JPH032846B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to an ointment base composition for athlete's foot, and particularly to a base composition capable of producing an ointment that has strong medicinal efficacy and is pleasant to the touch. Conventionally, vaseline and polyethylene glycol have been used as ointment bases for athlete's foot, but polyethylene glycol, which has a soft feel, is often used. In addition, the medicinal ingredients include salicylic acid, methyl salicylate, benzalkonium chloride,
These include boric acid, N-undecinoyl amino acid, nicotinic acid, cresol, and trimethylcetylammonium pentachlorophenate, but they can only be used in dilute concentrations because they are highly irritating to the affected area, and they do not show sufficient medicinal efficacy. I can't say that there is. The present inventors proposed a glycerin ester of a fatty acid having 2 to 14 carbon atoms as a therapeutic agent for athlete's foot with excellent bactericidal activity (Japanese Patent Application Laid-open No. 43211/1983). This glyceride has medicinal efficacy even when used alone, but when used in combination with other medicinal ingredients, it exhibits extremely significant medicinal efficacy and can be made into an excellent therapeutic agent for athlete's foot. However, although glyceride dissolves in petrolatum, it does not dissolve in polyethylene glycol, so it could only be used in petrolatum-based ointments that do not have a pleasant texture. Therefore, it has been desired to dissolve the above-mentioned medicinal ingredients in polyethylene glycol that is water-soluble and has a good feel, or to develop a base that has almost the same feel as polyethylene glycol. This invention was made in response to the above needs, and by combining specific polyalkylene glycols, glycerides can be dissolved, and by using this as a base, it can be combined with other medicinal ingredients. The object of the present invention is to provide an ointment base composition for athlete's foot that can be blended to produce a therapeutic agent for athlete's foot that is pleasant to the touch and has a strong medicinal effect. The present invention is an ointment base composition for athlete's foot, which contains the following three components A, B, and C as main components and does not contain water. (A) Mono-, di-, or triglycerides of fatty acids having 2 to 14 carbon atoms...2 to 20% by weight. (B) In the compound represented by the following general formula [], l
is 15 to 50, m is 20 to 250, and the average molecular weight per functional group is 2500 or more,
Or a compound obtained by esterifying some or all of the hydroxyl groups of the compound...5 to 30% by weight. (C) In the compound represented by the following general formula [], l
is less than 15 and m is 1 to 20, or a compound in which part or all of the hydroxyl groups of the compound are esterified...50 to 90% by weight. X [(AO) _l , (C ₂ H ₄ O) _n H] _o ... [] (wherein, X is a residue of a compound having 1 to 10 active hydrogens, A is C ₃ H ₆ , C ₄ H ₈ alone or a mixture thereof, l is 50 or less, m is 1 to 250,
n is 1-10. ) The fatty acids having 2 to 14 carbon atoms in (A) above include acetic acid, propionic acid, butyric acid, valeric acid, caproic acid, enanthic acid, caprylic acid, pelargonic acid,
Capric acid, undecanoic acid, lauric acid, tridecanoic acid, myristic acid, isobutyric acid, 2-ethylhexanoic acid, 3,5,5-trimethylhexanoic acid,
Examples include pivalic acid and neodecanoic acid. The above-mentioned component (A), glyceride, is synthesized by an esterification reaction of these fatty acids alone or in a mixture with glycerin, and can be used as a monoglyceride, diglyceride, or triglyceride alone or in a mixed state. In the above formula [], compounds having X as a residue include methyl alcohol, ethyl alcohol,
Butyl alcohol, octyl alcohol, lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl alcohol, oleyl alcohol, isostearyl alcohol, dimerized alcohol by Guerbet method (2-octyldodecanol, 2-decyltetradecanol, etc.), ethylene glycol, Propylene glycol, butylene glycol, hexylene glycol, dodecanediol, hexadecanediol, octadecanediol, glycerin, trimethylolpropane,
1,3,5-pentanetriol, erythritol, pentaerythritol, diglycerin, polyglycerin, dipentaerythritol, sorbitol, sorbitan, sorbide, glucose, fructose, mannose, xylose, methyl glucoside, trehalose, sucrose, diethanolamine, triethanolamine , ethylenediamine, etc. [] In the formula, n indicates the number of polyalkylene oxide polyethylene oxides directly bonded to X, l and m indicate the average number of moles of alkylene oxide and polyethylene oxide added in each polyalkylene oxide polyethylene oxide chain, l includes 0. Also, the order of addition of alkylene oxide and ethylene oxide in the polyalkylene oxide polyethylene oxide chain is not limited to the order shown in the formula [].
The formula indicates that these are block or random polymers. The compound of the formula [] uses the above compounds having X as a residue alone or in combination as a starting material, and
Produced by adding an alkylene oxide represented by AO and then adding ethylene oxide, or adding these in the reverse order, or adding these simultaneously, or further adding only ethylene oxide when l is 0. be done. Further, esters of part or all of this compound can be produced by conventional esterification. Among the compounds of formula [] obtained as above, those with large amounts of alkylene oxide and ethylene oxide added and within the range described in (B) above are (B)
component, and the amount of these additions is small, and the above-mentioned
(C) Those within the range described are considered to be component (C). this house
Component (C) includes those in which 1 is 0, and also includes polyethylene glycol having an average molecular weight of 150 to 800, which is commonly used as a base. These components (B) and (C) are blended with the component (A) to form a base composition for athlete's foot. Each of these ingredients is heated to approximately 80°C,
Mix uniformly by stirring. The same applies when component (C) is the polyethylene glycol described above. In the present invention, the number of carbon atoms in the fatty acid in component (A) is limited because outside this range, the bactericidal effect is significantly inferior, which is inconvenient, and if it exceeds the upper limit, the base may become hard. It is. The l and m of component (B) are limited because if they are smaller than the range mentioned above, it is not possible to mix the components (A) and (C) uniformly, and if they are larger than the range mentioned above. This is because the melting point and viscosity of the composition increase and the ointment becomes hard, which is disadvantageous. The reason why l and m of component (C) are limited is that if it is smaller than the above range, the melting point of the composition will be too low and it will have fluidity, and if it is larger than the above range, This is because the melting point and viscosity of the composition increase and the ointment becomes hard, which is disadvantageous. The mixing ratio of each component (A), (B), and (C) is limited as follows:
This is because, outside the above range, a uniform composition cannot be obtained, and the ointment may become fluid or hard. The ointment base composition of the present invention can be formulated as a therapeutic agent for athlete's foot by incorporating medicinal ingredients for athlete's foot and other ingredients if necessary. The medicinal ingredients include those mentioned above. Further, for the purpose of adjusting the hardness of the ointment, ethanol, propylene glycol, glycerin, dipropylene glycol, diglycerin, etc. can be blended. Although the amount of water originally contained in each component is permissible, the formulation can be formulated without adding water. The ointment base composition for athlete's foot of the present invention can use a medicinal glyceride as a base by using a specific polyalkylene glycol in combination; The therapeutic agent for athlete's foot has an extremely strong medicinal effect and is appropriately soft, so that it can be made into an ointment that feels good when applied. Furthermore, since water is not added, there is no occurrence of fatty acid odor due to hydrolysis of component (A), and the composition does not separate into two layers, maintaining a transparent and uniform state. Examples of the present invention will be described below. Example 1 Components (A), (B), and (C) shown in Table 1 were uniformly mixed to prepare an ointment base. In Table 1, the number of carbon atoms in the fatty acid of component (A) is shown in addition to C on the left side. Also
Components (B) and (C) do not have formulas corresponding to formula [], for example, X in product 1 of the present invention is propylene oxide, but in order to make the structure of the compound easier to understand, is displayed. The numbers appended to these alkylene oxides are the average number of moles added, and % is weight %. The compatibility, hardness, and melting point of the products of the present invention and comparative products prepared as described above were measured. The test method is to first place 100g of the composition in a 300ml beaker, heat it to 80°C, and stir until it becomes uniform. When the composition becomes homogeneous, stop stirring and slowly cool the beaker to 20°C to solidify the composition. In this state, the compatibility and hardness are determined, and the melting point is also measured. The criteria for determining compatibility are as follows. ○: Becomes a uniform state. ×: Separated into two or more layers. The criteria for determining hardness are as follows. ○: Soft. ×: Hard or flowing at 30℃. The test results are shown in Table 2. From the above results, it can be seen that the product of the present invention is superior to the comparative product in terms of compatibility and hardness, and has a melting point suitable for use as an ointment base.

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[Table] Next, water was added to each composition of invention products 1 to 12 in Table 1 so that the water content was 30% by weight. The compositions of products 1 to 12 of the present invention and their 30% water content products were mixed at 70°C for 30 minutes and then allowed to stand at 50°C for 30 days, and their states were examined. The results are shown in Table 3, and the composition of the present invention remained transparent and uniform, and did not generate any fatty acid odor. On the other hand, the product containing 30% water by weight caused separation and produced a fatty acid odor. From the above results, it can be seen that it is not preferable for the composition of the present invention to contain water. Example 2 An ointment for athlete's foot was manufactured using the following formulation. (Formulation) Salicylic _acid ...2.0% by weight Cetyltrimethylammonium pentachlorophenate _1.0 % by weight _C8 triglyceride 10.0% by weight HO _{( C2H4O} ) ₁₀₀ ( _C3H6O ) ₇₀ ( _C2H4O ) ₁₀₀ H
12.0% by weight HO (C ₂ H ₄ O ₉ )H 74.5% by weight (Manufacturing method) All ingredients are heated to 80°C and dissolved, and stirred until a uniform transparent liquid is obtained. Then cool slowly. The melting point of the ointment obtained above is 40°C,
It was soft, had a relatively low viscosity when applied, had a refreshing feel, and had excellent therapeutic effects.

Claims (1)

[Scope of Claims] 1. An ointment base composition for athlete's foot, characterized in that it contains the following three components A, B, and C as main components and does not contain added water. (A) Mono-, di-, or triglycerides of fatty acids having 2 to 14 carbon atoms...2 to 20% by weight. (B) In the compound represented by the following general formula [], l
is 15 to 50, m is 20 to 250, and the average molecular weight per functional group is 2500 or more,
Or a compound obtained by esterifying some or all of the hydroxyl groups of the compound...5 to 30% by weight. (C) In the compound represented by the following general formula [], l
is less than 15 and m is 1 to 20, or a compound in which part or all of the hydroxyl groups of the compound are esterified...50 to 90% by weight. X [(AO) _l , (C ₂ H ₄ O) _n H] _o ... [] (wherein, X is a residue of a compound having 1 to 10 active hydrogens, A is C ₃ H ₆ , C ₄ H ₈ alone or a mixture thereof, l is 50 or less, m is 1 to 250,
n is 1-10. ) 2 The fatty acids in component A are acetic acid, propionic acid, butyric acid, valeric acid, caproic acid, enanthic acid, caprylic acid, pelargonic acid, capric acid, undecanoic acid, lauric acid, tridecanoic acid, myristic acid, isobutyric acid, and 2-ethyl hexanoic acid, 3,5,
The ointment base composition for athlete's foot according to claim 1, which is one or more selected from 5-trimethylhexanoic acid, pivalic acid, and neodecanoic acid. 3 [In the formula, X is methyl alcohol, ethyl alcohol, butyl alcohol, octyl alcohol, lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl alcohol,
Oleyl alcohol, isostearyl alcohol, 2-octyldodecanol, 2-decyltetradecanol, ethylene glycol, propylene glycol, butylene glycol, hexylene glycol, dodecanediol, hexadecanediol, octadecanediol, glycerin, trimethylolpropane, 1, 3,5-pentanetriol, erythritol, pentaerythritol, diglycerin, polyglycerin, dipentaerythritol, sorbitol, sorbitan, sorbide, glycose, fructose, mannose, xylose, methyl glucoside, trehalose, sucrose, diethanolamine, triethanolamine and ethylenediamine Claim 1, which is one or more residues selected from
The ointment base composition for athlete's foot according to item 1 or 2. 4. The ointment base composition for athlete's foot according to any one of claims 1 to 3, wherein component C is polyethylene glycol having an average molecular weight of 150 to 800.