Compositions for percutaneous administration

Details Compositions for percutaneous administration Compositions for percutaneous administration

1993-02-24

1994-06-14

Goldberg, Jerome D.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514947, A61K 3155

Patent

active

053210220

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

This invention relates to compositions for percutaneous administration of 1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1H-1, 4-diazepin-1-yl)-1H-benzimidazole.


PRIOR ART

1-(2-Ethoxyethyl)-2-(hexahydro-4-methyl-1H-1, 4-diazepin-1-yl)-1H-benzimidazole (hereinafter referred to as emedastine) is a compound of the following formula: ##STR1## which has a strong antihistaminic activity, and is useful for the prophylaxis and treatment of diseases caused by histamine such as allergic bronchial asthma, allergic dermatitis and allergic rhinitis, and the like (cf: U.S. Pat. No. 4430343).
The above mentioned U.S. Patent discloses that an ointment for percutaneous preparation containing emedastine or a pharmaceutically acceptable salt thereof can be prepared by using a conventional base, and in Examples thereof there is disclosed an ointment comprising emedastine difumarate and polyethylene glycol.
The above mentioned ointment comprising emedastine difumarate and polyethylene glycol is suitable, for example, for local treatment of allergic dermatitis, but in this ointment, the percutaneous absorption of emedastine is not satisfactory (cf: Experiments 1-2 described hereinbelow), and hence, the above mentioned ointment is not suitable enough for treatment based on the systemic action of emedastine, for example, for treatment of allergic bronchial asthma.
The present inventors have studied to provide compositions for percutaneous administration of emedastine based on the systemic action thereof, that is, compositions for percutaneous administration having a high percutaneous absorption ability of emedastine. An object of this invention is to provide compositions for percutaneous administration of emedastine having an excellent percutaneous absorption ability.


DISCLOSURE OF THE INVENTION

The present inventors have attempted various experiments, and found that when a composition comprising emedastine and aliphatic monocarboxylic acid lower alkyl esters or aliphatic dicarboxylic acid di-lower alkyl esters is percutaneously administered, the percutaneous absorption ability of emedastine is excellent, and have accomplished this invention.
That is, the object of this invention is to provide compositions for percutaneous administration of emedastine, which comprises emedastine and aliphatic monocarboxylic acid lower alkyl esters or aliphatic dicarboxylic acid di-lower alkyl esters.
The compositions of this invention can be prepared by mixing with stirring emedastine and the above mentioned esters at room temperature, if necessary, under warming.
The compositions of this invention can also be prepared by adding an aqueous solution of about one equivalent of an organic base (cf: triethanolamine, ethanolamine, etc.) or an inorganic base (cf: sodium hydroxide, sodium carbonate, etc.) to a mixture of a pharmaceutically acceptable salt of emedastine and the above mentioned esters, followed by mixing the mixture.
The aliphatic monocarboxylic acid lower alkyl esters include, for example, C.sub.1 -C.sub.4 alkyl esters of an aliphatic saturated monocarboxylic acid having 6-18 carbon atoms or C.sub.1 -C.sub.4 alkyl esters of oleic acid, preferably aliphatic saturated monocarboxylic acid C.sub.1 -C.sub.4 alkyl esters wherein the total number of carbon atoms is 8-22, and oleic acid C.sub.1 -C.sub.4 alkyl esters. These esters are, for example, ethyl octanoate, ethyl decanoate, ethyl hexanoate, ethyl laurate, ethyl myristate, isopropyl myristate, butyl myristate, isobutyl palmitate, butyl stearate, methyl oleate, ethyl oleate, butyl oleate, and the like.
The aliphatic dicarboxylic acid di-lower alkyl esters include, for example, di-(C.sub.1 -C.sub.4) alkyl esters of an aliphatic dicarboxylic acid having 6-10 carbon atoms, preferably ones wherein the total number of carbon atoms is 10-14, and are, for example, diethyl sebacate, diisopropyl adipate, diethyl suberate, diethyl adipate, and the like.
The above mentioned esters can be used either alone or in the form of a mixture of two or more esters. The amount thereof is usually

REFERENCES:
patent: 4299826 (1981-11-01), Luedders
patent: 4430343 (1984-02-01), Iemura et al.

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