JP2009235065A5

JP2009235065A5 -

Info

Publication number: JP2009235065A5
Application number: JP2009048952A
Authority: JP
Filing date: 2009-03-03
Publication date: 2012-05-31
Anticipated expiration: 2029-03-03

Description

発明者らは、ヒトの皮脂成分に含まれるトリグリセリドを構成する脂肪酸の大部分が高級脂肪酸であることに着目し、鋭意研究を重ねた結果、不飽和の高級脂肪酸のトリグリセリドに優れた経皮吸収促進作用があるという知見を得た。 The inventors paid attention to the fact that most of the fatty acids constituting the triglycerides contained in human sebum components are higher fatty acids, and as a result of intensive research, the transdermal absorption excellent in triglycerides of unsaturated higher fatty acids. The knowledge that it has a promoting action was obtained.

本発明の経皮吸収促進剤では、高級脂肪酸は不飽和脂肪酸であることも特徴とする。 The percutaneous absorption enhancer of the present invention, a higher fatty acid is an unsaturated fatty der Rukoto also features.

本発明の経皮吸収促進剤は、少なくとも１つの脂肪酸がヒトの皮脂成分を構成する炭素数１４以上の不飽和の高級脂肪酸であるトリグリセリドからなるので、薬物経皮吸収性に優れ、且つ皮膚刺激が少なく安全性にも優れていると推測される。
また、本発明の皮膚処理用製剤は、薬物適用前に用いると、適用皮膚部にトリグリセリドを移行・含有させることができるので、その後、薬物含有経皮製剤を適用した際に薬物の経皮吸収性を促進することができる。
更に、本発明の経皮吸収型製剤及び経皮吸収型貼付剤は、本発明の経皮吸収促進剤と薬物とを含有させたので、トリグリセリドが、薬物の皮膚透過性を向上させ、薬物の経皮吸収性を促進すると推測される。 Since the transdermal absorption enhancer of the present invention comprises triglyceride, which is an unsaturated higher fatty acid having 14 or more carbon atoms, constituting at least one fatty acid component of human sebum, it has excellent drug transdermal absorbability and skin irritation. It is estimated that there are few and it is excellent also in safety.
Further, when the preparation for skin treatment of the present invention is used before drug application, it can transfer and contain triglyceride in the applied skin part, and then when the drug-containing transdermal preparation is applied, the drug is transdermally absorbed. Sexuality can be promoted.
Furthermore, since the transdermal preparation and transdermal patch of the present invention contain the transdermal absorption enhancer of the present invention and a drug, the triglyceride improves the skin permeability of the drug, It is presumed to promote transdermal absorption.

本発明の高級脂肪酸は、炭素数１４以上であれば特に限定されないが、炭素数１４〜２０が好ましく、炭素数１６〜１８がヒトの皮脂成分に多く含まれる点において特に好ましい。また、高級脂肪酸は、薬物溶解性という観点から不飽和脂肪酸である。 The higher fatty acid of the present invention is not particularly limited as long as it has 14 or more carbon atoms, but preferably has 14 to 20 carbon atoms, and is particularly preferable in that a large amount of 16 to 18 carbon atoms is contained in human sebum components. Further, higher fatty acid is a perspective of the drug solubility or et unsaturated fatty acids.

本発明の高級脂肪酸としては、オレイン酸、パルミトレイン酸、パルミチン酸、及びリノール酸が好ましく、炭素数１８のオレイン酸が経皮吸収促進性と安全性という点において特に好ましい。オレイン酸は、ヒトの皮膚の皮脂を構成する主要成分であるので、他の脂肪酸に比べて、特に皮膚刺激性が低く、安全性に優れると考えられる。 As the higher fatty acid of the present invention, O maleic acid, palmitoleic acid, palmitic acid, and linoleic acid are preferable, oleic acid having 18 carbon atoms are particularly preferable in terms of percutaneous absorption-promoting and safety. Since oleic acid is a main component constituting the sebum of human skin, it is considered to be particularly low in skin irritation and excellent in safety compared to other fatty acids.

Claims

A transdermal absorption enhancer comprising a triglyceride in which at least one fatty acid is an unsaturated higher fatty acid having 14 or more carbon atoms.

The transdermal absorption enhancer according to claim 1 , wherein the higher fatty acid is oleic acid.

A skin treatment preparation comprising the percutaneous absorption enhancer according to claim 1 or 2 and used before the drug is applied.

The preparation for skin treatment according to claim 3 , wherein the dosage form is a patch, liquid, ointment, cream, lotion, aerosol or spray.

A transdermal absorption-type preparation containing the percutaneous absorption enhancer according to claim 1 or 2 and a drug.

A transdermal absorption type patch comprising a support and a layer containing the percutaneous absorption enhancer and a drug according to claim 1 or 2 formed on the support.