Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2001-10-15
2002-11-12
Reamer, James H. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S427000
Reexamination Certificate
active
06479532
ABSTRACT:
TECHNICAL FIELD
This invention relates to an antimycotic composition comprising pyrrolnitrin and at least one member selected from the group consisting of lanoconazole, butenafine or a salt thereof, and an allylamine-series antimycotic agent as active ingredients and, as such, finds application in the field of medical care.
BACKGROUND ART
Pyrrolnitrin is a drug having antimycotic activity which is represented by the chemical formula (1) given hereunder and has been used widely in a single-agent regimen or a-multiple-agent regimen including other antimycotic drugs.
Referring to the above multiple-agent regimen, there is known an antimycotic composition comprising pyrrolnitrin and an imidazole-series antimycotic agent, such as clotrimazole, as active ingredients (JP Kokai S61-56127).
Meanwhile, lanoconazole, butenafine, and terbinafine, an allylamine-series antimycotic agent, which are represented by the hereunder-given chemical formulas (2)~(4), respectively, are invariably drugs having antifungal activity and have been used in single-agent regimens.
However, there is not known any antimycotic composition comprising pyrrolnitrin and at least one member selected from the group consisting of lanoconazole, butenafine or a salt thereof, and terbinafine, which is an allylamine-series antimycotic agent, or a salt thereof as active ingredients.
While the above-mentioned antimycotic drugs each used alone display excellent antimycotic activity, development of a more potent antimycotic drug has been awaited for alleviation of side effects, improvement in the patient's compliance, and reduction in the cost of active substance bulk.
DISCLOSURE OF INVENTION
The inventors of this invention found that the combined use of pyrrolnitrin and lanoconazole, the combined use of pyrrolnitrin and butenafine or a salt thereof, and the combined use of pyrrolnitrin and an allylamine-series antimycotic agent, particularly terbinafine or a salt thereof, respectively result in a synergistic effect as compared with the effect of any of these drugs used independently, thus providing an antimycotic composition having potentiated antimycotic and fungicidal activities.
The antimycotic composition of this invention is characterized by comprising pyrrolnitrin and at least one member selected from the group consisting of lanoconazole, butenafine or a salt thereof, and an allylamine-series antimycotic agent as active ingredients.
Preferably, the antimycotic composition of this invention is characterized by comprising pyrrolnitrin and lanoconazole as active ingredients.
Also preferably, the antimycotic composition of this invention is characterized by comprising pyrrolnitrin and butenafine or a salt thereof.
The salt of butenafine for use in the above antimycotic composition of the invention includes the hydrochloride, among others.
Further preferably, the antimycotic composition of this invention is characterized by comprising pyrrolnitrin and an allylamine-series antimycotic agent.
The allylamine-series antimycotic agent for use in the above antimycotic composition of this invention is preferably terbinafine or a salt thereof.
The salt of terbinafine may for example be the hydrochloride.
BEST MODE FOR CARRYING OUT THE INVENTION
The ratio by weight of pyrrolnitrin to lanoconazole, that of pyrrolnitrin to butenafine or its salt, and that of pyrrolnitrin to the allylamine-series antimycotic agent in the specific antimycotic compositions of the invention are invariably 10:1~1:10, preferably 5:1~1:5, more preferably 2:1~1:2, and the ratio should be adjusted according to the type of antimycotic drug, the target pathogenic microorganism, the severity of illness, and other variables.
The dosage, as active substance, of said antimycotic compositions of the invention can be judiciously selected according to the dosage form, the ratio of active ingredients, the pathogenic microorganism to be dealt with, and severity of illness, among other variables, but generally these antimycotic compositions are respectively administered within the dose range of 0.01~10 mg/day, preferably 0.05~5 mg/day.
In addition to the above-mentioned active ingredients, each antimycotic composition of the invention may contain suitable amounts of an antipruritic, antiinflammatory, analgesic or local anesthetic agent, such as crotamiton, diphenhydramine, lidocaine, dibucaine, methyl salicylate, menthol, camphor, glycyrrhetinic acid, azulene, etc.; biocides, such as benzalkonium chloride, benzethonium chloride, chlorhexidine, phenol, chlorobutanol, iodine, etc.; a keratolytic or emolient, such as salicylic acid, diethyl sebacate, urea, sulfur, etc.; and/or an astringent or tissue-repairing agent, such as zinc chloride, allantoin, etc.
The dosage form for the antimycotic composition of this invention is not particularly restricted. Preferably, however, it includes various dosage forms for external application which are similar to those of hitherto-known antimycotic drugs, thus including solutions, gels, creams, ointments, aerosols, dusts, vaginal suppositories and so forth.
The antimycotic composition of this invention can be formulated with various pharmaceutical bases or carriers such as those mentioned below and, then, processed into the above dosage forms by the routine procedures, for example the protocols described in The Pharmacopoeia of Japan XIII.
To mention a few examples, vaseline, white wax, paraffin, polyethylene glycol, etc. can be formulated when the composition is to be molded into ointments; oils and fats, higher fatty acids, higher alcohols, fatty acid esters, purified water, polyhydric alcohols, emulsifiers, etc. can be added for the preparation of creams; carboxyvinyl polymers, water-soluble basic substances (alkali hydroxides, etc.), hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinyl alcohol, polyvinylpyrrolidone, purified water, lower alcohols, polyhydric alcohols, polyethylene glycol, etc. can be added for the preparation of gels; and lower alcohols, glycerol, propylene glycol, purified water, etc. can be added for the preparation of solutions.
The following test examples illustrate the effect of the antimycotic composition of this invention.
REFERENCES:
patent: 170139 (1986-02-01), None
patent: 7-309755 (1995-11-01), None
Kamimura Toshiaki
Obata Saburo
Yabuta Tsuguo
Fujisawa Pharmaceutical Co. Ltd.
Reamer James H.
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