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1. WO2012060431 - PATCH

Publication Number WO/2012/060431
Publication Date 10.05.2012
International Application No. PCT/JP2011/075354
International Filing Date 02.11.2011
IPC
A61K 31/4168 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
41641,3-Diazoles
4168having a nitrogen atom attached in position 2, e.g. clonidine
A61K 9/70 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
70Web, sheet or filament bases
A61K 47/06 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
A61K 47/32 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
A61P 9/12 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
12Antihypertensives
CPC
A61K 31/4168
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
41641,3-Diazoles
4168having a nitrogen attached in position 2, e.g. clonidine
A61K 9/7023
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
70Web, sheet or filament bases ; ; Films; Fibres of the matrix type containing drug;
7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
A61K 9/7046
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
70Web, sheet or filament bases ; ; Films; Fibres of the matrix type containing drug;
7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
703characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
7038Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
7046the adhesive comprising macromolecular compounds
A61K 9/7053
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
70Web, sheet or filament bases ; ; Films; Fibres of the matrix type containing drug;
7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
703characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
7038Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
7046the adhesive comprising macromolecular compounds
7053obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
A61P 9/12
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
12Antihypertensives
Applicants
  • 積水メディカル株式会社 SEKISUI MEDICAL Co.,Ltd. [JP]/[JP] (AllExceptUS)
  • 宇田川 弘子 UDAGAWA Hiroko [JP]/[JP] (UsOnly)
  • 稲葉 義和 INABA Yoshikazu [JP]/[JP] (UsOnly)
  • 野田 幸彦 NODA Yukihiko [JP]/[JP] (UsOnly)
  • 小端 久美 OBATA Kumi [JP]/[JP] (UsOnly)
  • 寺島 寛人 TERASHIMA Hiroto [JP]/[JP] (UsOnly)
Inventors
  • 宇田川 弘子 UDAGAWA Hiroko
  • 稲葉 義和 INABA Yoshikazu
  • 野田 幸彦 NODA Yukihiko
  • 小端 久美 OBATA Kumi
  • 寺島 寛人 TERASHIMA Hiroto
Agents
  • 山本 拓也 YAMAMOTO Takuya
Priority Data
2010-24690602.11.2010JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) PATCH
(FR) TIMBRE
(JA) 貼付剤
Abstract
(EN)
A patch with stable transdermal absorbability, regardless of temperature changes during storage, in a crystallized formulation of clonidine is provided. This patch is characterized by including a backing, and a plaster layer integrally laminated on one surface of the backing, said plaster layer containing 5 to 30 wt% of clonidine containing crystallized clonidine, 25 to 90 wt% of a polymer base (A) having a viscosity-average molecular weight of at least 800,000, and 5 to 60 wt% of a liquid additive capable of dissolving the clonidine, wherein the weight ratio of the liquid additive to the polymer base (A) [liquid additive/polymer base (A)] is 0.1 to 2.0.
(FR)
L'invention concerne un timbre présentant une absorbabilité transdermique stable, quels que soient les changements de température survenant pendant le stockage, doté d'une préparation cristallisée de clonidine. Le timbre selon l'invention se caractérise en ce qu'il comprend un support et une couche pansement stratifiée d'un seul bloc sur une surface du support, ladite couche contenant de 5 à 30% en poids de clonidine contenant de la clonidine cristallisée, de 25 à 90% en poids d'une base polymère (A) présentant un poids moléculaire moyen en viscosité d'au moins 800 000 et de 5 à 60% en poids d'un additif liquide apte à dissoudre la clonidine, le rapport de poids additif liquide-base polymère (A) étant compris entre 0,1 et 2.
(JA)
 クロニジンの結晶析出製剤において、保存中の温度変化にもかかわらず経皮吸収性の安定した貼付剤を提供する。本発明の貼付剤は、支持体と、上記支持体の一面に積層一体化され、結晶状態のクロニジンを含むクロニジン5~30重量%と、粘度平均分子量が80万以上である高分子基剤(A)25~90重量%と、上記クロニジンを溶解させることができる液状添加剤5~60重量%とを含有し、且つ上記高分子基剤(A)に対する上記液状添加剤の重量比[液状添加剤/高分子基剤(A)]が、0.1~2.0である膏体層とを含むことを特徴とする。
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