JP2000086500A - Aerosol type ointment composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an aerosol type ointment hardly scattering blowout products, scarcely causing the flow of a stuck liquid on application, and having a high adhesion rate to applied sites. SOLUTION: This aerosol type ointment composition comprises a stock solution containing a mineral oil and a thickener, and a propellant. The stock solution has a viscosity of 1,000-200,000 cps at 20 deg.C. The thickener is selected from paraffin waxes, fats, fatty oils, vegetable extraction waxes, animal extraction waxes, higher alcohols and hydrocarbon-based polymers. The mineral oil is preferably a hydrocarbon-based compound which is liquid at in a range of 0 deg.C to 60 deg.C. The propellant is selected from a liquefied petroleum gas, dimethyl ether and compressed gases. The stock solution and the propellant are preferably used in a weight ratio of 30:70 to 70:30.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an aerosol-type ointment composition whose contents are discharged as an ointment-like substance or a gel-like substance.

[0002]

2. Description of the Related Art Ointments have been known as one of the external preparations applied to the skin of the human body and the like. Actually, ointments, quasi-drugs or cosmetics containing the drug as an active ingredient are actually used. It is frequently used as such. Conventionally, ointments are usually provided as an emulsion in which a water-soluble component and an oil-soluble component are emulsified by an appropriate activator or emulsifier, or as a high-viscosity composition in which an oil-soluble component is thickened by a thickener. Have been.

[0003] However, the conventional ointment has low storage stability and oil components may be separated during storage, and so-called liquid spreading (spreadability) when applied to a target site for hands is low. In addition, there is a problem to be improved in that practical use is not always preferable.

[0004]

SUMMARY OF THE INVENTION The present invention has been made to formulate an aerosol formulation so that an ointment can be conveniently applied. That is, a basic object of the present invention is to provide an aerosol-type ointment composition. Further, a specific object of the present invention is to provide an aerosol-type ointment composition which has a small amount of spouts at the time of application, a small liquid flow (liquid dripping) of the adhered matter, and a high adherence rate to an applied place. .

[0005]

The aerosol-type ointment composition according to the present invention comprises a stock solution containing mineral oil and a thickener,
And a propellant, and the stock solution has a viscosity at 20 ° C. of 1,000 to 200,000 cps.

[0006] In the above, the thickener contained in the stock solution is preferably at least one selected from paraffin wax, fats and oils, plant-extracted wax, animal-extracted wax, higher alcohols and hydrocarbon polymers. . Also,
It is preferable that the hydrocarbon polymer as a thickener is at least one of polyethylene and polyisobutylene having a weight average molecular weight of 3500 to 26000.
Further, the mineral oil contained in the stock solution is preferably a liquid hydrocarbon-based compound in the range of 0 ° C to 60 ° C.

[0007] The propellant in the aerosol-type ointment composition of the present invention is preferably at least one selected from liquefied petroleum gas, dimethyl ether and compressed gas. Then, the ratio between the stock solution and the propellant is 30:70 by weight.
It is preferably within the range of 70:30.

In such an aerosol-type ointment composition, the stock solution contains a mineral oil and a thickener and has a relatively high specific viscosity. Coexists, the contents have appropriate fluidity as a whole, and suitable injection characteristics can be obtained.

In addition, when the propellant is vaporized when sprayed or discharged, the viscosity of the stock solution is in a specific range, so that the stock solution is less scattered and the deposits at the application site are in a good ointment form. Or, it becomes gel-like, and there is no liquid dripping, and suitable liquid spreading characteristics can be obtained.

[0010]

BEST MODE FOR CARRYING OUT THE INVENTION The aerosol-type ointment composition of the present invention basically comprises a stock solution containing a mineral oil and a thickener, and a propellant, and the stock solution has a temperature of 20 ° C.
Is 1000 to 200,000 cps. The stock solution contains, in addition to the mineral oil and the thickener, an active ingredient and various additives depending on the final use or as necessary.

The stock solution contains a mineral oil and a thickener as essential components, and has a specific viscosity characteristic of a viscosity at 20 ° C. of 1,000 to 200,000 cps. In the actual composition, the kind of the mineral oil and the thickener to be used and their ratio are determined so that the condition for the viscosity is satisfied. The viscosity of the stock solution is 50 at 20 ° C.
It is particularly preferable that it is 00 to 150,000 cps.
Here, "viscosity" means the rotor N measured by a BH type viscometer.
o. 7 refers to the value measured at a temperature of 20 ° C. after 60 seconds.

If the viscosity of the undiluted solution is excessive, there is a high possibility that the aerosol product will not be able to obtain suitable ejection characteristics or ejection characteristics. On the other hand, if the viscosity of the undiluted solution is too low, the ejected matter is not likely to be in a suitable ointment or gel form. That is, at the time of application, the squirt is more scattered, causing a liquid flow of the adhering matter, and as a result, the adhering rate to the application location is lower.

As a specific example of the mineral oil, one or more selected from petroleum hydrocarbon compounds, tar hydrocarbon compounds, and plant hydrocarbon compounds can be used. It is preferable that the compound is a hydrocarbon compound which is liquid in the range of ° C. Specific examples of such a substance include mineral spirit, liquid paraffin, and the like.

In the present invention, the content of the mineral oil is determined so long as the stock solution containing the thickener has the above-mentioned predetermined viscosity characteristics, and at the same time, can obtain favorable injection characteristics in relation to the propellant. Although not particularly limited, it is usually 60 to 95% by weight, preferably 70 to 95% by weight in the stock solution.
90% by weight.

[0015] A stock solution is formed together with the mineral oil described above, and as a thickening agent contained for adjusting the viscosity of the stock solution, paraffin wax, oils and fats, plant-extracted wax, animal-extracted wax, higher alcohol and hydrocarbon-based At least one or two or more selected from polymers are used. The use ratio of this thickener may be a ratio at which the obtained stock solution has a desired viscosity state.

The paraffin wax as a thickener is
Those in which carbon atoms are bonded in a linear or branched manner, particularly those having a melting point of 50 ° C. or more are preferably used. The content of the paraffin wax in the entire composition is usually 1.0 to 30% by weight, preferably 5 to 30% by weight.
To 15% by weight.

Oils and fats are a general term for oils and fats, and specific examples thereof include cocoa butter and coconut oil. Particularly, they are solids at ordinary temperature and have a melting point of 25 ° C. or more. Are preferably used. The content of the fats and oils in the entire composition is usually 1.0 to 5
0% by weight, preferably 10 to 25% by weight.

Specific examples of the plant-extracted wax include carnauba wax and candelilla wax.
Those having a melting point of 50 ° C. or more are preferably used. The content of the plant-extracted wax in the entire composition is usually 1.0 to 50% by weight, preferably 10 to 25% by weight.
It is said.

Specific examples of animal-extracted wax include beeswax, whale wax, lanolin and the like, and those having a melting point of 50 ° C. or more are preferably used. The content of the animal-extracted wax in the entire composition is usually
The content is 1.0 to 50% by weight, preferably 10 to 25% by weight.

The higher alcohol is an aliphatic alcohol having 6 or more carbon atoms, and specific examples thereof include oleyl alcohol, cetyl alcohol, stearyl alcohol, and behenyl alcohol. The content of the higher alcohol in the entire composition is usually 1.0 to 50% by weight, preferably 10 to 25% by weight.
% By weight.

The hydrocarbon polymer is one or both of polyethylene and polyisobutylene having a weight average molecular weight of 3500 to 26000, and is commercially available, for example, under the trade name of "Plastibase". The content of the hydrocarbon polymer in the whole composition is usually 1.0 to 30% by weight, preferably 5 to 20% by weight.
% By weight.

An active ingredient or an additive can be added to the stock solution as described above. Specifically, various compounds and mixtures can be used in an appropriate form depending on the specific use of the aerosol-type ointment composition. Examples of the active ingredient or additive include, for example, anti-inflammatory analgesic, antipruritic, antifungal, bactericide, anti-purulent disease agent, refreshing agent, antioxidant, solubilizer, fragrance, dye, and others. it can. These substances can be used alone or in combination of two or more.

Specific examples of the active ingredient or additive include:
Indomethacin, L-menthol, aloe extract, silk extract, hinoki oil, ultraviolet absorber, bufexamac,
Glycyrrhetinic acid, acrinol, zinc oxide, dibucaine hydrochloride, allantoin, lidocaine, isopropylmethylphenol, potassium iodide, benzalkonium chloride, penicillin V, tetracycline hydrochloride, fradiomycin, kanamycin, peppermint oil, diisopropyl adipate, propylene glycol, polyvinyl Alcohol, isopropyl myristate, and the like can be mentioned.

In the present invention, liquefied petroleum gas (LPG), dimethyl ether (DME), compressed gas, or two or more of them are used as the propellant constituting the aerosol-type ointment composition together with the stock solution. Here, the liquefied petroleum gas is usually a mixture of butane and propane, and it is useful to use butane alone. Dimethyl ether is used alone or with liquefied petroleum gas. Examples of the compressed gas include carbon dioxide gas, nitrogen gas, compressed air and nitrous oxide gas, and one or more of them are used alone or together with at least one of liquefied petroleum gas and dimethyl ether.

The undiluted solution and the propellant are filled in appropriate amounts in a pressure-resistant container for aerosol having a spray valve, whereby an aerosol product containing the aerosol-type ointment composition is obtained. Here, the ratio between the stock solution and the propellant is not particularly limited,
Usually, the weight ratio is 70:30 to 30:70, preferably 60:40 to 40:60.

When an aerosol product filled with the aerosol-type ointment composition of the present invention is used to spray the ointment composition as a content through a spray valve toward, for example, the human body or other application site, the effect of the propellant is obtained. As a result, the stock solution becomes a fine mist or mist, and adheres to the application location. However, since the viscosity of the undiluted solution at a temperature of 20 ° C. of 1000 to 200,000 cps becomes an ointment-like or gel-like deposit, scattering of the ejecta at the time of application is small, and the liquid flow of the deposit is small. , The adhesion rate to the application location is high. And the undiluted solution
By containing a liquid mineral oil in a normal state, good liquid spreading properties can be obtained, and therefore, it can be used very suitably as an external preparation.

The aerosol-type ointment composition of the present invention, for example, is applied as a topical medicine, a quasi-drug, a cosmetic, or a cosmetic containing a drug as an active ingredient by discharging the necessary amount to a desired application site and attaching it. It can be used very conveniently in practice.

[0028]

Hereinafter, embodiments of the present invention will be described.
The present invention is not limited by these. Examples 1 to 12 According to the formulation shown in Table 1, a mineral oil and a thickener were mixed with an active ingredient to prepare a stock solution. An ointment aerosol product was manufactured by filling in a container. As the valve in the pressure-resistant container, a valve having a stem diameter of 0.45 mm and a housing having a hole diameter of 1.00 mm was used. The weight average molecular weight of polyethylene as a thickener in Table 1 is 24,000, and the weight average molecular weight of polyisobutylene is 20,000.
The viscosity of the stock solution is a value at a temperature of 20 ° C.

Evaluation of Aerosol Composition Each of the aerosol products obtained in the above Examples and Comparative Examples was subjected to an injection test, and the adhesion rate of ejected substances and the feeling of use were examined. That is, after holding each aerosol product in a thermostat at a temperature of 25 ° C. for 30 minutes or more, a vertically fixed flat metal plate having a length of 20 cm and a width of 20 cm is applied, and the aerosol product is located at a position 10 cm away from this. From about 3 seconds, and the ratio of the actual amount of adhesion to the amount of stock solution injected at that time was determined as the adhesion ratio. Specifically, weight loss x (g) and amount of adhesion of aerosol product (increase of metal plate)
y (g) was measured, and the value of the ratio (y / ax) was determined with the ratio of the stock solution in the entire contents as a (% by weight). A large numerical value of the adhesion ratio means that the degree of scattering of the stock solution is small.

Further, 10 panelists were allowed to actually use each of the aerosol products described above, and the overall feeling of use including the presence or absence of liquid dripping was evaluated at that time. Was determined. Table 2 also shows these results.

Comparative Examples 1 to 12 In each of the above Examples 1 to 12, a stock solution was prepared in the same manner except that the thickener was removed, and in the same manner as in the above Examples except that this stock solution was used. An aerosol product was manufactured, the same spray test was performed, and the adhesion rate and usability were evaluated. Table 3 shows the results of the formulation and the evaluation.

[0032]

[Table 1]

[0033]

[Table 2]

[0034]

[Table 3]

From the results shown in Table 2, it is clear that the aerosol-type ointment compositions according to the examples of the present invention can obtain a very high adhesion rate and a good feeling in use. On the other hand, from the results in Table 3, it is understood that, in the aerosol-type ointment composition of the comparative example, the viscosity of the stock solution was not within the predetermined range, so that a high adhesion rate was not obtained and the feeling of use was not good. .

[0036]

As described above, according to the aerosol-type ointment composition of the present invention, the stock solution has a relatively high viscosity because it contains a mineral oil and a thickener. In, the coexistence of the propellant causes the contents to have appropriate fluidity as a whole and obtain suitable ejection characteristics, and also when the propellant is vaporized when ejected or discharged. Regardless, the dispersion of the undiluted solution is small, and the deposits at the application site are in a good ointment or gel form, and there is no liquid dripping, and suitable liquid spreading properties can be obtained.

Claims (6)

[Claims] 1. A stock solution containing a mineral oil and a thickener, and a propellant, wherein the stock solution has a viscosity at 20 ° C. of 1,000 to 200,000 c.
An aerosol-type ointment composition characterized by ps. 2. The thickener contained in the stock solution is at least one selected from paraffin wax, oils and fats, plant extraction wax, animal extraction wax, higher alcohols and hydrocarbon polymers. The aerosol-type ointment composition according to claim 1, 3. The aerosol-type ointment according to claim 2, wherein the hydrocarbon polymer as a thickener is at least one of polyethylene and polyisobutylene having a weight average molecular weight of 3500 to 26000. Composition. 4. Mineral oil contained in the undiluted solution is 0 to 60 ° C.
The aerosol-type ointment composition according to any one of claims 1 to 3, wherein the composition is a liquid hydrocarbon-based compound in the range of ° C. 5. The aerosol-type ointment composition according to claim 1, wherein the propellant is at least one selected from liquefied petroleum gas, dimethyl ether and compressed gas. 6. The ratio between the stock solution and the propellant is 30: 7 by weight.
The aerosol-type ointment composition according to any one of claims 1 to 5, wherein the composition is within a range of 0 to 70:30.