JP2729244B2 - Aerosol products - Google Patents

Description

Description: TECHNICAL FIELD The present invention relates to an aerosol product, and more particularly, to an aerosol product used for application to humans, animals and the like.

[Conventional technology]

Conventionally, aerosol products applied in the form of a mist include antiperspirants, repellents, anti-inflammatory analgesics and the like using Freon gas. In addition, as the aerosol product using no chlorofluorocarbon gas, for example, an aerosol product using an aerosol composition as described in JP-A-54-32185 has been developed.

[Problems to be solved by the invention]

However, aerosol products that use CFCs (chlorofluorocarbons) as a propellant do not decompose into the stratosphere because CFCs are released into the atmosphere and themselves are difficult to decompose. In recent years, destruction of the ozone layer by releasing chlorine has been regarded as a problem. Therefore, development of an aerosol product using a propellant that does not destroy the ozone layer is desired.
On the other hand, an aerosol product which does not use chlorofluorocarbon as a propellant as described in JP-A-54-32185 has been developed, but this aerosol product separates liquefied petroleum gas (hereinafter referred to as LPG). It is made for the purpose of obtaining a fine mist spray state by mixing and spraying the gas phase of LPG in the content more, and it has the disadvantage that the mist scatters around before reaching the application surface At the same time, flammable liquefied gas dimethyl ether (hereinafter referred to as DME) is used together with alcohol and water, and when this DME adheres to human skin and evaporates rapidly, water and oil on the skin surface are removed. In some cases, the skin surface was whitened and the skin was almost one step before frostbite.

[Means for solving the problem]

Therefore, the present inventors have proposed to use DME instead of Freon gas as a propellant for aerosol composition in aerosol products.
A flammable gas containing as a main component is used, and a volatilization inhibitor having a high flash point is added to the aerosol composition, and the injection amount of the aerosol composition is regulated to a predetermined value to notify the Ministry of International Trade and Industry. Satisfies the requirements for slight flammability specified in No.557 (explosion concentration: 0.25 g or more, flame length is less than 25 cm, hereinafter referred to as legally required low flammability), relatively rough fog In addition to obtaining a spray state with little scattering around when spraying in the form, DME even when spraying on the skin
To prevent the risk of skin damage due to rapid vaporization of, and to be able to prolong the retention time of the active ingredient on the skin surface, as a result of further research based on this new finding, The present invention has been completed.

Therefore, the aerosol product of the present invention is characterized in that at 20 ° C., 30 to 60% by volume of water, 20 to 60% by volume of ethyl alcohol and / or isopropyl alcohol, and DME
Of flammable liquefied gas containing 11 to 40% by volume, containing 0.1 to 12% by weight of active ingredient based on the total volume
And 0.1 to 10% by weight of a polyhydric alcohol, and a one-part aerosol composition is charged into a pressure-resistant container for aerosol so as to form a uniform dissolving phase.
The aerosol injection device having a pressure of 0.1 to 0.5 g / sec is attached to the pressure-resistant container.

In addition, the said ethyl alcohol consists of denatured or undenatured ethyl alcohol.

Examples of the high volatilization inhibitor having a high flash point include polyhydric alcohols, and particularly preferred are butylene glycol and
One type selected from propylene glycol, squalane, and glycerin or a mixture thereof can be exemplified.

As the active ingredient, the active ingredient of the target aerosol product is used.For example, if the repellent aerosol is the repellent active ingredient, if the antiperspirant aerosol is the antiperspirant active ingredient, the body colon aerosol is used. If the body colon active ingredient is an anti-inflammatory analgesic aerosol, the anti-inflammatory analgesic is used.If the dermatitis therapeutic is aerosol, the dermatitis therapeutic is used. Can be

When diethyltoluamide and a volatilization inhibitor such as butylene glycol are used in combination as the repellent active ingredient, when the contents are applied to the skin surface, the diethyltoluamide is sufficiently retained on the skin surface to prevent the repellent effect. It can last for a long time.

The injection amount per unit time, 0.1 to 0.5 g / sec, is a necessary condition for preventing the liquid from dripping on the coated surface of the product and satisfying the requirement of the low flammability in the regulation.

If the amount of water used in the present invention is less than 30% by volume, it is difficult to satisfy the legally required flammability requirement.
If it exceeds, it is not suitable for dissolving the oil-soluble active ingredient. Also,
If the content of ethyl alcohol and / or isopropyl alcohol (hereinafter referred to as alcohol) is less than 20% by volume, it is unsuitable for dissolving the oil-soluble active ingredient, and if it exceeds 60% by volume, the requirement for legally low flammability is not satisfied. If the amount of the flammable liquefied gas is less than 10% by volume, the requirement for flammability in the law is satisfied, but the injection of the entire contents is hindered. On the other hand, when the content exceeds 40% by volume, it is difficult to satisfy the requirement for slight flammability in regulations. As the combustible liquefied gas, a gas containing DME as a main component can be used. Then, since a relatively large amount of water is used, a mixed gas containing a large amount of DME is formed.
It is desirable to use LPG at 5 to 40% by volume with respect to 60 to 95% by volume. Further, for the LPG, ordinary propane, izobtan, normal butane can be used alone or in combination, but preferably, in order to adjust the product internal pressure.
It is better to use LPG at a pressure of 20 ° C. and a gauge pressure of about 1.5 to 5.0 kg / cm ² . And the above-mentioned water as an active ingredient,
Alcohol and combustible liquefied gas can be used as long as they are soluble in the component system, but in general, for example, active ingredients used for human body application such as antiperspirants, repellents, anti-inflammatory analgesics are soluble in alcohol. Water is often insoluble in water, and when the amount of the active ingredient exceeds 12% by weight, the active ingredient does not dissolve in the above-mentioned component system and is unsuitable. When the amount is less than 0.1% by weight, the medicinal effect cannot be exhibited. Furthermore, the use of a volatilization inhibitor having a high flash point, as described above, prevents the risk of skin damage due to rapid vaporization of DME, and prolongs the retention time of the active ingredient on the skin surface. If it is less than 0.1% by weight, the above-mentioned effects are poor, and if it exceeds 10% by weight, stickiness is produced when used, which is not good. Preferably, it is used in the range of 2 to 10% by weight. Next, if the injection amount per unit time is less than 0.1 g / sec, the feeling of use is poor, and if it is 0.5 g / sec or more, it is difficult not only to satisfy the requirements for legally low flammability but also to remove the contents. This is because when applied on the skin, liquid dripping occurs and the feeling of use becomes poor. As the injection device, it is necessary to control the flow rate that can use a general injection device, the stem hole diameter is 0.25 φ ~ 0.4 φ mm, the hole diameter of the housing vapor tap is 025 φ ~ 0.4 φ mm, and the lower hole diameter is 0.4 φ ~ A combination of 0.8 mm and a hole diameter of stem ≤ vapor tap hole diameter <pilot hole diameter should be used within the above range. The stem hole diameter has the largest effect on the flow rate regulation of the contents, and is 0.4 mm
If it exceeds, it does not satisfy the requirement for slight flammability in regulation. Also 0.
Those with a diameter of less than 25 mm are difficult to make for both molded and drilled products and are not common. The hole diameter of the housing paper tap is
Less than 0.25φmm is not as common as stem hole diameter, 0.4φmm
If the pressure exceeds the limit, the combustible liquefied gas is taken in too much gas phase when injecting the contents due to the combination with the pilot hole, so that the state of the mist becomes too fine and an intermittent injection state (breathing injection) occurs. The pilot hole diameter of the housing is the second most important factor after the stem hole diameter, and if the diameter exceeds 0.8 mm, the flow rate, that is, the injection amount per unit time becomes too large, and does not satisfy the legally required low flammability. On the other hand, when the diameter is less than 0.4 mm, the same state as when the diameter of the vapor tap hole is too large is not good.

Next, setting the hole diameter in the order as described above has no effect on flow rate regulation when the stem hole diameter is larger than others,
This is because even if the diameter of the vapor tap hole and the diameter of the pilot hole are large, if the hole diameter of the vapor tap is large, the above-mentioned breathing injection may not occur.

Next, the hole diameter of the aerosol button, which is a part of the injection device, is used between 0.25φmm and 0.4φmm, and a flow control hole (middle orifice) of 0.25φmm to 0.3φmm is further provided in the passage of the contents. By providing such an arrangement, the injection amount can be further reduced. Since the ratio of liquefied gas contained in the contents is small, it is good to use a button with a normal mechanical breakup as the button, but the hole diameter is 0.25 φmm
Less than 0.4 mm
If it exceeds, the injection amount will increase, and the requirement for slight flammability in the regulation will not be satisfied. The contents are ejected from the inside of the pressure-resistant container to the outside through the passage as described above. The housing has a vapor tap hole and a pilot hole, and the pilot hole communicates with the dip tube. The liquid that has risen in the dip tube is mixed with the content liquid and the liquefied gas gas phase in the housing, and is injected to the outside from the injection hole of the button through the middle orifice through the stem hole. Therefore, a small diameter portion may be provided in these passages in order to suppress the flow rate in another way.

Next, the present invention will be described in more detail with reference to examples, but the present invention is not limited to these examples.

Example 1 Repellent An aerosol composition having the following composition was prepared.

DEET (diethyltoluamide, manufactured by Yoshitomi Pharmaceutical Co., Ltd.) 7.9 g 1,3 butylene glycol 6.0 g 99% geraniol denatured alcohol 20.0 ml Purified water 35.8 ml DME 30.0 ml LPG (3.5 g / cm ² pressure at 25 ° C.) 2.0 ml (Note) ml is a value at 20 ° C. (the same applies to the following Examples and Comparative Examples).

To fill the aerosol pressure-resistant container with the aerosol composition, first, DEET and 1,3-butylene glycol are dissolved in 99% geraniol-denatured alcohol, and purified water is added thereto to prepare a stock solution. This is carried out by filling a container and then press-fitting a mixture with DME and LPG as a propellant. Here, ml is a value at 20 ° C. (the same applies hereinafter). Next, a stem hole diameter of 0.3 mm, a vapor tap diameter of 0.3 mm, and a pilot hole diameter of 0.6 mm
Then, a valve with a dip tube was loaded, and then a button having an injection hole hole diameter of 0.3 mm and a midori orifice diameter of 0.3 mm was attached to obtain an aerosol product for a repellent.

Example 2 Antiperspirant An aerosol composition having the following composition was prepared.

Aluminum Chloride Vide Oxide 3.0 g 1,3-butylene glycol 3.0 g 95% brucine denatured alcohol 39.0 ml Purified water 29.0 ml DME 24.0 ml LPG (pressure at 25 ° C. 2.7 kg / cm ² ) 2.0 ml Aerosol of the aerosol composition First, aluminum chloride hydride and 1,3-butylene glycol are dissolved and dispersed in 95% brucine-denatured alcohol, and purified water is added to the solution to prepare a stock solution. The aerosol pressure-resistant container is then filled with a stem hole diameter of 0.33φm.
m, a valve with a dip tube having a vapor tap diameter of 0.33 φmm and a pilot hole diameter of 0.64 φmm, and then press-fitting a mixture with DME and LPG as a propellant. Next, injection hole hole diameter 0.25φmm, Midori orifice diameter 0.3φm
By attaching the m button, an aerosol product for an antiperspirant was obtained.

The spray rate of this aerosol product was 0.4 g / sec at 25 ° C. Also, the requirement for slight flammability is an explosion concentration of 0.28 g / flame length of 22
cm.

Example 3 Body Colon An aerosol composition having the following composition was prepared.

Perfume 2 g L-menthol 0.2 g Glycerin 5.0 ml 99% Rose P denatured alcohol 20.0 ml Purified water 47.8 ml DME 24.0 ml LPG 1.0 ml At first, the aerosol composition was filled into a pressure-resistant container for aerosol, firstly perfume, L-menthol and Glycerin 99%
Dissolved in Rose P denatured alcohol, and purified water was added thereto to prepare a stock solution, which was filled in a pressure resistant container for aerosol.
This is performed by loading a valve with a dip tube having a diameter of 25 mm, a diameter of 0.3 mm and a diameter of 0.5 mm, and then press-fitting a mixture of DME and LPG as a propellant.
Next, the injection hole diameter is 0.3φmm, and the midorifice diameter is 0.3φ
By attaching the mm button, an aerosol product for body colon was obtained.

The spray rate of this aerosol product was 0.2 g / sec at 25 ° C. Also, the requirement for slight flammability is an explosion concentration of 0.29 g / flame length of 17
cm.

Example 4 Anti-inflammatory analgesic Camphor 3.0 g Menthol 3.0 g Methyl salicylate 2.5 g Glycol salicylate 1.5 g Propylene glycol 5.0 g 99% native alcohol 20.0 ml Isopropyl alcohol 5.0 ml Purified water 30.0 ml DME 27.0 ml LPG (pressure 3.0 at 25 ° C.) kg / cm ² ) 3.0 ml The above-mentioned aerosol composition was charged into a pressure-resistant container for aerosol at first by using camphor, menthol, methyl salicylate,
Dissolve glycolic acid salicylate, polyethylene glycol and perfume in 99% undenatured alcohol, add purified water to it to prepare a stock solution, fill it into a pressure-resistant container for aerosol, and then put a stem hole in the pressure-resistant container for aerosol. Diameter
0.3φmm, vapor tap hole diameter 0.35φmm, pilot hole diameter 0.55φm
The procedure is carried out by charging a valve with a dip tube at m and then injecting a mixture with DME and LPG as propellant. Then, an aerosol product for an anti-inflammatory analgesic was obtained by mounting a button having a hole diameter of the injection hole of 0.3 mm and a midorifice diameter of 0.35 mm.

Comparative Example 1 An aerosol product for a repellent was obtained in the same manner as in Example 1 except that 1,3 butylene glycol was omitted as a component of the aerosol composition.

Comparative Example 2 An aerosol product for an antiperspirant was obtained in the same manner as in Example 2 except that 1,3 butylene glycol was omitted as a component of the aerosol composition.

Comparative Example 3 An aerosol product for a body colon was obtained in the same manner as in Example 3, except that glycerin was removed as a component of the aerosol composition.

Comparative Example 4 An aerosol product for an anti-inflammatory analgesic was obtained in the same manner as in Example 4 except that propylene glycol was omitted as a component of the aerosol composition.

Next, an experiment on the retention time of the active ingredient was conducted on Example 1 and Comparative Example 1 under the following experimental conditions and evaluation method.

The spray rate of this aerosol product was 0.3 g / sec at 25 ° C. Also, the requirement for slight flammability is an explosion concentration of 0.27 g / flame length 18
cm. The results of an investigation of the repellent effect of the aerosol product as described below are shown in the table.

(Reservation time of active ingredient) Each of the products of Example 1 and Comparative Example 1 is sprayed onto one of the forearms of five healthy adult men over 15 cm for 3 seconds.

Prepare two 30 × 30 × 40 cm gauges releasing 50 Aedes albopictus unblood-sucking power, and after a lapse of a predetermined time, put both arms sprayed with the repellent as described above into the gauges for 2 minutes, respectively.
The number of mosquitoes sucked during that time was measured. The results are shown in Table 1.

In addition, so that only the skin sprayed with the repellent is exposed,
The unsprayed part was covered with vinyl gloves.

Further, with respect to Examples 1 to 4 and Comparative Examples 1 to 4, experiments on degreasing on the skin, the state of fog, and flammability were performed under the following experimental conditions and evaluation methods.

The spray rate of this aerosol product was 0.4 g / sec at 25 ° C. Also, the requirement for slight flammability is an explosion concentration of 0.27 g / flame length of 23
cm.

(Degreasing on the skin) Spray 10 cm over 1 cm on one forearm of 10 healthy adult males. This was sprayed four times at the same location every 15 minutes, and after 1 hour, the skin condition was visually and finger-sensitively compared. In all cases, no change was observed, and in some cases, the skin complained of skin pats. In the case of △, a majority of the people felt the skin pats and some of them showed whitening due to degreasing on the skin.

(Fog state) When sprayed on the forearm at a distance of 10 cm, those with few fine particles that can be applied uniformly are good, and those where the particles are rough and partially concentrated or adhere too finely and scatter around Many were marked as △.

(Flammability) A flammability test was conducted based on the provisions of Notification No. 557 of the Ministry of International Trade and Industry. Those that passed the above-mentioned flammability were defined as ○, and those that did not pass were ×.

 Table 2 shows the results of the experiment.

[Effects of the Invention] As described above, the present invention satisfies the requirements for legally low flammability, obtains a spray state with a relatively rough mist and little scattering around when spraying, and sprays on the skin Even in this case, there is a remarkable effect that the danger of skin damage due to rapid vaporization of DME can be prevented, and the retention time of the active ingredient on the skin surface can be extended.

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁶ Identification code Agency reference number FI Technical display location B65D 83/16 B65D 83/14 D 83/28 83/42 83/58

Claims (2)

(57) [Claims] 1. A component comprising 30 to 60% by volume of water at 20 ° C., 20 to 60% by volume of ethyl alcohol and / or isopropyl alcohol, and 11 to 40% by volume of a flammable liquefied gas containing 60 to 95% by volume of dimethyl ether. In the system, 0.1 to 12% by weight of active ingredient and polyhydric alcohol 0.1
~ 10% by weight, and a one-part aerosol composition to form a uniform dissolving phase is filled into a pressure-resistant container for aerosol, and the injection amount per unit time is 0.1 to 0.5 g / sec at 25 ° C. An aerosol product characterized in that an aerosol injection device as described below is attached to the pressure-resistant container. 2. The aerosol product according to claim 1, wherein the polyhydric alcohol is one selected from butylene glycol, propylene glycol, squalane, and glycerin, or a mixture thereof.