Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1996-01-05
2000-01-25
Fay, Zohreh
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514399, 514912, A61K 3150, A61K 31415
Patent
active
060179201
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to an antifungal composition for external use containing as an active ingredient an antifungal agent having a high affinity for keratin. More particularly, the present invention relates to an antifungal composition for external use being retentive in the stratum corneum, which contains one or more oily liquid substances selected from the group consisting of methyl salicylate, glycol salicylate, crotamiton, and peppermint oil or menthol, in order to enhance the penetration into the stratum corneum of the active antifungal agent having a high affinity for keratin, by which said antifungal agent is more retentive in the stratum corneum.
BACKGROUND ART
In superficial mycosis, fungi invade mainly into the epidermal stratum corneum, and grow therein. Thus, in order to exhibit excellent pharmacological activities in the treatment of superficial mycosis, antifungal agents should stay in a high concentration in the infected epidermal stratum corneum for a prolonged time, in addition to their potent antifungal activity.
Recently, in order to achieve the above purpose, there have been developed and practically used antifungal agents having a high affinity for keratin, which exhibit clinical effects thereof in the treatment of superficial mycosis only by a single application per day. However, in order to obtain a sufficient affinity for the epidermal stratum corneum, antifungal agents should be formulated so that they can penetrate into the epidermal stratum corneum. However, these antifungal agents having a high affinity for keratin are not readily soluble, and it is difficult to increase their solubility when incorporated in the base. As a result, the penetration into the epidermal stratum corneum of these agents is not sufficient so as to form an antifungal composition for external use which is retentive in the stratum corneum using a high affinity for keratin of the active antifungal agent per se at the maximum.
DISCLOSURE OF INVENTION
The present inventors have intensively studied in order to improve the penetration into the stratum corneum of antifungal agents having a high affinity for keratin and the retentivity thereof, and have found that when formulating a composition for external use by incorporating one or more oily liquid substances selected from the group consisting of methyl salicylate, glycol salicylate, crotamiton, and peppermint oil or menthol, the active antifungal agents having a high affinity for keratin show an improved penetration into the stratum corneum as well as an improved retentivity in the stratum corneum, and finally have accomplished the present invention.
More particularly, it has been found that in the preparation of compositions for external use containing as an active ingredient an antifungal agent having a high affinity for keratin, by incorporating with methyl salicylate, glycol salicylate, crotamiton, peppermint oil or menthol, which can dissolve said antifungal agents well and shows a good penetration into the stratum corneum, the penetration into the epidermal stratum corneum of said antifungal agents is enhanced, and further said antifungal agents are more tightly bound to the components of the epidermal stratum corneum, and fixed thereon.
In the composition for external use of the present invention, one or more oily liquid substances selected from the group consisting of methyl salicylate, glycol salicylate, crotamiton, and peppermint oil or menthol can be incorporated thereto by adding and mixing them simultaneously when an antifungal agent having a high affinity for keratin is mixed into a conventional base for external use. Preferably, however, an antifungal agent having a high affinity for keratin is previously dissolved by using various solvents during which the above mentioned oily liquid substances such as methyl salicylate, etc. are added in an amount sufficient for completely dissolving said antifungal agent, and then the resulting solution is incorporated into a conventional base for external use by a conventiona
REFERENCES:
patent: 4636520 (1987-01-01), Umio et al.
Chemical Abstract 98:185586 (1982) . Kamishita.
Kamishita Takuzo
Miyazaki Takashi
Fay Zohreh
Toko Yakuhin Kogyo Kabushiki Kaisha
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