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1. WO2020095975 - TRANSDERMAL PATCH CONTAINING FENTANYL AS ACTIVE INGREDIENT

Publication Number WO/2020/095975
Publication Date 14.05.2020
International Application No. PCT/JP2019/043585
International Filing Date 07.11.2019
IPC
A61K 31/4468 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
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
445Non-condensed piperidines, e.g. piperocaine
4468having a nitrogen atom directly attached in position 4, e.g. clebopride, fentanyl
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 47/10 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
08containing oxygen
10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols ; Poloxamers; PEG/POE alkyl ethers
A61K 47/14 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
08containing oxygen
14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
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
Applicants
  • 株式会社メドレックス MEDRX CO., LTD. [JP]/[JP]
Inventors
  • 山中 勝弘 YAMANAKA Katsuhiro
  • 濱本 英利 HAMAMOTO Hidetoshi
  • 三輪 泰司 MIWA Yasushi
  • 中江 崇 NAKAE Takashi
Agents
  • 清水 尚人 SHIMIZU Naoto
Priority Data
2018-21132709.11.2018JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) TRANSDERMAL PATCH CONTAINING FENTANYL AS ACTIVE INGREDIENT
(FR) TIMBRE TRANSDERMIQUE CONTENANT DU FENTANYL COMME PRINCIPE ACTIF
(JA) フェンタニルを有効成分とする貼付剤
Abstract
(EN)
The present invention mainly addresses the problem of a novel transdermal patch that is particularly suitable for fentanyl, has the ability to prevent re-adhesion, and has excellent sustained-release performance such that the transdermal patch can be used over a long period of time. The present invention is, for example, a transdermal patch containing fentanyl as an active ingredient, and characterized by including an ointment having fentanyl, an adhesive agent, a volatile hydrocarbon solvent (A), and a heteroatom-containing volatile organic solvent (B), wherein the boiling point of the solvent (A) is higher than the boiling point of the solvent (B), and the contained amount of the solvent (A) in the ointment is greater than the contained amount of the solvent (B) in the ointment. The transdermal patch according to the present invention can prevent inappropriate use, is advantageous in terms of transdermal absorption of fentanyl and adjustment of the pharmacokinetic profile, has excellent fentanyl sustained-release properties, and can be used over a long period of time.
(FR)
La présente invention aborde principalement le problème de la réalisation d'un nouveau timbre transdermique qui est particulièrement approprié pour le fentanyl, a la capacité d'empêcher une réadhésion, et possède d'excellentes performances de libération prolongée, de sorte que le timbre transdermique peut être utilisé sur une longue période. La solution selon la présente invention porte, par exemple, sur un timbre transdermique contenant du fentanyl en tant que principe actif et caractérisé en ce qu'il comprend un onguent contenant du fentanyl, un agent adhésif, un solvant hydrocarboné volatil (A) et un solvant organique volatil contenant un hétéroatome (B), le point d'ébullition du solvant (A) étant supérieur au point d'ébullition du solvant (B) et la quantité contenue du solvant (A) dans l'onguent étant supérieure à la quantité contenue du solvant (B) dans l'onguent. Le timbre transdermique selon la présente invention peut empêcher une utilisation inappropriée, est avantageux en termes d'absorption transdermique de fentanyl et d'ajustement du profil pharmacocinétique, possède d'excellentes propriétés de libération prolongée de fentanyl et peut être utilisé sur une longue période.
(JA)
特にフェンタニルに適した貼付剤であって、再貼付防止能を持っていることに加え、長時間使用できる徐放性能に優れた新たな貼付剤を提供することを主な課題とする。 本発明として、例えば、フェンタニルを有効成分とする貼付剤であって、 フェンタニル、粘着剤、揮発性炭化水素溶媒(A)、及びヘテロ原子を含む揮発性有機溶媒(B)を有する膏体を含み、溶媒(A)の沸点が溶媒(B)の沸点より高く、膏体中における溶媒(A)の含有量が膏体中における溶媒(B)の含有量より多いことを特徴とする貼付剤を挙げることができる。 本発明によれば、誤用防止に加え、フェンタニルの皮膚からの吸収ないし薬物動態プロファイルの調整において有利であり、フェンタニルの徐放性に優れた長時間使用可能な貼付剤とすることができる。
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