JP5882970B2 - 活性物質ブプレノルフィンを投与するための経皮治療システム - Google Patents
活性物質ブプレノルフィンを投与するための経皮治療システム Download PDFInfo
- Publication number
- JP5882970B2 JP5882970B2 JP2013208722A JP2013208722A JP5882970B2 JP 5882970 B2 JP5882970 B2 JP 5882970B2 JP 2013208722 A JP2013208722 A JP 2013208722A JP 2013208722 A JP2013208722 A JP 2013208722A JP 5882970 B2 JP5882970 B2 JP 5882970B2
- Authority
- JP
- Japan
- Prior art keywords
- buprenorphine
- transdermal therapeutic
- active ingredient
- layer
- therapeutic system
- 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.)
- Active
Links
- RMRJXGBAOAMLHD-IHFGGWKQSA-N buprenorphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)CN2CC1CC1 RMRJXGBAOAMLHD-IHFGGWKQSA-N 0.000 title claims description 54
- 229960001736 buprenorphine Drugs 0.000 title claims description 54
- 230000001225 therapeutic effect Effects 0.000 title claims description 19
- 239000013543 active substance Substances 0.000 title description 2
- 239000010410 layer Substances 0.000 claims description 58
- 239000004480 active ingredient Substances 0.000 claims description 52
- 239000011159 matrix material Substances 0.000 claims description 34
- 239000000853 adhesive Substances 0.000 claims description 20
- 230000001070 adhesive effect Effects 0.000 claims description 17
- 229920000058 polyacrylate Polymers 0.000 claims description 11
- -1 polysiloxane Polymers 0.000 claims description 10
- 150000001735 carboxylic acids Chemical class 0.000 claims description 9
- 229920001296 polysiloxane Polymers 0.000 claims description 9
- 150000001412 amines Chemical group 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 7
- 235000013870 dimethyl polysiloxane Nutrition 0.000 claims description 6
- 239000004205 dimethyl polysiloxane Substances 0.000 claims description 6
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 claims description 6
- 229920002367 Polyisobutene Polymers 0.000 claims description 5
- 239000004820 Pressure-sensitive adhesive Substances 0.000 claims description 4
- 239000007788 liquid Substances 0.000 claims description 4
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 claims description 3
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 claims description 3
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 claims description 3
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 claims description 3
- 239000005642 Oleic acid Substances 0.000 claims description 3
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 claims description 3
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims description 3
- 239000011241 protective layer Substances 0.000 claims description 3
- OYHQOLUKZRVURQ-HZJYTTRNSA-N Linoleic acid Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(O)=O OYHQOLUKZRVURQ-HZJYTTRNSA-N 0.000 claims description 2
- DTOSIQBPPRVQHS-PDBXOOCHSA-N alpha-linolenic acid Chemical compound CC\C=C/C\C=C/C\C=C/CCCCCCCC(O)=O DTOSIQBPPRVQHS-PDBXOOCHSA-N 0.000 claims description 2
- 235000020661 alpha-linolenic acid Nutrition 0.000 claims description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 2
- 235000020778 linoleic acid Nutrition 0.000 claims description 2
- OYHQOLUKZRVURQ-IXWMQOLASA-N linoleic acid Natural products CCCCC\C=C/C\C=C\CCCCCCCC(O)=O OYHQOLUKZRVURQ-IXWMQOLASA-N 0.000 claims description 2
- 229960004488 linolenic acid Drugs 0.000 claims description 2
- KQQKGWQCNNTQJW-UHFFFAOYSA-N linolenic acid Natural products CC=CCCC=CCC=CCCCCCCCC(O)=O KQQKGWQCNNTQJW-UHFFFAOYSA-N 0.000 claims description 2
- 229940100640 transdermal system Drugs 0.000 claims description 2
- 235000021313 oleic acid Nutrition 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- JOOXCMJARBKPKM-UHFFFAOYSA-N 4-oxopentanoic acid Chemical compound CC(=O)CCC(O)=O JOOXCMJARBKPKM-UHFFFAOYSA-N 0.000 description 18
- 210000003491 skin Anatomy 0.000 description 18
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 15
- 229940040102 levulinic acid Drugs 0.000 description 9
- RMRJXGBAOAMLHD-CTAPUXPBSA-N buprenorphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)CN2CC1CC1 RMRJXGBAOAMLHD-CTAPUXPBSA-N 0.000 description 7
- 230000000694 effects Effects 0.000 description 7
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 description 5
- 239000002253 acid Substances 0.000 description 5
- 239000011248 coating agent Substances 0.000 description 5
- 238000000576 coating method Methods 0.000 description 5
- 239000002904 solvent Substances 0.000 description 5
- 229920000642 polymer Polymers 0.000 description 4
- 239000000047 product Substances 0.000 description 4
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 3
- 230000008901 benefit Effects 0.000 description 3
- 239000013065 commercial product Substances 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- 230000007423 decrease Effects 0.000 description 3
- 230000001419 dependent effect Effects 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 239000007787 solid Substances 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 206010028980 Neoplasm Diseases 0.000 description 2
- 238000002425 crystallisation Methods 0.000 description 2
- 230000008025 crystallization Effects 0.000 description 2
- 239000012456 homogeneous solution Substances 0.000 description 2
- 239000003960 organic solvent Substances 0.000 description 2
- GOXQRTZXKQZDDN-UHFFFAOYSA-N 2-Ethylhexyl acrylate Chemical compound CCCCC(CC)COC(=O)C=C GOXQRTZXKQZDDN-UHFFFAOYSA-N 0.000 description 1
- OMIGHNLMNHATMP-UHFFFAOYSA-N 2-hydroxyethyl prop-2-enoate Chemical compound OCCOC(=O)C=C OMIGHNLMNHATMP-UHFFFAOYSA-N 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 238000012404 In vitro experiment Methods 0.000 description 1
- XTXRWKRVRITETP-UHFFFAOYSA-N Vinyl acetate Chemical compound CC(=O)OC=C XTXRWKRVRITETP-UHFFFAOYSA-N 0.000 description 1
- 230000037374 absorbed through the skin Effects 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000006978 adaptation Effects 0.000 description 1
- 229920005601 base polymer Polymers 0.000 description 1
- 230000005540 biological transmission Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 201000011510 cancer Diseases 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- 239000006185 dispersion Substances 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 210000002615 epidermis Anatomy 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 238000000265 homogenisation Methods 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 229960004232 linoleic acid Drugs 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Substances OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 239000000178 monomer Substances 0.000 description 1
- 230000003533 narcotic effect Effects 0.000 description 1
- 229960002969 oleic acid Drugs 0.000 description 1
- 229940005483 opioid analgesics Drugs 0.000 description 1
- 239000003961 penetration enhancing agent Substances 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 239000011505 plaster Substances 0.000 description 1
- 230000002028 premature Effects 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000000717 retained effect Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 239000002699 waste material Substances 0.000 description 1
Images
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- 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
-
- 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
- A61K9/7069—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained otherwise than by reactions only involving carbon to carbon unsaturated bonds, e.g. polysiloxane, polyesters, polyurethane, polyethylene oxide
-
- 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
- A61K9/7084—Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches
-
- 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
- A61K9/7092—Transdermal patches having multiple drug layers or reservoirs, e.g. for obtaining a specific release pattern, or for combining different drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M37/00—Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Addiction (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Medical Informatics (AREA)
- Anesthesiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Rheumatology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
メチルエチル)−4,5−エポキシ−18,19−ジヒドロ−3−ヒドロキシ−6−メトキシ−α−メチル−6,14−エテノモルフィナン−7−メタノール)は、この種類の他の
化合物に優るその利点が高い活性にある、部分合成の鎮静剤である。このことは、およそ1mgの一日量で、末期で非常に好ましくない診断を受けた癌又は腫瘍患者において、疼痛からの開放が達成し得ることを意味する。これに関連して、合成オピオイド及びその類似物に優るブプレノルフィンの特徴は、ブプレノルフィンの依存性がこれらの化合物より低いことである。その不利な点は、ブプレノルフィンの高い、即ち、467.64ダルトンの分子量のために、その経皮吸収を達成することが困難なことである。
らの機能を記載している。この活性成分は、ポリアクリレートマトリックス中で均一溶液状態であり、カルボン酸は透過促進剤及び可溶化剤としての役割を果たしている。
麻薬であるブプレノルフィンを用いた非常に低い負荷のシステム、及び使用されたこのシステムの適用後に結果として生じる最小残存含量は、更に安全性の観点から非常に望ましい。
1 支持層;
2 ブプレノルフィン/カルボン酸溶液の分散液滴を有する、ポリシロキサンに基づくマトリックス層;
3 使用前に除去される保護層;
4 ポリアクリレート接着剤に基づく皮膚接触層;
5 ブプレノルフィンを含まない感圧接着層;
6 支持層(例えば、皮膚色に着色した)。
リノレン酸から成るグループから選択される。適切な実施態様では、適用時間中に過飽和状態を達成することが可能である。過飽和系では、活性成分の熱力学的活量が、そしてそれ故単位面積当りの透過速度も過飽和要因に一致して増加する。結果として、有利なことに、送達面積及びシステムの面積も最小化することが可能である。保存時には、ブプレノルフィン及び酸のいずれもポリマーマトリックス中に残り、その結果、この期間中システムは飽和以下であり、そして活性成分の結晶化は排除される。
カルボン酸としてレブリン酸を負荷したマトリックス層を用いることにより、15〜30g/m2のコーティング質量を有する皮膚接触層で十分であることが見出された。
mgの活性成分含量を有する25cm2の参照TTSに相当することが見出された。35
μg/hのTTS参照製品の表示送達を基準にして、これは参照製品の場合17%の活性成分利用率を与え、また実施例1のTTSの場合53%の活性成分利用率を与える。このことは、実施例1の経皮システムを用いて、実質的に活性成分利用率の改善目的が達成されたことを明らかに示す。従って、活性成分としてブプレノルフィンを含有する本発明のTTSを用いて、少なくとも30%、好ましくは少なくとも40%、より好ましくは少なくとも50%のインビボ活性成分利用率を達成することが可能である。更に発生する利点
は、高い透過速度のために、これらのシステムが参照システムよりおよそ30%小さい表面積で使用し得るという点である。
A
ステンレススチール容器中で、ブプレノルフィン(3.65kg)を、レブリン酸(3.65kg)とエタノール(2.6kg)中に懸濁した。撹拌しながら、74質量%の固形
分を有するn−ヘプタン溶液の形態でのポリシロキサン接着剤(60.6kg)及びヘプ
タン(9.72kg)を加えた。混合物を、ブプレノルフィン塩基が完全に溶解するまで
撹拌して、4.55%のブプレノルフィンを含み、そして64.8%の固形分を有するブ
プレノルフィン含有接着剤溶液(80.22kg)を得た(接着剤溶液1)。
皮膚接触層として、2−エチルヘキシルアクリレート、ビニルアセテート及び2−ヒドロキシエチルアクリレートから調製したポリアクリレート接着剤を使用した。51質量%の固形分を有するこの接着剤の溶液(31.87kg)を、酢酸エチル(6.5kg)及
び純品の形態の又は他の化合物との混合物としてのオレイン酸(1.91kg)と混合し
、均質化後に活性成分を含まないポリアクリレート溶液(約40kg)を得た(接着剤溶
液2)。
当業者に公知の補助手段を用い、選択された接着剤に対して接着性となるように処理されているフィルムに、ブプレノルフィン含有接着剤溶液1をコーティングした。コーティング厚さは、溶媒を除去した結果マトリックス層のコーティング質量が55g/m2にな
るように選択した。この層中のブプレノルフィン及びレブリン酸の濃度は、それぞれ7質量%及び9質量%であった。次いで、それに続くシステムの支持層を、「乾燥した」マトリックス層上に積層した。
いで、接着処理したフィルムを、最初に作製したマトリックス層から除去し、そしてそのマトリックス層を皮膚接触層上に積層した。
マトリックス層の濃度及び層厚を表1に従って変更した以外は、実施例1と同じ方法で製造を行なった。
実施例6として、Gruenenthal GmbH社の市販の製品Transtec(登録商標)を使用した。
を用いてインビトロ実験を実施した。この目的のため、2.54cm2の面積を有する型
抜きを積層体から打ち抜き、そしてそれぞれ市販製品Transtec(登録商標)の型抜きと比較して試験を行った。Transtec(登録商標)は、3種の異なる投薬量のものが市販されているが、その投薬量はそれらの表面積に比例していた。Franzセルのアクセプター媒体中のブ
プレノルフィンの濃度を測定した(表2)。加えて、実験後にTTSのブプレノルフィン及びレブリン酸含量を分析した。実施例1の分析結果を、更なる実施例の分析結果と一緒に表とグラフ形式で示す。
の代替ではなく、異なるTTS処方間を識別するために代わりに使用されたものであるとしても、表2に示された結果は、インビトロ条件下で実施例1のTTSが、Transtec(登
録商標)と全く同じ量のブプレノルフィンを送達することを示すと評価することができる
。すでに上記したように、実施例1のTTSを、ヒトにおける薬物動態研究において、参照システムとして既に市販されているこのTTSと比較し、実施例1によるTTSの場合の53%の活性成分利用率と比較して、参照製品のTTSでは、17%の活性成分利用率が実証された。
酸含量を分析した。残存量及び残存量から計算した送達されたレブリン酸の相対量を、表3に示す。
Claims (9)
- 活性成分不透過性の支持層、活性成分のブプレノルフィン及びオレイン酸、リノール酸及びリノレン酸から成るグループから選択される少なくとも1つのカルボン酸を含む少なくとも1つの感圧接着性マトリックス層、並びに所望により使用前に剥離される保護層を含む、皮膚へブプレノルフィンを投与するための経皮治療システムであって、マトリックス層がポリシロキサン又はポリイソブチレンに基づいて構築され、ブプレノルフィンが前記カルボン酸中に溶解しており、そしてこの溶液がマトリックス層中に液滴の形態で分散していることを特徴とするシステム。
- ポリシロキサンがアミン抵抗性ジメチルポリシロキサンであることを特徴とする、請求項1に記載の経皮治療システム。
- ポリシロキサンがアミン抵抗性及び非アミン抵抗性ジメチルポリシロキサンの混合物であり、非アミン抵抗性ジメチルポリシロキサンが40質量%までの濃度で存在することを特徴とする、請求項1に記載の経皮治療システム。
- カルボン酸が活性成分のブプレノルフィンよりも速やかに皮膚に拡散することを特徴とする、請求項1〜3のいずれか1項に記載の経皮治療システム。
- カルボン酸が皮膚温度で液体であることを特徴とする、請求項1〜4のいずれか1項に記載の経皮治療システム。
- マトリックス層がポリアクリレートに基づく層と拡散可能な接触状態にあることを特徴とする、請求項1〜5のいずれか1項に記載の経皮治療システム。
- ポリアクリレート層が自己接着性皮膚接触層として具体化されることを特徴とする、請求項6に記載の経皮治療システム。
- ポリアクリレート接着剤が遊離カルボキシル基を有さないことを特徴とする、請求項7に記載の経皮治療システム。
- 疼痛治療に使用するための、請求項1〜8のいずれか1項に記載の経皮治療システム。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102006054731A DE102006054731B4 (de) | 2006-11-21 | 2006-11-21 | Transdermales therapeutisches System zur Verabreichung des Wirkstoffs Buprenorphin und Verwendung desselben in der Schmerztherapie |
DE102006054731.4 | 2006-11-21 |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009537503A Division JP5763296B2 (ja) | 2006-11-21 | 2007-11-07 | 活性物質ブプレノルフィンを投与するための経皮治療システム |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2014028844A JP2014028844A (ja) | 2014-02-13 |
JP5882970B2 true JP5882970B2 (ja) | 2016-03-09 |
Family
ID=39326133
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009537503A Active JP5763296B2 (ja) | 2006-11-21 | 2007-11-07 | 活性物質ブプレノルフィンを投与するための経皮治療システム |
JP2013208722A Active JP5882970B2 (ja) | 2006-11-21 | 2013-10-04 | 活性物質ブプレノルフィンを投与するための経皮治療システム |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009537503A Active JP5763296B2 (ja) | 2006-11-21 | 2007-11-07 | 活性物質ブプレノルフィンを投与するための経皮治療システム |
Country Status (26)
Country | Link |
---|---|
US (5) | US9308202B2 (ja) |
EP (2) | EP2769714B1 (ja) |
JP (2) | JP5763296B2 (ja) |
KR (1) | KR101444967B1 (ja) |
CN (1) | CN101528207B (ja) |
AR (1) | AR064268A1 (ja) |
AU (1) | AU2007323387B2 (ja) |
BR (1) | BRPI0719115B8 (ja) |
CA (1) | CA2670290C (ja) |
CY (2) | CY1118154T1 (ja) |
DE (1) | DE102006054731B4 (ja) |
DK (2) | DK2769714T3 (ja) |
ES (2) | ES2581574T3 (ja) |
HK (2) | HK1132921A1 (ja) |
HU (2) | HUE026978T2 (ja) |
IL (2) | IL198743A (ja) |
IN (1) | IN2009CN02662A (ja) |
MX (2) | MX344241B (ja) |
NZ (1) | NZ575500A (ja) |
PL (2) | PL2769714T3 (ja) |
PT (1) | PT2769714E (ja) |
RU (1) | RU2484822C2 (ja) |
SI (2) | SI2769714T1 (ja) |
TW (1) | TWI411452B (ja) |
WO (1) | WO2008061625A2 (ja) |
ZA (1) | ZA200901695B (ja) |
Families Citing this family (51)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8252321B2 (en) | 2004-09-13 | 2012-08-28 | Chrono Therapeutics, Inc. | Biosynchronous transdermal drug delivery for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and the treatment of hyperglycemia, alzheimer's disease, sleep disorders, parkinson's disease, aids, epilepsy, attention deficit disorder, nicotine addiction, cancer, headache and pain control, asthma, angina, hypertension, depression, cold, flu and the like |
TWI541246B (zh) | 2008-12-08 | 2016-07-11 | 歐陸斯迪公司 | 二氫羥戊甲嗎啡 |
ES2545094T3 (es) * | 2010-12-14 | 2015-09-08 | Acino Ag | Sistema terapéutico transdérmico para la administración de un principio activo |
DE102011076653A1 (de) * | 2011-05-27 | 2012-11-29 | Acino Ag | Transdermales therapeutisches System enthaltend Buprenorphin und eine alpha-Hydroxysäure |
WO2013006643A1 (en) | 2011-07-06 | 2013-01-10 | The Parkinson's Institute | Compositions and methods for treatment of symptoms in parkinson's disease patients |
EP3936133A1 (en) | 2011-11-23 | 2022-01-12 | TherapeuticsMD, Inc. | Natural combination hormone replacement formulations and therapies |
US9301920B2 (en) | 2012-06-18 | 2016-04-05 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
ES2647516T3 (es) * | 2011-12-12 | 2017-12-22 | Lts Lohmann Therapie-Systeme Ag | Sistema de administración transdérmica que comprende buprenorfina |
US20150196640A1 (en) | 2012-06-18 | 2015-07-16 | Therapeuticsmd, Inc. | Progesterone formulations having a desirable pk profile |
US20130338122A1 (en) | 2012-06-18 | 2013-12-19 | Therapeuticsmd, Inc. | Transdermal hormone replacement therapies |
US10806740B2 (en) | 2012-06-18 | 2020-10-20 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
US10806697B2 (en) | 2012-12-21 | 2020-10-20 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
AU2013305563B2 (en) | 2012-08-24 | 2018-09-27 | Integurx Therapeutics, Llc | Chemical compositions and methods for enhancing transdermal delivery of therapeutic agents |
TW201431570A (zh) | 2012-11-22 | 2014-08-16 | Ucb Pharma Gmbh | 用於經皮投服羅替戈汀(Rotigotine)之多天式貼片 |
AU2013205080B2 (en) * | 2012-12-12 | 2016-07-07 | Lts Lohmann Therapie-Systeme Ag | Transdermal Delivery System |
US9180091B2 (en) | 2012-12-21 | 2015-11-10 | Therapeuticsmd, Inc. | Soluble estradiol capsule for vaginal insertion |
US10568891B2 (en) | 2012-12-21 | 2020-02-25 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
US10537581B2 (en) | 2012-12-21 | 2020-01-21 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
EP2934497B1 (en) * | 2012-12-21 | 2016-11-23 | Teikoku Pharma USA, Inc. | Compositions and methods for transdermal delivery of hormones and other medicinal agents |
US11266661B2 (en) | 2012-12-21 | 2022-03-08 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
US10471072B2 (en) | 2012-12-21 | 2019-11-12 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
US11246875B2 (en) | 2012-12-21 | 2022-02-15 | Therapeuticsmd, Inc. | Vaginal inserted estradiol pharmaceutical compositions and methods |
CN103893154A (zh) * | 2012-12-26 | 2014-07-02 | 江苏康倍得药业有限公司 | 包含丁丙诺啡的透皮给药*** |
EP2938391B1 (en) * | 2012-12-28 | 2022-07-27 | Teikoku Seiyaku Co., Ltd. | Extended buprenorphine transdermal delivery compositions |
JP5768222B2 (ja) * | 2013-03-01 | 2015-08-26 | パナソニックIpマネジメント株式会社 | 転写装置および印刷装置 |
GB201309654D0 (en) | 2013-05-30 | 2013-07-17 | Euro Celtique Sa | Method |
SI2810646T1 (sl) * | 2013-06-04 | 2016-11-30 | Lts Lohmann Therapie-Systeme Ag | Transdermalni sistem za dajanje |
ES2703623T3 (es) * | 2013-06-28 | 2019-03-11 | Purdue Pharma Lp | Antagonistas opioides para uso en el tratamiento de una arritmia inducida por analgésicos opioides |
EP3016641B1 (de) | 2013-07-03 | 2018-09-05 | LTS Lohmann Therapie-Systeme AG | Transdermales therapeutisches system mit elektronischem bauteil |
EP2921184A1 (de) * | 2014-03-19 | 2015-09-23 | LTS LOHMANN Therapie-Systeme AG | Überpflaster mit verbesserter Verträglichkeit und einer langen Haftungsdauer und Verfahren zu seiner Herstellung |
EP4238580A3 (en) | 2014-05-20 | 2023-10-25 | LTS Lohmann Therapie-Systeme AG | Transdermal delivery system including an interface mediator |
CN106456567A (zh) | 2014-05-20 | 2017-02-22 | Lts勒曼治疗***股份公司 | 在经皮递送***中调节活性剂释放的方法 |
EP3145502B1 (en) | 2014-05-20 | 2022-07-06 | LTS Lohmann Therapie-Systeme AG | Transdermal delivery system containing rotigotine |
CA2947767A1 (en) | 2014-05-22 | 2015-11-26 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
AU2016211330A1 (en) | 2015-01-28 | 2017-08-03 | Chrono Therapeutics Inc. | Drug delivery methods and systems |
CN107660207B (zh) | 2015-03-10 | 2020-09-29 | 罗德科技公司 | 丁丙诺啡乙酸盐及用于制备丁丙诺啡的方法 |
AU2016228779A1 (en) | 2015-03-12 | 2017-09-07 | Chrono Therapeutics Inc. | Craving input and support system |
US10328087B2 (en) | 2015-07-23 | 2019-06-25 | Therapeuticsmd, Inc. | Formulations for solubilizing hormones |
EP3349737A4 (en) * | 2015-09-14 | 2019-05-15 | Amneal Pharmaceuticals LLC | SYSTEM FOR TRANSDERING |
AR102214A1 (es) * | 2015-10-08 | 2017-02-15 | Amarin Tech S A | Un dispositivo para la administración transdermal de buprenorfina |
US10286077B2 (en) | 2016-04-01 | 2019-05-14 | Therapeuticsmd, Inc. | Steroid hormone compositions in medium chain oils |
BR112018070199A2 (pt) | 2016-04-01 | 2019-01-29 | Therapeuticsmd Inc | composição farmacêutica de hormônio esteroide |
JP2020503950A (ja) | 2017-01-06 | 2020-02-06 | クロノ セラピューティクス インコーポレイテッドChrono Therapeutics Inc. | 経皮薬剤送達の装置及び方法 |
ES2900255T3 (es) * | 2017-09-04 | 2022-03-16 | Lts Lohmann Therapie Systeme Ag | Sistema de administración transdérmica que incluye un emulsionante |
WO2019064026A1 (en) | 2017-09-29 | 2019-04-04 | Orexo Ab | NEW PHARMACEUTICAL COMPOSITIONS |
DE102017127433A1 (de) * | 2017-11-21 | 2019-05-23 | Lts Lohmann Therapie-Systeme Ag | TTS auf Basis von klebenden Weichmacher-Polymer-Matrices |
BR112020018300A2 (pt) * | 2018-03-13 | 2020-12-22 | Lts Lohmann Therapie-Systeme Ag | Sistema terapêutico transdérmico compreendendo um polímero híbrido de silicone e acrílico |
JP7420797B2 (ja) | 2018-05-29 | 2024-01-23 | モーニングサイド ベンチャー インベストメンツ リミテッド | 薬剤送達の方法及びシステム |
GB201904767D0 (en) | 2019-04-04 | 2019-05-22 | Orexo Ab | New pharmaceutical compositions |
US11752114B2 (en) | 2019-04-17 | 2023-09-12 | Lts Lohmann Therapie-Systeme Ag | Transdermal therapeutic system |
WO2022039195A1 (ja) * | 2020-08-19 | 2022-02-24 | 東洋インキScホールディングス株式会社 | 貼付剤 |
Family Cites Families (28)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB1136214A (en) | 1965-06-15 | 1968-12-11 | Reckitt & Sons Ltd | Thebaine and oripavine derivatives |
US3474101A (en) | 1960-09-05 | 1969-10-21 | Reckitt & Sons Ltd | Thebaine and oripavine derivatives |
US4806341A (en) * | 1985-02-25 | 1989-02-21 | Rutgers, The State University Of New Jersey | Transdermal absorption dosage unit for narcotic analgesics and antagonists and process for administration |
US5656286A (en) | 1988-03-04 | 1997-08-12 | Noven Pharmaceuticals, Inc. | Solubility parameter based drug delivery system and method for altering drug saturation concentration |
CA2002299A1 (en) * | 1988-11-10 | 1990-05-10 | Eugene G. Drust | Compositions for the transdermal delivery of buprenorphine salts |
US5240711A (en) * | 1989-11-29 | 1993-08-31 | Lts Lohmann Therapie-Systeme Gmbh & Co. Kg | Transdermal therapeutic system comprising as active component buprenorphine |
DE3939376C1 (ja) | 1989-11-29 | 1991-05-08 | Lts Lohmann Therapie-Systeme Gmbh & Co. Kg, 5450 Neuwied, De | |
DE4446600A1 (de) | 1994-12-24 | 1996-06-27 | Lohmann Therapie Syst Lts | Transdermale Resorption von Wirkstoffen aus unterkühlten Schmelzen |
US5968547A (en) * | 1997-02-24 | 1999-10-19 | Euro-Celtique, S.A. | Method of providing sustained analgesia with buprenorphine |
DE19922662C1 (de) * | 1999-05-18 | 2000-12-28 | Sanol Arznei Schwarz Gmbh | Transdermales therapeutisches System (TTS) Tolterodin enthaltend |
DE19958554C2 (de) * | 1999-07-02 | 2002-06-13 | Lohmann Therapie Syst Lts | Mikroreservoirsystem auf Basis von Polysiloxanen und ambiphilen Lösemitteln und ihre Herstellung |
PT1191927E (pt) | 1999-07-02 | 2003-07-31 | Lohmann Therapie Syst Lts | Sistema de microrreservatorios a base de polissiloxanos e solventes ambifilicos |
JP2003522144A (ja) | 2000-02-08 | 2003-07-22 | ユーロ−セルティーク,エス.エイ. | オピオイドアゴニストおよびアンタゴニストを含む制御放出組成物 |
US6682757B1 (en) | 2000-11-16 | 2004-01-27 | Euro-Celtique, S.A. | Titratable dosage transdermal delivery system |
JP2004525960A (ja) | 2001-02-16 | 2004-08-26 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | 尿失禁、特に切迫尿失禁の治療用経皮デリバリーディバイスの製造にブプレノルフィンを使用する方法 |
DE10141651B4 (de) | 2001-08-24 | 2007-02-15 | Lts Lohmann Therapie-Systeme Ag | Transdermales Therapeutisches System (TTS) mit dem Wirkstoff Fentanyl und Verfahren zu seiner Herstellung |
DE10213772A1 (de) | 2002-03-27 | 2003-10-09 | Gruenenthal Gmbh | Zusammenhängende Einheit aus vereinzelbaren transdermalen therapeutischen Systemen |
US20050118245A1 (en) | 2002-03-27 | 2005-06-02 | Wilsmann Klaus M. | Assembled unit consisting of individually separable, transdermal, therapeutic systems |
DE50307717D1 (de) * | 2002-08-09 | 2007-08-30 | Gruenenthal Gmbh | Opiod-rezeptor-antagonisten in transdermalen systemen mit buprenorphin |
US20050191340A1 (en) * | 2002-08-09 | 2005-09-01 | Gruenenthal Gmbh | Opioid-receptor antagonists in transdermal systems having buprenorphine |
PT1572167E (pt) * | 2002-12-13 | 2008-10-03 | Euro Celtique Sa | Regime posológico de buprenorfina papa analgesia |
RU2324372C2 (ru) * | 2003-03-25 | 2008-05-20 | Моринда, Инк. | Селективное ингибирование продукции эстрогена и обеспечение эстрогенного действия в организме человека |
DE102004045599A1 (de) | 2004-09-17 | 2006-03-23 | Grünenthal GmbH | System zur sequentiellen, transdermalen Verabreichung von systemisch wirksamen Substanzen |
DE102004062647A1 (de) | 2004-12-21 | 2006-06-29 | Kronotec Ag | Holzfaserdämmstoffplatte bzw.- matte |
DE102004062614B4 (de) * | 2004-12-24 | 2011-12-29 | Lts Lohmann Therapie-Systeme Ag | Transdermales therapeutisches System mit aktivierbarer Übersättigung und kontrollierter Permeationförderung sowie Verfahren zu dessen Herstellung |
ES2647516T3 (es) | 2011-12-12 | 2017-12-22 | Lts Lohmann Therapie-Systeme Ag | Sistema de administración transdérmica que comprende buprenorfina |
AU2013205080B2 (en) | 2012-12-12 | 2016-07-07 | Lts Lohmann Therapie-Systeme Ag | Transdermal Delivery System |
SI2810646T1 (sl) | 2013-06-04 | 2016-11-30 | Lts Lohmann Therapie-Systeme Ag | Transdermalni sistem za dajanje |
-
2006
- 2006-11-21 DE DE102006054731A patent/DE102006054731B4/de active Active
-
2007
- 2007-11-07 CN CN2007800392326A patent/CN101528207B/zh active Active
- 2007-11-07 KR KR1020097010295A patent/KR101444967B1/ko active IP Right Grant
- 2007-11-07 IN IN2662CHN2009 patent/IN2009CN02662A/en unknown
- 2007-11-07 HU HUE14169050A patent/HUE026978T2/en unknown
- 2007-11-07 RU RU2009123368/15A patent/RU2484822C2/ru active
- 2007-11-07 DK DK14169050.3T patent/DK2769714T3/en active
- 2007-11-07 US US12/515,848 patent/US9308202B2/en active Active
- 2007-11-07 EP EP20140169050 patent/EP2769714B1/de active Active
- 2007-11-07 NZ NZ575500A patent/NZ575500A/en not_active IP Right Cessation
- 2007-11-07 SI SI200731679T patent/SI2769714T1/sl unknown
- 2007-11-07 PL PL14169050T patent/PL2769714T3/pl unknown
- 2007-11-07 SI SI200731789A patent/SI2094249T1/sl unknown
- 2007-11-07 WO PCT/EP2007/009622 patent/WO2008061625A2/de active Application Filing
- 2007-11-07 HU HUE07846537A patent/HUE028971T2/en unknown
- 2007-11-07 ES ES07846537.4T patent/ES2581574T3/es active Active
- 2007-11-07 AU AU2007323387A patent/AU2007323387B2/en active Active
- 2007-11-07 JP JP2009537503A patent/JP5763296B2/ja active Active
- 2007-11-07 CA CA2670290A patent/CA2670290C/en active Active
- 2007-11-07 ES ES14169050.3T patent/ES2543977T3/es active Active
- 2007-11-07 MX MX2014000088A patent/MX344241B/es unknown
- 2007-11-07 PT PT141690503T patent/PT2769714E/pt unknown
- 2007-11-07 MX MX2009005341A patent/MX2009005341A/es active IP Right Grant
- 2007-11-07 DK DK07846537.4T patent/DK2094249T3/en active
- 2007-11-07 EP EP07846537.4A patent/EP2094249B1/de active Active
- 2007-11-07 BR BRPI0719115A patent/BRPI0719115B8/pt active IP Right Grant
- 2007-11-07 PL PL07846537T patent/PL2094249T3/pl unknown
- 2007-11-19 TW TW096143699A patent/TWI411452B/zh not_active IP Right Cessation
- 2007-11-19 AR ARP070105127A patent/AR064268A1/es unknown
-
2009
- 2009-03-10 ZA ZA2009/01695A patent/ZA200901695B/en unknown
- 2009-05-14 IL IL198743A patent/IL198743A/en not_active IP Right Cessation
- 2009-11-27 HK HK09111101.4A patent/HK1132921A1/xx unknown
-
2013
- 2013-10-04 JP JP2013208722A patent/JP5882970B2/ja active Active
-
2015
- 2015-02-03 HK HK15101145.5A patent/HK1200373A1/xx unknown
- 2015-08-03 CY CY20151100674T patent/CY1118154T1/el unknown
-
2016
- 2016-02-25 US US15/053,139 patent/US20160175447A1/en not_active Abandoned
- 2016-04-21 IL IL245290A patent/IL245290A0/en unknown
- 2016-07-11 CY CY20161100649T patent/CY1117770T1/el unknown
-
2017
- 2017-04-27 US US15/499,304 patent/US20170224676A1/en not_active Abandoned
-
2018
- 2018-06-08 US US16/003,855 patent/US20180289698A1/en not_active Abandoned
-
2019
- 2019-02-28 US US16/288,911 patent/US20190192506A1/en not_active Abandoned
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP5882970B2 (ja) | 活性物質ブプレノルフィンを投与するための経皮治療システム | |
FI103478B (fi) | Menetelmä transdermaalisen terapeuttisen järjestelmän valmistamiseksi, jossa vaikuttavan aineen virtausta on suurennettu | |
EP3179989B1 (en) | Silicone-containing acrylic polymers for transdermal drug delivery compositions | |
US10729686B2 (en) | Pharmaceutical compositions | |
CZ307857B6 (cs) | Transdermální náplast pro podávání fentanylu nebo jeho analogu | |
WO2008021113A2 (en) | Transdermal methods and systems for treating alzheimer's disease | |
TW201000153A (en) | Composition and methods for the transdermal delivery of pharmaceutical compounds | |
AU774740B2 (en) | Microreservoir system on the basis of polysiloxanes and ambiphilic solvents | |
CA3162229A1 (en) | Transdermal therapeutic system containing agomelatine | |
AU2004210406B2 (en) | Transdermal therapeutic system suitable for heat application for promoting the permeation of active substances, and the use thereof | |
KR20130022602A (ko) | 경피 흡수 제제 및 그 제조방법 | |
CN101627979B (zh) | ***透皮缓释贴片 | |
KR20100105866A (ko) | 우레아 성분을 가진 경피 치료 시스템 | |
AU2013270470A1 (en) | Transdermal therapeutic system for administering the active substance buprenorphine | |
KR101964295B1 (ko) | 피부 자극이 감소된 메만틴 경피전달 시스템 | |
CN116056689A (zh) | 艾司***-混悬剂-tts | |
WO2006024339A2 (en) | Controlled-release multilayer patch for the topical use | |
MX2008014151A (es) | Preparaciones de absorcion percutanea de drogas contra demencia. |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20141028 |
|
A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20150115 |
|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20150423 |
|
A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20150616 |
|
A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20150915 |
|
A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20151211 |
|
TRDD | Decision of grant or rejection written | ||
A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20160112 |
|
A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20160204 |
|
R150 | Certificate of patent or registration of utility model |
Ref document number: 5882970 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |