JP5665861B2 - ドネペジル含有経皮吸収製剤 - Google Patents
ドネペジル含有経皮吸収製剤 Download PDFInfo
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- JP5665861B2 JP5665861B2 JP2012512893A JP2012512893A JP5665861B2 JP 5665861 B2 JP5665861 B2 JP 5665861B2 JP 2012512893 A JP2012512893 A JP 2012512893A JP 2012512893 A JP2012512893 A JP 2012512893A JP 5665861 B2 JP5665861 B2 JP 5665861B2
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- donepezil
- skin
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- skin irritation
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- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
ドネペジル含有経皮吸収製剤を調製した。表1記載の配合量にて材料を混合し、塗布液とした。塗布液を離型処理したポリエチレンテレフタレートフィルム上に展延し、温風をあてて溶剤を乾燥除去して薬物層を形成し、これに支持体(サンドマットPET、帝人デュポンフィルム株式会社製)を積層した。その後、適宜裁断して実施例1〜9及び比較例1のドネペジル含有経皮吸収製剤を得た。なお、表1に記載の割合はドネペジル含有経皮吸収製剤の全量基準(質量%)である。
ヘアレスマウスの体側部皮膚を剥離し、角質層側に実施例6及び比較例1のドネペジル含有経皮吸収製剤(約3cm2)を貼付した後、真皮側をレセプター層側にして、37℃の温水を外周部に循環させたフロースルーセルに装着した。レセプター層にpH7.4のリン酸緩衝液(PBS)を用い、約5mL/hrの流速で、実施例6の経皮吸収製剤については3時間毎、比較例1の経皮吸収製剤については2時間毎に24時間までサンプリングを行った。得られたレセプター溶液の流量を正確に測定し、高速液体クロマトグラフ法によりドネペジルの薬物濃度を測定し、1時間あたりのドネペジルの皮膚透過速度を算出した。結果を図1に示す。実施例6のドネペジル含有経皮吸収製剤は、比較例1のものと比較してより高い皮膚透過速度を示した。
ヒト正常表皮細胞を重層培養したヒト3次元培養表皮モデル(LabCyte EPI−MODEL、ジャパン・ティッシュ・エンジニアリング社製)を用いた。LabCyteはトランスウェル内で培養された培養皮膚である。実験にはLabCyteをトランスウェルとともに使用した。
・薬物単独添加群:試験溶液として4×10−4Mの塩酸ドネペジルのみを媒体に分散させたものを添加した群。
・コレステロール添加群:試験溶液として4×10−4Mの塩酸ドネペジルと1質量%のコレステロールを媒体に分散させたものを添加した群。
相対産生量=(コレステロール添加群のメディエータ産生量)/(薬物単独添加群のメディエータ産生量)×100
2cm×2cmの実施例5〜9及び比較例1のドネペジル含有経皮吸収製剤を、ウサギの剃毛済み背部皮膚に貼付した。貼付24時間後に剥離し、剥離後1時間及び48時間目に紅斑・痂皮及び浮腫形成について肉眼的に観察し、表3に示すDraizeらの評価基準に基づいて採点し、皮膚一次刺激指数(PII)を算出した。結果を図2に示す。ドネペジル含有経皮吸収製剤は、コレステロールの配合によりPIIを減少させ、コレステロールの配合量が0.5〜5質量%の間である場合、コレステロール未配合の比較例1と比べて十分にPIIを減少させた。
Claims (2)
- ドネペジル及びその薬学的に許容される塩から選択される1以上の薬物、並びに、コレステロールからなる皮膚刺激低減剤を含有する、経皮吸収製剤。
- 前記皮膚刺激低減剤の含有量は、経皮吸収製剤の全量基準で0.5〜5質量%である、請求項1に記載の経皮吸収製剤。
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2012512893A JP5665861B2 (ja) | 2010-04-28 | 2011-04-27 | ドネペジル含有経皮吸収製剤 |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2010104120 | 2010-04-28 | ||
JP2010104120 | 2010-04-28 | ||
JP2012512893A JP5665861B2 (ja) | 2010-04-28 | 2011-04-27 | ドネペジル含有経皮吸収製剤 |
PCT/JP2011/060298 WO2011136288A1 (ja) | 2010-04-28 | 2011-04-27 | ドネペジル含有経皮吸収製剤 |
Publications (2)
Publication Number | Publication Date |
---|---|
JPWO2011136288A1 JPWO2011136288A1 (ja) | 2013-07-22 |
JP5665861B2 true JP5665861B2 (ja) | 2015-02-04 |
Family
ID=44861585
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2012512893A Active JP5665861B2 (ja) | 2010-04-28 | 2011-04-27 | ドネペジル含有経皮吸収製剤 |
Country Status (6)
Country | Link |
---|---|
US (1) | US20130053358A1 (ja) |
EP (1) | EP2564848B1 (ja) |
JP (1) | JP5665861B2 (ja) |
ES (1) | ES2547888T3 (ja) |
TW (1) | TWI501790B (ja) |
WO (1) | WO2011136288A1 (ja) |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TWI433904B (zh) * | 2011-01-12 | 2014-04-11 | Taiwan Biotech Co Ltd | 多奈哌齊經皮貼片 |
WO2015072564A1 (ja) | 2013-11-17 | 2015-05-21 | 株式会社メドレックス | 経皮吸収型コロイド液剤 |
US11660344B2 (en) | 2013-11-17 | 2023-05-30 | Medrx Co., Ltd. | Transdermal colloidal solution agent |
CN106456562B (zh) * | 2014-02-20 | 2020-01-31 | 安能泰制药有限公司 | 含有多奈哌齐的透皮药物递送系统 |
US9987361B1 (en) | 2014-12-29 | 2018-06-05 | Noven Pharmaceuticals, Inc. | Compositions and method for sustained drug delivery by active transdermal technology |
JPWO2016190002A1 (ja) * | 2015-05-26 | 2018-03-08 | ニプロ株式会社 | 貼付剤 |
CN109922796B (zh) | 2016-06-23 | 2023-04-07 | 考里安有限责任公司 | 具有亲水和疏水域的粘合剂基质和治疗剂 |
US10945968B2 (en) | 2016-07-27 | 2021-03-16 | Corium, Inc. | Memantine transdermal delivery systems |
WO2018022814A1 (en) * | 2016-07-27 | 2018-02-01 | Corium International, Inc. | Transdermal delivery systems with pharmacokinetics bioequivalent to oral delivery |
CA3032148A1 (en) | 2016-07-27 | 2018-02-01 | Corium International, Inc. | Sodium bicarbonate in situ conversion driven transdermal delivery of amine drug |
AU2018392686A1 (en) | 2017-12-20 | 2020-07-09 | Corium Pharma Solutions, Inc. | Transdermal adhesive composition comprising a volatile liquid therapeutic agent having low melting point |
KR102024996B1 (ko) * | 2017-12-27 | 2019-09-25 | 동아에스티 주식회사 | 도네페질을 함유하는 치매 치료용 경피흡수제제 |
US20210290603A1 (en) * | 2020-03-18 | 2021-09-23 | Chemistryrx | Methods for treating acne |
WO2023240105A1 (en) * | 2022-06-07 | 2023-12-14 | Biomimetix Jv, Llc | Hydrophobic compositions including a hydrophilic active ingredient and methods relating thereto |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH11315016A (ja) * | 1998-03-03 | 1999-11-16 | Eisai Co Ltd | 抗痴呆薬を含有した経皮適用製剤又は坐剤 |
WO2003032960A1 (fr) * | 2001-10-17 | 2003-04-24 | Hisamitsu Pharmaceutical Co., Inc. | Preparations pour absorption percutanee |
WO2008021113A2 (en) * | 2006-08-17 | 2008-02-21 | Core Tech Solutions, Inc. | Transdermal methods and systems for treating alzheimer's disease |
WO2009075258A1 (ja) * | 2007-12-10 | 2009-06-18 | Cosmed Pharmaceutical Co., Ltd. | 経皮吸収製剤 |
Family Cites Families (9)
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DE3836971C1 (ja) | 1988-10-31 | 1990-05-17 | Weck, Wolfgang, Dr.Med., 6990 Bad Mergentheim, De | |
US6512010B1 (en) * | 1996-07-15 | 2003-01-28 | Alza Corporation | Formulations for the administration of fluoxetine |
JP4138910B2 (ja) * | 1997-07-02 | 2008-08-27 | 帝國製薬株式会社 | 経皮吸収性が良好で且つ皮膚刺激性の少ない塩酸アゼラスチン含有経皮製剤 |
US6193993B1 (en) | 1998-03-03 | 2001-02-27 | Eisai Co., Ltd. | Suppository containing an antidementia medicament |
AU1585601A (en) * | 1999-11-04 | 2001-05-14 | Xel Herbaceuticals | Transdermal administration of huperzine |
US20080138388A1 (en) * | 2005-02-04 | 2008-06-12 | Hisamitsu Pharmaceutical Co., Inc. | Transdermal Absorption Patch |
JP5097359B2 (ja) | 2006-05-09 | 2012-12-12 | 久光製薬株式会社 | ドネペジル経皮吸収型製剤 |
WO2011074637A1 (ja) * | 2009-12-16 | 2011-06-23 | 後藤 武 | 抗認知症薬物の経皮吸収製剤 |
CN102858372A (zh) * | 2010-04-28 | 2013-01-02 | 久光制药株式会社 | 皮肤刺激抑制剂和经皮吸收制剂 |
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2011
- 2011-04-27 EP EP11775069.5A patent/EP2564848B1/en active Active
- 2011-04-27 ES ES11775069.5T patent/ES2547888T3/es active Active
- 2011-04-27 US US13/643,427 patent/US20130053358A1/en not_active Abandoned
- 2011-04-27 WO PCT/JP2011/060298 patent/WO2011136288A1/ja active Application Filing
- 2011-04-27 JP JP2012512893A patent/JP5665861B2/ja active Active
- 2011-04-28 TW TW100114873A patent/TWI501790B/zh active
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH11315016A (ja) * | 1998-03-03 | 1999-11-16 | Eisai Co Ltd | 抗痴呆薬を含有した経皮適用製剤又は坐剤 |
WO2003032960A1 (fr) * | 2001-10-17 | 2003-04-24 | Hisamitsu Pharmaceutical Co., Inc. | Preparations pour absorption percutanee |
WO2008021113A2 (en) * | 2006-08-17 | 2008-02-21 | Core Tech Solutions, Inc. | Transdermal methods and systems for treating alzheimer's disease |
WO2009075258A1 (ja) * | 2007-12-10 | 2009-06-18 | Cosmed Pharmaceutical Co., Ltd. | 経皮吸収製剤 |
Non-Patent Citations (1)
Title |
---|
JPN6011026921; 桝渕幸吉: 最近の皮膚外用剤 第1版, 1991, p.195-8, 南山堂 * |
Also Published As
Publication number | Publication date |
---|---|
TW201206505A (en) | 2012-02-16 |
JPWO2011136288A1 (ja) | 2013-07-22 |
ES2547888T3 (es) | 2015-10-09 |
EP2564848A4 (en) | 2013-11-06 |
WO2011136288A1 (ja) | 2011-11-03 |
EP2564848B1 (en) | 2015-09-02 |
TWI501790B (zh) | 2015-10-01 |
EP2564848A1 (en) | 2013-03-06 |
US20130053358A1 (en) | 2013-02-28 |
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