JPH10508296A - 経皮薬剤導入用マトリックス - Google Patents
経皮薬剤導入用マトリックスInfo
- Publication number
- JPH10508296A JPH10508296A JP8510432A JP51043296A JPH10508296A JP H10508296 A JPH10508296 A JP H10508296A JP 8510432 A JP8510432 A JP 8510432A JP 51043296 A JP51043296 A JP 51043296A JP H10508296 A JPH10508296 A JP H10508296A
- Authority
- JP
- Japan
- Prior art keywords
- acrylate
- copolymer
- group
- drug delivery
- transdermal drug
- 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.)
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
- A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
- A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
- A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
- A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
- A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
- A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
- A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
- A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
- A61K9/7061—Polyacrylates
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- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08F—MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
- C08F290/00—Macromolecular compounds obtained by polymerising monomers on to polymers modified by introduction of aliphatic unsaturated end or side groups
- C08F290/02—Macromolecular compounds obtained by polymerising monomers on to polymers modified by introduction of aliphatic unsaturated end or side groups on to polymers modified by introduction of unsaturated end groups
- C08F290/04—Polymers provided for in subclasses C08C or C08F
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- C—CHEMISTRY; METALLURGY
- C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
- C09J—ADHESIVES; NON-MECHANICAL ASPECTS OF ADHESIVE PROCESSES IN GENERAL; ADHESIVE PROCESSES NOT PROVIDED FOR ELSEWHERE; USE OF MATERIALS AS ADHESIVES
- C09J155/00—Adhesives based on homopolymers or copolymers, obtained by polymerisation reactions only involving carbon-to-carbon unsaturated bonds, not provided for in groups C09J123/00 - C09J153/00
- C09J155/005—Homopolymers or copolymers obtained by polymerisation of macromolecular compounds terminated by a carbon-to-carbon double bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Polymers & Plastics (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.経皮薬剤導入製剤であって: (1)支持体; (2)前記支持体の片面に付着しており、且つ (a)(i)アルキル基の中に4〜10個の炭素原子を含むアルキルアクリレー ト及びアルキル基の中に4〜10個の炭素原子を含むアルキルメタクリレートより 成る群から選ばれる1又は複数種のAモノマー;並びに (ii)任意的に、前記Aモノマーと共重合可能な1又は複数種のエチレ ン系不飽和Bモノマー;並びに (iii)前記A及びBモノマーと共重合可能であり、且つ500〜500,000 の域の分子量を有するマクロモノマー; を含んで成るコポリマー; (b)前記コポリマーの中に溶解されている軟化剤;並びに (c)前記軟化剤が治療的に有効なものでないとき、治療的に有効な量の薬剤 ; を含んで成るマトリックス; を含んで成り、ここで前記コポリマー中のコモノマーの構造及び量、前記コポ リマーの内部粘度、並びに前記薬剤及び軟化剤の量及び構造は、2×10-6cm2/d yne〜約4×10-3cm2/dyneの域のコンプライアンス値を有するマトリックスを供 するものである;前記経皮薬剤導入製剤。 2.前記1又は複数種のBモノマーがカルボン酸、カルボン酸エステル、ヒド ロキシ、スルホンアミド、尿素、カルバメート、カルボキサミド、アミン、オキ シ、オキソ及びシアノより成る群から選ばれる官能基を含んで成る、請求項1記 載の経皮薬剤導入製剤。 3.前記1又は複数種のBモノマーがアクリル酸、メタクリル酸、マレイン酸 、ヒドロキシアルキル基の中に2〜4個の炭素原子を含むヒドロキシアルキルア クリレート、ヒドロキシアルキル基の中に2〜4個の炭素原子を含むヒドロキシ アルキルメタクリレート、アクリルアミド、メタクリルアミド、アルキル基の中 に1〜8個の炭素原子を含むアルキル置換化アクリルアミド、ジアセトンアクリ ルアミド、アルキル基の中に1又は2個の炭素原子を有するジアルキルアクリル アミド、N−ビニル−N−メチルアセトアミド、N−ビニルバレロラクタム;N −ビニルカプロラクタム、N−ビニル−2−ピロリドン、グリシジルメタクリレ ート、アルコキシ基の中に1〜4個の炭素原子を含むアルコキシエチルアクリレ ート、アルコキシ基の中に1〜4個の炭素原子を含むアルコキシエチルメタクリ レート、2−エトキシエトキシエチルアクリレート、フルフリルメタクリレート 、フルフリルアクリレート、テトラヒドロフルフリルアクリレート、テトラヒド ロフルフリルメタクリレート、プロピレングリコールモノメタクリレート、プロ ピレングリコールモノアクリレート、ポリエチレングリコールアクリレート、ポ リエチレングリコールメチルエーテルアクリレート、ポリエチレングリコールメ タクリレート、ポリエチレンオキシドメチルエーテルアクリレート、ジ(低級) アルキルアミノエチルアクリレート、ジ(低級)アルキルアミノエチルメタクリ レート、ジ(低級)アルキルアミノプロピルメタクリルアミド、アクリロニトリ ル、メタクリロニトリル及びビニルアセテートより成る群から選ばれる、請求項 1記載の経皮薬剤導入製剤。 4.前記Aモノマーが前記コポリマー中の全モノマーの総重量に基づき約40〜 約95重量%の量で存在している、請求項1記載の経皮薬剤導入製剤。 5.前記Aモノマーが前記コポリマー中の全モノマーの総重量に基づき約50〜 約70重量%の量で存在している、請求項1記載の経皮薬剤導入製剤。 6.前記Aモノマーがイソオクチルアクリレート、2−エチルヘキシルアクリ レート、ブチルアクリレート及びシクロヘキシルアクリレートより成る群から選 ばれる、請求項1記載の経皮薬剤導入製剤。 7.前記Bモノマーが前記コポリマーの総重量に基づき0〜60重量%の量で存 在する、請求項1記載の経皮薬剤導入製剤。 8.前記Bモノマーが、前記コポリマーの総重量に基づき25重量%より多く、 前記コポリマーの総重量に基づき約50重量%以下の量で存在している、請求項1 記載の経皮薬剤導入製剤。 9.前記Bモノマーがヒドロキシエチルアクリレート、ヒドロキシエチルメタ クリレート、グリセリルアクリレート、N,N−ジメチルアクリルアミド、2− エトキシエトキシエチルアクリレート、2−エトキシエチルアクリレート、テト ラヒドロフルフリルアクリレート、アクリル酸、アクリルアミド及びビニルアセ テートより成る群から選ばれる、請求項1記載の経皮薬剤導入製剤。 10.前記マクロモノマーが5,000〜30,000の域における分子量を有する、請求 項1記載の経皮薬剤導入製剤。 11.前記マクロモノマーが前記コポリマー中の全モノマーの総重量に基づき約 15重量%以下の量で存在する、請求項1記載の経皮薬剤導入製剤。 12.前記マクロモノマーが前記コポリマー中の全モノマーの総重量に基づき約 5重量%以下の量で存在する、請求項1記載の経皮薬剤導入製剤。 13.前記マクロモノマーが次式の化合物 (式中、XはA及びBモノマーと共重合可能なエチレン系不飽和基を含んで成る 成分であり、R2は水素原子又は低級アルキルであり、R3は低級アルキル基又は 遊離基開始剤の残基であり、nは200〜500の整数であり、そして各R4は −CN及び−CO2R6(ここでR5は水素原子又は低級アルキル基であり、そしてR6 は低級アルキル基である)より成る群から独立して選ばれる一価の基である)で ある、請求項1記載の経皮薬剤導入製剤。 14.前記マクロモノマーがポリメチルメタクリレートマクロモノマー、スチレ ン/アクリロニトリルマクロモノマー及びポリスチレンマクロモノマーより成る 群から選ばれる、請求項1記載の経皮薬剤導入製剤。 15.前記軟化剤が前記マトリックスの総重量に基づき20重量%より多く、且つ 約60重量%未満の量で存在している、請求項1記載の経皮薬剤導入製剤。 16.前記軟化剤がC8−C22脂肪酸、C8−C22脂肪アルコール、C8−C22脂 肪酸の低級アルキルエステル、C8−C22脂肪酸のモノグリセリド、C6−C8二 酸のジ(低級)アルキルエステル、 テトラヒドロフルフリルアルコールポリエチレングリコールエーテル、ポリエチ レングリコール、プロピレングリコール、エトキシエトキシエタノール、ジエチ レングリコールモノメチルエーテル、N,N−ジメチルドデシルアミン−N−オ キシド、2−(2−エトキシエトキシ)エタノール、及び上記の組合せより成る 群から選ばれる、請求項1記載の経皮薬剤導入製剤。 17.前記軟化剤がジメチルスルホキシド、グリセロール、エタノール、酢酸エ チル、アセト酢酸エステル、N−メチルピロリドン、イソプロピルアルコール、 ポリエチレンオキシドのアルキルアリールエーテル、ポリエチレンオキシドモノ メチルエーテル及びポリエチレンオキシドジメチルエーテルより成る群から選ば れる、請求項1記載の経皮薬剤導入製剤。 18.前記軟化剤がニコチン、ニトログリセリン、クロフェニルアミン、ニコチ ン酸ベンジルエステル、オルフェナドリン、スコポラミン及びバルプロン酸より 成る群から選ばれる、請求項1記載の経皮薬剤導入製剤。 19.感圧皮膚接着剤であって: (1)(a)アルキル基の中に4〜10個の炭素原子を含むアルキルアクリレー ト及びアルキル基の中に4〜10個の炭素原子を含むアルキルメタクリレートより 成る群から選ばれる1又は複数種のAモノマー;並びに (b)任意的に、前記Aモノマーと共重合可能な1又は複数種のエチレ ン系不飽和Bモノマー;並びに (c)前記A及びBモノマーと共重合可能であり、且つ500〜500,000の 域の分子量を有するマクロモノマー、好ましくは実質上線形のマクロモノマー; を含んで成るコポリマー; (2)前記コポリマーの中に溶解されている軟化剤; を含んで成り、ここで前記コポリマー中のコモノマーの構造及び量、前記コポ リマーの内部粘度、並びに前記軟化剤の量及び構造は、2×10-6cm2/dyne〜約 4×10-3cm2/dyneの域のコンプライアンス値を有する感圧皮膚接着剤を供する ものである、前記感圧皮膚接着剤。 20.前記1又は複数種のBモノマーがカルボン酸、カルボン酸エステル、ヒド ロキシ、スルホンアミド、尿素、カルバメート、カルボキサミド、アミン、オキ シ、オキソ及びシアノより成る群から選ばれる官能基を含んで成る、請求項19記 載の感圧皮膚接着剤。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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US30583394A | 1994-09-14 | 1994-09-14 | |
US08/305,833 | 1994-09-14 | ||
PCT/US1995/012163 WO1996008229A2 (en) | 1994-09-14 | 1995-09-12 | Matrix for transdermal drug delivery |
Publications (2)
Publication Number | Publication Date |
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JPH10508296A true JPH10508296A (ja) | 1998-08-18 |
JP4102901B2 JP4102901B2 (ja) | 2008-06-18 |
Family
ID=23182561
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP51043296A Expired - Fee Related JP4102901B2 (ja) | 1994-09-14 | 1995-09-12 | 経皮薬剤導入用マトリックス |
Country Status (14)
Country | Link |
---|---|
US (2) | US7097853B1 (ja) |
EP (1) | EP0781122B1 (ja) |
JP (1) | JP4102901B2 (ja) |
KR (1) | KR100382706B1 (ja) |
AT (1) | ATE194281T1 (ja) |
AU (1) | AU702593B2 (ja) |
CA (1) | CA2198390C (ja) |
DE (1) | DE69517816T2 (ja) |
DK (1) | DK0781122T3 (ja) |
ES (1) | ES2147858T3 (ja) |
GR (1) | GR3033859T3 (ja) |
NZ (1) | NZ293849A (ja) |
PT (1) | PT781122E (ja) |
WO (1) | WO1996008229A2 (ja) |
Cited By (6)
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JP2005263756A (ja) * | 2004-03-22 | 2005-09-29 | Kosumedei:Kk | 親水性粘着剤を用いた親水性皮膚外用粘着剤組成物および親水性貼付剤 |
JP2007277441A (ja) * | 2006-04-10 | 2007-10-25 | Kao Corp | 生分解性樹脂用可塑剤 |
JP2013256536A (ja) * | 2000-09-29 | 2013-12-26 | Three M Innovative Properties Co | フェンタニルの経皮デリバリのための組成物 |
JP2014080419A (ja) * | 2012-09-28 | 2014-05-08 | Nitto Denko Corp | アミンオキシドを含有する貼付製剤 |
JP2015025101A (ja) * | 2013-07-29 | 2015-02-05 | 三菱レイヨン株式会社 | アクリル系樹脂組成物 |
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- 1995-09-12 DK DK95933919T patent/DK0781122T3/da active
- 1995-09-12 EP EP95933919A patent/EP0781122B1/en not_active Revoked
- 1995-09-12 ES ES95933919T patent/ES2147858T3/es not_active Expired - Lifetime
- 1995-09-12 AT AT95933919T patent/ATE194281T1/de not_active IP Right Cessation
- 1995-09-12 JP JP51043296A patent/JP4102901B2/ja not_active Expired - Fee Related
- 1995-09-12 NZ NZ293849A patent/NZ293849A/xx not_active IP Right Cessation
- 1995-09-12 KR KR1019970701693A patent/KR100382706B1/ko not_active IP Right Cessation
- 1995-09-12 PT PT95933919T patent/PT781122E/pt unknown
- 1995-09-12 DE DE69517816T patent/DE69517816T2/de not_active Revoked
- 1995-09-12 CA CA002198390A patent/CA2198390C/en not_active Expired - Fee Related
-
1997
- 1997-11-12 US US08/968,519 patent/US7097853B1/en not_active Expired - Fee Related
-
2000
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-
2005
- 2005-12-23 US US11/318,312 patent/US20060099242A1/en not_active Abandoned
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JP2013256536A (ja) * | 2000-09-29 | 2013-12-26 | Three M Innovative Properties Co | フェンタニルの経皮デリバリのための組成物 |
JP2016053083A (ja) * | 2000-09-29 | 2016-04-14 | スリーエム イノベイティブ プロパティズ カンパニー | フェンタニルの経皮デリバリのための組成物 |
WO2004087228A1 (ja) * | 2003-03-28 | 2004-10-14 | Japan Science And Technology Agency | 生体適合性と温度応答性を併せ持つ高分子 |
JP2005263756A (ja) * | 2004-03-22 | 2005-09-29 | Kosumedei:Kk | 親水性粘着剤を用いた親水性皮膚外用粘着剤組成物および親水性貼付剤 |
JP4567998B2 (ja) * | 2004-03-22 | 2010-10-27 | コスメディ製薬株式会社 | 親水性粘着剤を用いた親水性皮膚外用粘着剤組成物および親水性貼付剤 |
JP2007277441A (ja) * | 2006-04-10 | 2007-10-25 | Kao Corp | 生分解性樹脂用可塑剤 |
JP2014080419A (ja) * | 2012-09-28 | 2014-05-08 | Nitto Denko Corp | アミンオキシドを含有する貼付製剤 |
JP2015025101A (ja) * | 2013-07-29 | 2015-02-05 | 三菱レイヨン株式会社 | アクリル系樹脂組成物 |
Also Published As
Publication number | Publication date |
---|---|
US7097853B1 (en) | 2006-08-29 |
US20060099242A1 (en) | 2006-05-11 |
PT781122E (pt) | 2000-11-30 |
CA2198390A1 (en) | 1996-03-21 |
DE69517816T2 (de) | 2000-12-28 |
ES2147858T3 (es) | 2000-10-01 |
AU3639795A (en) | 1996-03-29 |
NZ293849A (en) | 1998-10-28 |
DK0781122T3 (da) | 2000-10-30 |
WO1996008229A3 (en) | 1996-07-25 |
KR970705974A (ko) | 1997-11-03 |
DE69517816D1 (de) | 2000-08-10 |
AU702593B2 (en) | 1999-02-25 |
JP4102901B2 (ja) | 2008-06-18 |
WO1996008229A2 (en) | 1996-03-21 |
EP0781122A2 (en) | 1997-07-02 |
GR3033859T3 (en) | 2000-10-31 |
EP0781122B1 (en) | 2000-07-05 |
ATE194281T1 (de) | 2000-07-15 |
CA2198390C (en) | 2009-08-11 |
KR100382706B1 (ko) | 2003-10-10 |
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