External preparations for treating dermatoses

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C514S762000, C514S861000, C514S863000, C514S864000

Reexamination Certificate

active

06248779

ABSTRACT:

TECHNICAL FIELD
The present invention relates to external preparations for the treatment of dermatoses.
BACKGROUND ART
External preparations containing an adrenocortical hormone have so far been used widely in the treatment of dermatoses, in particular intractable dermatoses such as atopic dermatitis and contact dermatitis and it is known that they have high pharmacological effects (Gekkan Yakuji (Pharmaceuticals Monthly); 26, 8, 55, 1984). Japanese Kokai Publication Sho-62-149620, for instance, discloses an external preparation containing an adrenocortical hormone as a principal active component.
However, adrenocortial hormone-containing external preparations may possibly induce adverse effects at the sites of application, for example increased easy infectivity, skin thinning, vascular wall embrittlement and abnormal activation of the pilosebaceous system and, in addition, the drug substances endermically absorbed may possibly produce systemic adverse effects. Thus, the closest attention should be paid to their doses. Therefore, for hydrocortisone acetate, for instance, which is a typical adrenocortical hormone, the Japanese Pharmacopoeia prescribes an upper limit use concentration of about 1% by weight and, for dexamethasone and prednisolone, an upper limit concentration of about 0.1 to 0.5% by weight.
On the other hand, external preparations with reduced adverse effects are also available, for example external preparations containing a nonsteroidal antiinflammatory agent and/or an antihistaminic agent. However, as compared with adrenocortical hormone-containing ones, they are much less effective against such intractable dermatoses as mentioned above (Shinyaku to Chiryo (New Remedies and Therapy); 25, 298, 41, 1984).
As mentioned above, adrenocortical hormones have high pharmacological effects but are disadvantageous in that they have strong side effects. Therefore, it is earnestly desired that preparations with which clinical effects comparable to those attained with the conventional preparations can be produced at lower adrenocortical hormone concentrations be developed. In the state of the art, even if higher clinical effects are required, it is impossible to increase their contents to levels exceeding those currently employed, when their side effects are taken into consideration.
For solving these problems, Japanese Kokai Publication Sho-61-40210 discloses a preparation for treating dermatoses and skin protection which comprises vitamin E and Japanese Kokai Publication Sho-53-136521 discloses a preparation for the treatment of vegetating dermatoses which contains &agr;-tocopherol. However, these are insufficiently effective in intractable dermatoses possibly due to the low concentration of vitamin E or &agr;-tocopherol in the preparations.
Japanese Kokai Publication Hei-06-179619 discloses an external preparation for the treatment of dermatoses which contains vitamin E and a transdermal absorption enhancer. However, when it is administered continuedly for achieving satisfactory therapeutic effects, the transdermal absorption enhancer may possibly produce skin irritating effects.
Furthermore, Japanese Kokai Publication Hei-06-247852 discloses an external preparation for the treatment of dermatoses which contains 1 to 30% by weight of vitamin E and 1 to 30% by weight of squalene. It is known that this vitamin E- and squalene-containing external preparation for treating dermatoses can be widely applied to dermatoses without producing such adverse effects as encountered with the steroid-containing preparations mentioned above. However, for producing higher clinical effects, preparations showing still stronger effects are desired.
SUMMARY OF THE INVENTION
In a first aspect of the present invention, it is an object thereof to provide an external preparation for the treatment of dermatoses which has an efficacy at least equivalent to that of external preparations containing an adrenocortical hormone as an active ingredient and which produces only reduced adverse effects. In the first aspect thereof, the present invention provides an external preparation for the treatment of dermatoses which comprises vitamin E and squalane.
In a second aspect, it is an object of the present invention to provide an external preparation for the treatment of dermatoses in which the adrenocortical hormone content is lower as compared with conventional preparations and which can produce high clinical efficacy with reduced side effects. In the second aspect thereof, the present invention provides an external preparation for the treatment of dermatoses which comprises an adrenocortical hormone, vitamin E and squalane.
In a third aspect, it is an object of the present invention to provide an external preparation for the treatment of dermatoses which is highly efficacious but reduced in side effects. In this third aspect, the present invention provides an external preparation for the treatment of dermatoses which comprises a nonsteroidal antiinflammatory agent, vitamin E and squalane and/or squalene.
In a fourth aspect, it is an object of the present invention to provide an external preparation for the treatment of dermatoses which is highly efficacious but reduced in side effects. In this fourth aspect, the present invention provides an external preparation for the treatment of dermatoses which comprises an antihistaminic agent, vitamin E and squalane and/or squalene.
In a fifth aspect, it is an object of the present invention to provide an external preparation for the treatment of dermatoses which is highly efficacious but reduced in side effects. In the fifth aspect, the present invention provides an external preparation for the treatment of dermatoses which comprises vitamin E, squalene and squalane.
DETAILED DISCLOSURE OF THE INVENTION
First, the present invention is described in detail in its first aspect.
The external preparation for the treatment of dermatoses according to the first aspect of the present invention comprises vitamin E and squalane.
The term “vitamin E” as used herein includes tocopherol (vitamin E) and derivatives thereof and, as examples thereof as listed in the Japanese Pharmacopoeia, there may be mentioned dl-&agr;-tocopherol, tocopherol acetate (vitamin E acetate ester), tocopherol succinate (vitamin E succinate ester), etc. As extrapharmacopoeial species, there may be mentioned, for example, &agr;-tocopherol, &bgr;-tocopherol, &ggr;-tocopherol, &dgr;-tocopherol, tocopherol nicotinate (vitamin E nicotinate ester), tocopherol phosphate (vitamin E phosphate ester) and tocopherol linolenate (vitamin E linolenate ester).
The term “squalane” as used herein means a saturated hydrocarbon derived by reduction from squalene which is a unsaturated hydrocarbon occurring in the liver oil of deep-sea fish, in particular sharks, or in vegetable oils such as olive oil, rice bran oil, wheat germ oil, sesame oil and cotton seed oil. The term also includes synthetic squalane obtained by synthesis from isoprene.
The above-mentioned vitamin E and squalane both have a curative effect on dermatoses, although the effect is weak, and even when the content of either one is low, a synergistic therapeutic effect can be produced by increasing the content of the other. Even when the contents of both are low, a distinct therapeutic effect can be produced by using the composition continuedly. As for the contents of both in the external preparation, therefore, vitamin E is used preferably in a proportion of 0.1 to 98% by weight, more preferably exceeding 2% by weight to not more than 98% by weight, still more preferably 5 to 60% by weight and most preferably 10 to 50% by weight, while squalane is used in an amount of 2 to 98% by weight, more preferably not less than 2% by weight to less than 98% by weight, still more preferably 5 to 60% by weight and most preferably 10 to 50% by weight.
The external preparation for the treatment of dermatoses according to the first aspect of the present invention may further contain a transdermal absorption enhancer in addition to vitamin E and squalane.
Said transdermal a

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