Tape preparation comprising etodolac in ionic liquid form

A - Human Necessities – 61 – K

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IPC codes

A61K 31/407 (2006.01) A61K 9/70 (2006.01) A61K 47/06 (2006.01) A61K 47/10 (2006.01) A61K 47/14 (2006.01) A61P 29/00 (2006.01) A61K 31/167 (2006.01)

Type

Patent

Patent number

CA 2708233

Description

Disclosed is a tape preparation comprising etodolac in an ionic liquid form, which has high transdermal absorbability. Etodolac is reacted with an organic amine compound to produce an ionic liquid of etodolac. By using the ionic liquid, it becomes possible to increase the transdermal absorbability of etodolac. Further for the purpose of enhancing the transdermal absorbability and the tissue penetration ability of an ionic solution of etodolac, the composition of an organic solvent system for the ionic solution of etodolac is investigated, and it is found that a mixed solvent of an alcohol and an ester (1:2 to 2:1) is suitable as the organic solvent. Still further, an appropriate adhesion force can be achieved by properly selecting a softening agent. In this manner, a tape preparation having good transdermal absorbability can be prepared. The tape preparation can exert its pharmacological efficacy rapidly, and is therefore extremely effective for the teatment of a chronic pain such as rheumatoid arthritis, osteoarthritis and lumbago, an inflammatory diseases such as shoulder periarthritis and tendovaginitis, cervical syndrome, a pain induced by a surgery or an injury, or the like.

La présente invention concerne une préparation de ruban adhésif comportant de l'étodolac sous forme de liquide ionique, présentant une aptitude élevée à l'absorption transdermique. On fait réagir l'étodolac avec un composé organique d'amine pour produire un liquide ionique d'étodolac. Grâce à l'utilisation du liquide ionique, il est possible d'accroître l'aptitude à l'absorption transdermique de l'étodolac. En outre, en vue d'améliorer l'aptitude à l'absorption transdermique et la capacité de pénétration tissulaire d'une solution ionique d'étodolac, on a testé une composition d'un système de solvant organique d'étodolac, et l'on a noté qu'un mélange de solvant à base d'un alcool et d'un ester (1:2 to 2:1) est approprié en tant que solvant organique. Par ailleurs, une force d'adhésion appropriée peut être obtenue par la sélection appropriée d'un agent d'adoucissage. Ainsi, la préparation de ruban adhésif peut exercer rapidement son efficacité pharmacologique, et est donc très efficace pour le traitement d'une douleur chronique telle que la polyarthrite rhumatoïde, l'arthrose et le lumbago, d'une maladie inflammatoire telle que la périarthrite de l'épaule et le tendovaginite, le syndrome cervical, une douleur induite par une chirurgie ou une lésion, ou analogues.

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