Antifungal composition

a technology of composition and antifungal agent, applied in the field of pharmaceutical composition, can solve the problems of (i) poor solubility of compounds represented by the general formula in an aqueous medium

Inactive Publication Date: 2010-07-08
POLA PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0016]According to the present invention, there may be provided a system for compensating a change in the bioavailability of compounds represented by the general formula (1) due to a variation in the formulation components.

Problems solved by technology

For example, summer is a season in which the disease easily reoccurs, and thus, repetitive treatments are required.
However, the compounds represented by the general formula (I) are poorly-soluble in an aqueous medium in terms of solubility, and must be formulated by using a solubilizing agent.
As a result, the control of a variation in the bioavailability of medicaments to be caused by such a solubilizing agent has been the single and greatest problem in a formulation study.

Method used

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Examples

Experimental program
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Effect test

example 1

[0035]Skin agents 1 to 5 for external use, each of which is the pharmaceutical composition of the present invention, were prepared in accordance with the following prescription. That is, luliconazole was dissolved by adding an appropriate amount of ethanol, and to the resulting solution, triacetin and glucono-δ-lactone were added and uniformly dispersed. After that, hydroxypropylcellulose was gradually added, and water was further added to obtain homogenous skin agents for external use. Any of those agents had a viscosity of 100 to 800 mPa·s (viscometer: RE80R manufactured by Toki Sangyo Co., Ltd., and conditions for viscosity measurement: cone angle; 0.8°, cone radius; 2.4 cm, rotation frequency; 10 rpm, and temperature; 25° C.), was not so dripping, and thus was suited as a formulation for seborrheic dermatitis to be administered to the hair line and the like. Further, those agents were free of ingredients strongly exhibiting solvent characteristics likemethyl ethyl ketone (MEK) a...

example 2

[0043]In the same manner as in Example 1, Skin agent 6 for external use as the pharmaceutical composition of the present invention was prepared in accordance with the following prescription. The concentration of luliconazole in the horny cell layer at 2 hours after the application of the agent was 4.532 μg / cm2, and the concentration in Comparative Example 1 in which propylene glycol in the preparation was replaced by ethanol was 0.221 μg / cm2. The S-E isomer measured by HPLC after harsh preservation (60° C., 1 week) was 1.65% in Skin agent 6 for external use, which was higher compared with 1.45% in Comparative Example 1. Propylene glycol is found to be usable as an ingredient for promoting the absorption to the horny cell layer.

TABLE 6Ingredientw / v %Luliconazole1Propylene glycol50EthanolAppropriate amountTotal100 mL

example 3

[0044]In the same manner as in Example 1, Skin agent 7 for external use as the pharmaceutical composition of the present invention was prepared in accordance with the following prescription. The concentration of luliconazole in the horny cell layer at 2 hours after the application of the agent was 0.584 μg / cm2, and the concentration in Comparative Example 2 in which 2-ethyl-1,3-hexanediol in the preparation was replaced by ethanol was 0.950 μg / cm2. The S-E isomer measured by HPLC after harsh preservation (60° C., 1 week) was 1.06% in Skin agent 7 for external use, which was higher compared with 0.38% in Comparative Example 2. 2-ethyl-1,3-hexanediol is found to be usable as an ingredient for inhibiting the absorption to the horny cell layer.

TABLE 7Ingredientw / v %Luliconazole1Hydroxypropylcellulose1.5Water202-ethyl-1,3-hexanediol5EthanolAppropriate amountTotal100 mL

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Abstract

Disclosed is a pharmaceutical composition for antifungal use, comprising: 1) one or more compounds selected from compounds represented by the general formula (1) below and physiologically acceptable salts thereof; 2) one or more compounds selected from polypropylene glycol, diesters of dibasic acids, triacetin, 2-ethyl-1,3-hexanediol, lauromacrogol, and polyoxyethylene-polyoxypropylene glycol; and 3) one or more compounds selected from glucono-δ-lactone, propylene glycol, glycerin, and lactic acid. General formula (1) (In the formula, X represents a halogen or hydrogen).
wherein X represents a halogen or hydrogen.

Description

TECHNICAL FIELD[0001]The present invention relates to a pharmaceutical composition, and more specifically, to a pharmaceutical composition for antifungal use.BACKGROUND ART[0002]In Japan having a hot and humid climatic property, measures against mycoses caused by pathogenic fungi are a particularly important pharmaceutical theme. Reoccurrence of such a disease is repeatedly caused by remaining living microbes even if the disease appears to have been perfectly cured. For example, summer is a season in which the disease easily reoccurs, and thus, repetitive treatments are required. Therefore, an antifungal agent having an excellent medicinal effect has been demanded. Further, simultaneously, mycoses include those which develop on hand and foot portions such as tinea pedis and tinea unguium, those which develop on the body skin such as tinea, and those which develop on the scalp such as seborrheic dermatitis, and there is also a demand for development of a versatile dosage form which c...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A01N43/50A01P3/00
CPCA61K9/0014A61K47/10A61K47/12A61K47/14A61K47/22A61K47/32A61K47/34A61K31/4178A61K47/26A61P17/08A61P31/10
Inventor MASUDA, TAKAAKINISHIDA, NAOTOKOBAYASHI, NAOKOSASAGAWA, HIDEAKI
Owner POLA PHARMA
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