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPH07106979B2 (en) |
Citations (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5562013A (en) * | 1978-11-02 | 1980-05-10 | Rakuule Yakuhin Hanbai Kk | Aqueous poultice comprising transcutaneous absorbable anti-inflammatory agent |
| JPS5562014A (en) * | 1978-11-02 | 1980-05-10 | Rakuule Yakuhin Hanbai Kk | Aqueous poultice having no skin irritation effect |
| JPS5829706A (en) * | 1981-08-14 | 1983-02-22 | Toko Yakuhin Kogyo Kk | Antiphlogistic and analgesic agent for external use |
| JPS58189115A (en) * | 1982-04-30 | 1983-11-04 | Kowa Co | Drug for external use |
| JPS6023312A (en) * | 1983-07-15 | 1985-02-05 | Nitto Electric Ind Co Ltd | Pharmaceutical preparation |
| JPS60208909A (en) * | 1984-04-02 | 1985-10-21 | Hisamitsu Pharmaceut Co Inc | Anti-inflammatory analgesic agent for external use |
| JPS60252412A (en) * | 1984-05-29 | 1985-12-13 | Nichiban Co Ltd | Therapeutic poultice preparation |
| JPS6112614A (en) * | 1984-06-27 | 1986-01-21 | Lion Corp | Drug for external use |
| JPS61172831A (en) * | 1985-01-26 | 1986-08-04 | Nakanishi Michio | Anti-inflammatory, analgesic drug composition |
| JPS61275212A (en) * | 1985-04-25 | 1986-12-05 | Hisamitsu Pharmaceut Co Inc | Ketoprofen-containing poultice |
| JPS62240614A (en) * | 1986-04-11 | 1987-10-21 | Sekisui Chem Co Ltd | Plaster |
-
1988
- 1988-05-27 JP JP63131039A patent/JPH07106979B2/en not_active Expired - Fee Related
Patent Citations (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5562013A (en) * | 1978-11-02 | 1980-05-10 | Rakuule Yakuhin Hanbai Kk | Aqueous poultice comprising transcutaneous absorbable anti-inflammatory agent |
| JPS5562014A (en) * | 1978-11-02 | 1980-05-10 | Rakuule Yakuhin Hanbai Kk | Aqueous poultice having no skin irritation effect |
| JPS5829706A (en) * | 1981-08-14 | 1983-02-22 | Toko Yakuhin Kogyo Kk | Antiphlogistic and analgesic agent for external use |
| JPS58189115A (en) * | 1982-04-30 | 1983-11-04 | Kowa Co | Drug for external use |
| JPS6023312A (en) * | 1983-07-15 | 1985-02-05 | Nitto Electric Ind Co Ltd | Pharmaceutical preparation |
| JPS60208909A (en) * | 1984-04-02 | 1985-10-21 | Hisamitsu Pharmaceut Co Inc | Anti-inflammatory analgesic agent for external use |
| JPS60252412A (en) * | 1984-05-29 | 1985-12-13 | Nichiban Co Ltd | Therapeutic poultice preparation |
| JPS6112614A (en) * | 1984-06-27 | 1986-01-21 | Lion Corp | Drug for external use |
| JPS61172831A (en) * | 1985-01-26 | 1986-08-04 | Nakanishi Michio | Anti-inflammatory, analgesic drug composition |
| JPS61275212A (en) * | 1985-04-25 | 1986-12-05 | Hisamitsu Pharmaceut Co Inc | Ketoprofen-containing poultice |
| JPS62240614A (en) * | 1986-04-11 | 1987-10-21 | Sekisui Chem Co Ltd | Plaster |
Also Published As
| Publication number | Publication date |
|---|---|
| JPH07106979B2 (en) | 1995-11-15 |
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