JPH02184683A - Consciousness level depressor - Google Patents

Abstract

PURPOSE:A consciousness level depressor for human and animal, containing a specific phthalide derivative as an active ingredient and having superior consciousness level depressive effect, persistence and high safety. CONSTITUTION:The objective consciousness level depressor containing >=1 kinds of phthalide derivatives expressed by the formula (R1 represents H, OH, methoxy, amino or dimethylamino; R2 and R3 represent H or methoxy; R4 represents H, amino or dimethylamino; R5 represents H, alkyl or alkoxyl) (example; butylphthalide, hepthylphthalide, isoamylphthalide or propoxyphthalide). By incorporating the depressor singly or in combination with a compound perfume into a product, it can be used in fragrances, room aromatics, cream, emulsions, cosmetic powder, body lotion, dentifrice, hair product, aerosol product, etc. The amount thereof to be incorporated is 0.3-50wt.%.

Description

[Detailed Description of the Invention] [Industrial Application Field] The present invention provides a method for inhaling phthalide derivatives such as butylphthalide, heptyl phthalide, propoxy phthalide, isoamyl phthalide, etc. that reduce the level of consciousness of humans or animals. The present invention relates to a composition that lowers the level of consciousness of a human or animal.

[Conventional technology]

Traditionally, so-called aromatherapy (
A treatment method called aroma therapy is known. The fragrances used in aromatherapy are mainly natural essential oils based on ancient traditions.

The effects are subjective and qualitative, and the effectiveness is not necessarily satisfactory. In addition, many essential oils have two strong scents, which affect the overall scent when creating a blended fragrance by blending, so the balance between scent intensity and palatability and the effective amount for producing effects is important. It was not always satisfactory.

On the other hand, if something has too strong a fragrance, people may dislike it no matter how fragrant it may be, and even if it has a pleasant fragrance, it may become unpleasant if you continue to smell it for a long time.

However, as the name suggests, aromatherapy cannot be used for aromatherapy unless the essential oils have a fragrance. To be used in therapy,
This was completely unthinkable at the technical level of the industry.

[Problem that the invention seeks to solve]

In view of the above circumstances, the present inventors have set a new technical problem of completely changing the way of thinking and obtaining a substance that truly has an excellent effect of lowering the level of consciousness despite its low scent intensity.

In other words, in the present invention, the technical problem to be solved, which is the starting point of the invention, is completely unknown and new.

Therefore, as a result of extensive and intensive research from various fields in order to solve this new technical problem, we found that, quite unexpectedly,
Circulating essential oil components such as butyl phthalide and its analogs isoamyl phthalide and propoxy phthalide have a slightly distinctive odor, but they lower the level of consciousness, and heptyl phthalide and others are almost odorless but can be inhaled. We have discovered a completely new fact that it has a stronger effect of lowering the level of consciousness, and based on this knowledge, we have completed the present invention.

[Means for solving problems]

That is, 1 the present invention relates to the general formula I (in the general formula, R represents a hydrogen atom, a hydroxyl group, a methoxy group, an amino group or a dimethylamino group, R2 represents a hydrogen atom or a methoxy group, and R3 represents a hydrogen atom or a methoxy group) , R4 represents a hydrogen atom, an amino group or a dimethylamino group, and R5 represents hydrogen, an alkyl group or an alkoxyl group.
The object of the present invention is to provide an agent for lowering the level of consciousness of humans or animals, which contains one or more species as active ingredients.

The effect of lowering the level of consciousness referred to here refers to the effect of freeing people or animals from physiological and psychological states caused by heightened levels of consciousness, such as irritation and excitement, that they experience in their daily lives, calming their mood, and calming their mental activities. It refers to the effect.

The level of consciousness reducing agent of the present invention can be used in the form of various compositions.

A composition refers to a composition in which an effective amount of a phthalide derivative is inhaled and produces an effect by stimulating olfactory receptors or being absorbed into the body through the respiratory tract, and is used in fragrance products such as perfumes, colognes, and room air fresheners. It also includes cosmetics such as soap and toothpaste, and pharmaceuticals.

The present invention will be explained in detail below.

Some of the phthalide derivatives in the present invention are:

It can be extracted from rhizomes or roots of Apiaceae plants, but it can also be synthesized by a known method, for example, by reacting phthalic anhydride with dialkyl cadmium or the like.

These phthalide derivatives can be used singly or as a mixture of two or more, and can also be used as a mixed composition with various media that can be mixed with the phthalide derivatives (for example, organic solvents, oils, blended fragrances, and perfumed products).

When a blended fragrance is used as a medium, the scent of each individual component contributes to the overall scent of the blended fragrance, but as mentioned above, some of these phthalide derivatives are almost odorless, so they do not contribute to the overall scent of the blended fragrance. has almost no effect.

From this point of view, the amount of phthalide derivatives to be used has a high degree of freedom, and even if 1% or more by weight of phthalide derivatives is added to a blended fragrance, the effect of lowering consciousness can be produced without changing the fragrance of the entire fragrance.

Furthermore, from the perspective of significantly producing a consciousness-lowering effect, 5% to 50% by weight of phthalide derivatives should be added.
It can be blended into a blended fragrance within the range of .

It can also be used as an eau de cologne using ethyl alcohol as a medium. Again, the phthalide derivatives can be incorporated alone or in combination with the perfume preparations described above.

In addition, by incorporating phthalide derivatives into products in other selected vehicles, either alone or in combination with blended fragrances, fragrances, room air fresheners, creams, emulsions, cosmetic powders, body lotions, deodorant sticks, toothpaste, hair, etc. It can be used in products, aerosol products, etc. In this case, the amount of the phthalide derivative used ranges from 0.3% by weight to 50% by weight.

Furthermore, it can also be used as an inhalation drug containing a phthalide derivative as an active ingredient.

Next, we will describe experiments on the effects of each phthalide derivative on lowering consciousness and the results.

[Pharmacological effect]

■ Anesthesia time for mice (1) Experimental method ddY male mice (4-5 weeks old, 126-31 g per week)
an air stream containing the following test substance (0.5-1 mg/3
The difference in pendoparbital sleep time (50 mg/kg intraperitoneal injection) was compared between the group in which the subjects were inhaled with 3 Q/min of air containing the test substance and the group in which the test substance was not inhaled.

(2) Test substance Substance A Nibutylphthalide Substance B: Hebutyl phthalide Substance C: Isoamyl phthalide Substance D: Propoxyphthalide The experimental results are shown in Table 1.

Table 1 (3) As is clear from the above results, it can be seen that phthalide derivatives have a remarkable effect of prolonging the anesthetic action time.

[Administration method, dosage]

The present invention is characterized by administration by inhalation, and unlike sedatives administered orally, subcutaneously, or intramuscularly, it is expected to have a milder effect on lowering consciousness than sedatives when given to healthy individuals. Therefore, it is desirable to provide the above-mentioned phthalide derivatives as part of a composition containing alcohol or perfume, or as part of a perfume composition used in a perfumed product.

The effect of the inhalation agent of the present invention that reduces consciousness is due to age.

Since it is influenced by individual differences, gender, mental and physical condition, etc., in some cases it may be necessary to administer a dose outside the range shown below, but in general, when administering a phthalide derivative to a healthy person, 0.1
It is preferable to inhale and administer the aroma volatilized from a perfumed product containing 5% to 5% over a certain period of time or continuously.

Furthermore, the phthalide derivative that is the active ingredient of the present invention has LD for acute toxicity to rats.

The value (intraperitoneal administration) was greater than Ig/kg, and safety was confirmed.

Therefore, it is particularly safe to use the agent for lowering the level of consciousness according to the present invention in the form of soaps, external preparations, and cosmetics.

〔Example〕

Next, examples will be given to clarify the present invention more specifically. The present invention is not limited thereby.

The blending amount is in weight%.

Example 1 Eau de Cologne and Perfume Eau de cologne was prepared by adding 30% heptyl phthalide to a citrus-based perfume and diluting it to 3% with 95% ethyl alcohol.

Further, using the same method, perfumes were obtained by diluting them to 5%, 10%, and 20%.

In addition, the same blended fragrance with 30% heptyl phthalide added to 95% ethyl alcohol and 20% heptyl phthalide added to 95% ethyl alcohol.
The perfume was obtained by diluting it to the following.

These colognes had the effect of lowering the level of consciousness of humans or animals when inhaled.

Example 2 Indoor air spray An indoor air spray was created with the following formulation.

Isoamyl phthalide Citrus blend fragrance 95% ethyl alcohol twin 80 propellant Example 3 Soap (1) Soap base (2) Butyl phthalide (3) Mixed fragrance (4) Pigment (weight%) 0.07 4.30 56.00 3.00 36.00 Too, o.

(% by weight) 95.0 1.0 4.0 Soap was manufactured by adding appropriate amounts of manufacturing methods (2), (3) and (4) to the soap base of (1), and then kneading with a machine or forming a frame. .

talc propoxy phthalide Mixed fragrance liquid paraffin Manufacturing method A bath powder was obtained by mixing and stirring (1) to (4).

(1) Dried sodium sulfate (2) Sodium hydrogen carbonate (4) Fragrance (5) Colorant Appropriate amounts of Preparation Methods (1) to (5) were sequentially added, mixed and stirred to obtain a bath salt type bath agent.

〔Effect of the invention〕

The consciousness level lowering agent according to the present invention not only has an excellent consciousness lowering effect but also has a long-lasting effect and is highly safe.

Therefore, the solution can not only be used advantageously for therapeutic purposes such as direct inhalation through a special pipe, but also for daily use for preventive or health purposes.For example, it can be used for a relatively long period of time as a room air freshener or bath additive. By doing so, it is possible to recover from stress after work or study, recovery from mental or physical fatigue, etc., so it is a very effective drug for refreshing people, especially for busy modern people. Particularly, the liquid solution is odorless or has a slight fragrance and is very safe, so it is particularly suitable for repeated use on a daily basis.

In other words, the present invention is effective not only in cases where the symptoms clearly appear and require immediate treatment, but also in recovering from a half-hearted mental state where the patient is irritated or feels uneasy, although the symptoms are not so obvious. therefore,
It can be said that this drug is exactly what modern people have been waiting for, as they are surrounded by various types of stress and have no time to relax throughout the day.

Furthermore, the agent for lowering the level of consciousness according to the present invention is extremely effective for animals other than humans, and can be administered by inhalation, making it extremely easy to administer. By administering it before the mission, experiments and missions can be carried out smoothly. In addition, in recent years, there has been an increase in the number of cases in which pets, like humans, become stressed and irritated, or even pose a threat to humans. It is also possible to do so.

Agent Patent Attorney 1) Parent Male

Claims (1)

[Claims] General formula I ▲There are mathematical formulas, chemical formulas, tables, etc.▼ I (In the general formula, R_1 is a hydrogen atom, a hydroxyl group, a methoxy group,
represents an amino group or a dimethylamino group, R_2 represents a hydrogen atom or a methoxy group, R_3 represents a hydrogen atom or a methoxy group, R_4 represents a hydrogen atom, an amino group or a dimethylamino group, and R_5 represents hydrogen, an alkyl group or Indicates an alkoxyl group. ) An agent for lowering the level of consciousness of humans or animals, which contains one or more phthalide derivatives represented by the following as an active ingredient.