Colloid systems and wetting agents; subcombinations thereof; pro – Continuous gas or vapor phase: colloid systems; compositions... – Discontinuous phase primarily liquid
Patent
1998-06-12
2000-10-17
Lovering, Richard D.
Colloid systems and wetting agents; subcombinations thereof; pro
Continuous gas or vapor phase: colloid systems; compositions...
Discontinuous phase primarily liquid
424 45, 514817, 514830, 514944, C09K 330, A61K 912
Patent
active
061333271
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to an aerosol preparation which when sprayed forms a sherbet-like solid on the sprayed site and has an enhanced cooling effect.
BACKGROUND ART
It is effective to cool the affected part in order to quickly calm the pain caused by contusion, sprain, muscular fatigue, etc. or the itch caused by athlete's foot, insect bite, etc. In the past, the aerosol preparations which when sprayed do not form a sherbet-like solid have been used frequently for such symptoms. However, since such aerosol preparations do not have a durable cooling effect on the skin, a durable calming effect of pain or itch on the affected part cannot be achieved by these aerosol preparations. The specifications of WO90/11068 and Japanese Patent Kokai 4-103526 disclose aerosol preparations which form a sherbet-like foam gel for solving such drawbacks. However, such prior art aerosol preparations require complicated procedures such as heating and emulsifying procedures for the production of the concentrate, and have a problem of low efficacy in the production.
In addition, it is essential to contain water in the known aerosol preparations which when sprayed form a sherbet-like solid, because the durable cooling effect of these preparations can be obtained by freezing water which is contained therein. Accordingly, it is impossible to contain drugs labile in water or highly lipophilic drugs in the known preparations.
DISCLOSURE OF THE INVENTION
As a result of extensive research in order to solve the above-mentioned purposes, the present inventors have found that an aerosol preparation comprising a lower alcohol, a higher alcohol and a liquefied gas does not require an emulsifying procedure for the production and has a durable cooling effect because the aerosol preparation forms a sherbet-like solid when sprayed, and whereby the present invention has been accomplished.
That is, the present invention relates to an aerosol preparation which when sprayed forms a sherbet-like solid, which comprises a concentrate containing a lower alcohol having 1 to 3 carbon atoms and a higher alcohol having at least 12 carbon atoms, and a propellant containing a liquefied gas.
Any known aerosol preparations form a solid, when sprayed, by freezing water which is contained therein, on the contrary, the aerosol preparation of the present invention does not always necessarily contain water, and it is characterized by that the aerosol preparation forms a solid under entirely new conditions when sprayed.
According to the aerosol preparation of the present invention, the higher alcohol which is cooled by the heat of vaporization of the liquefied gas including the lower alcohol forms a sherbet-like solid when sprayed.
In the present invention, the lower alcohol having 1 to 3 carbon atoms means a straight or branched alcohol, for example, methanol, ethanol, denatured ethanol, propanol, isopropanol, etc., and preferably ethanol. The amount of the lower alcohol is preferably 0.3 to 65% by weight based on the total amount of the preparation, more preferably 1.5 to 50% by weight and most preferably 15 to 35% by weight. If the amount of the lower alcohol is less than 0.3% by weight, the concentrate cannot be easily mixed with the propellant homogeneously. If the amount of the lower alcohol is more than 65% by weight, since the amount of the propellant is relatively reduced, the cold feeling is reduced.
The higher alcohol having at least 12 carbon atoms of the present invention means a straight or branched alcohol which can be homogeneously mixed with other components, for example, lauryl alcohol, cetanol, stearyl alcohol, cetostearyl alcohol, behenyl alcohol, lanolin alcohol, hydrogenated lanolin alcohol, etc, they may be used alone or by mixture with each other, and stearyl alcohol or cetanol is preferable.
The amount of the higher alcohol is preferably 0.005 to 14% by weight based on the total amount of the preparation, more preferably 0.015 to 10% by weight and most preferably 0.5 to 5% by weight. If the amount of the higher
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Kimura Fuminori
Shimamura Haruo
Uchiyama Tsuyoshi
Urushizaki Fumio
Lovering Richard D.
Taisho Pharmaceutical Co. Ltd.
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