Inhalation composition for awakening and vitality enhancement and inhalation composition supply device containing the same

Abstract

The present invention relates to an inhalation composition for awakening and vitality enhancement according to the examples, comprising caffeine and one or more enhancers selected from glucose and magnesium.

Description

Technical Field

[0001] The present invention relates to an inhalation composition for promoting wakefulness and vitality containing caffeine at a relatively low content, and an inhalation composition supply device containing the same.

Background Art

[0002] Caffeine is known as a substance that acts on the central nervous system to promote wakefulness and vitality and is widely used, but there is a problem that it relaxes the lower esophageal sphincter and stimulates the esophagus by promoting gastric acid secretion. Therefore, development has been made as an inhalant administered to the respiratory tract rather than oral administration.

[0003] However, the method of inhaling caffeine through the respiratory tract affects the human body at a significantly faster rate than ingestion through food or the like, and there is a possibility of inducing side effects such as headache, dizziness, sleep disorder, palpitation, and muscle spasm when over-ingested, which is a problem.

Summary of the Invention

Problems to be Solved by the Invention

[0004] Various embodiments provide an inhalation composition for promoting wakefulness and vitality that solves the problems of the aforementioned prior art, and an inhalation composition supply device containing the same. The embodiments can enhance the wakefulness and vitality effects while reducing the content of caffeine.

[0005] The problems to be solved through the embodiments are not limited to the aforementioned problems, and problems not mentioned will be clearly understood by those having ordinary knowledge in the technical field to which the embodiments belong from the present specification and the accompanying drawings.

Means for Solving the Problems

[0006] An inhalation composition for promoting wakefulness and vitality according to an embodiment contains caffeine and an enhancer containing one or more selected from glucose and magnesium. An inhalation composition supply device according to one embodiment includes a storage container for containing the aforementioned inhalation composition and an inhaler to which the storage container is connected. [Effects of the Invention]

[0007] The inhalation composition for alertness and vitality enhancement described in the examples, and the inhalation composition dispensing device containing the same, exhibit excellent alertness and vitality-enhancing effects even with a relatively low caffeine content, and can minimize caffeine-induced side effects.

[0008] The problems to be solved through embodiments of the present invention are not limited to those described above, and any problems not mentioned will be clearly understood by those skilled in the art in which the embodiments pertain from this specification and the accompanying drawings. [Brief explanation of the drawing]

[0009] [Figure 1A] This graph shows the results of general behavioral experiments on the inhalation compositions of the comparative examples and examples. [Figure 1B] This graph shows the results of general behavioral experiments on the inhalation compositions of the comparative examples and examples. [Figure 1C] This graph shows the results of general behavioral experiments on the inhalation compositions of the comparative examples and examples. [Figure 1D] This graph shows the results of general behavioral experiments on the inhalation compositions of the comparative examples and examples. [Modes for carrying out the invention]

[0010] The terminology used in the embodiments has been selected, as far as possible, to be widely used and general terms, while taking into account the function of the present invention. However, this may vary depending on the intent of the articulators, case law, or the emergence of new technologies. In certain cases, the applicant may have arbitrarily selected terms, in which case their meaning will be described in detail in the description of the invention. Therefore, the terminology used in the present invention is not simply a set of names, but must be defined based on the meaning of the term and the overall content of the present invention.

[0011] Throughout the specification, when a part "includes" a component, it means, unless otherwise specified, that it does not exclude other components, but rather that it may include other components. Furthermore, terms such as "...part" and "...module" used in the specification mean a unit that processes at least one function or operation, which may be embodied by hardware or software, or by a combination of hardware and software.

[0012] As used herein, when an expression such as “at least one of the following” precedes an array of components, it modifies the entire group of components, not each of the individual components in the array. For example, the expression “at least one of a, b, and c” must be interpreted as including a, b, c, or a and b, a and c, b and c, or a, b, and c.

[0013] Hereinafter, embodiments of the present invention will be described in detail with reference to the attached drawings so that they can be easily implemented by a person skilled in the art. However, the present invention can be embodied in a variety of different forms and is not limited to the embodiments described herein.

[0014] Throughout the specification, the examples are arbitrary classifications that facilitate the explanation of the invention, and each example does not need to be mutually exclusive. For example, a configuration disclosed in one example may be applied to and / or embodied in other examples and may be applied to and / or embodied with modifications that do not depart from the scope of the invention.

[0015] Furthermore, the terminology used in this invention is for illustrative purposes only and is not intended to limit these embodiments. In this invention, the singular form includes the plural form unless otherwise specified.

[0016] According to the examples, inhalation compositions for alertness and vitality enhancement can be provided. An inhalation composition for alertness and vitality enhancement according to one embodiment may contain caffeine and one or more enhancers selected from glucose and magnesium in order to provide alertness and vitality-enhancing effects with a relatively low caffeine content.

[0017] For example, caffeine may be present in an amount of 15% by weight or less based on the total weight of the inhalation composition. Alternatively, caffeine may be present in an amount of 8% by weight or less based on the total weight of the inhalation composition. If the caffeine content exceeds the above amounts, it may be problematic because the high caffeine content may induce side effects such as headaches and dizziness, sleep disorders, palpitations, and muscle spasms.

[0018] In one embodiment, the enhancer is one or more selected from glucose and magnesium. The enhancer, when included in the inhalation composition together with caffeine, can improve the alertness and vitality-enhancing effects.

[0019] The aforementioned enhancer may contain glucose and magnesium, or both glucose and magnesium. When both glucose and magnesium are included as enhancers, the awakening and vitality-enhancing effects of the inhalation composition according to the examples may be further improved.

[0020] An inhalation composition for alertness and vitality according to one embodiment may further contain, in addition to the aforementioned caffeine and enhancer, vitamin B3 and a solvent. As an example, caffeine and vitamin B3 may be included in a weight ratio of 2:1 to 2:3. When the amount of vitamin B3 is less than the above range, caffeine is not sufficiently dissolved in the inhalation composition. When the amount of vitamin B3 is more than the above range, the effect of increasing the solubility of caffeine is negligible.

[0021] In an inhalation composition for promoting wakefulness and vitality according to an embodiment, based on the total weight of the composition, the caffeine may be 2 to 15% by weight, the vitamin B3 may be 1 to 15% by weight, the enhancer may be 1 to 20% by weight, and the solvent may be 45 to 96% by weight.

[0022] In one embodiment, the solvent may be included in an amount equal to the remaining amount obtained by excluding caffeine, vitamin B3, and the enhancer from the total weight of the composition, which dissolves the caffeine, vitamin B3, and the enhancer. In one embodiment, the solvent may be included in an amount of 45 to 96% by weight based on the total weight of the inhalation composition. In one embodiment, the solvent may be included in an amount of 55 to 85% by weight based on the total weight of the inhalation composition. In one embodiment, the solvent may be included in an amount of 70 to 80% by weight based on the total weight of the inhalation composition.

[0023] The solvent included in the inhalation composition according to an embodiment may include any one or more of water, alcohol, propylene glycol, and vegetable glycerin. The solvent can dissolve caffeine, vitamin B3, and the enhancer.

[0024] The inhalation composition according to an embodiment may further include sodium chloride in the solvent. For example, the solvent may include water and sodium chloride. Sodium chloride may be included in an amount of 0.5 to 1.5% by weight based on the total weight of water. Also, sodium chloride may be included in an amount of 0.85 to 0.95% by weight based on the total weight of water.

[0025] As an example, the solvent included in the inhalation composition may include 98.5 to 99.5% by weight of water and 0.5 to 1.5% by weight of sodium chloride based on the total weight of the solvent. On the other hand, in the inhalation composition according to the examples, the enhancer may contain 1 to 20% by weight of glucose based on the total weight of the composition. Alternatively, the enhancer may contain 1 to 20% by weight of magnesium based on the total weight of the composition.

[0026] Furthermore, the enhancer may contain 1 to 20% by weight of glucose and magnesium, based on the total weight of the composition. If the enhancer contains both glucose and magnesium, it may contain 1 to 10% by weight of glucose and 1 to 10% by weight of magnesium. It may also contain 1 to 8% by weight of glucose and 1 to 8% by weight of magnesium, or 1 to 5% by weight of glucose and 1 to 5% by weight of magnesium.

[0027] The inhalation compositions according to the examples may further contain additives that can be used as inhalation compositions. For example, the inhalation composition may further contain one or more flavoring agents or flavoring components. As another example, if the inhalation composition is used in a metered-dose inhaler, the inhalation composition may further contain a propellant, but is not limited thereto.

[0028] On the other hand, according to the embodiment, an inhalation composition supply device may be provided, which includes a storage container for containing the aforementioned inhalation composition and an inhaler to which the storage container is coupled. As an example, the storage container may be detachably coupled to the inhaler. As another example, the storage container may be fixed to the inhaler and provided with an opening for refilling the inhalation composition.

[0029] One embodiment of the inhalation composition for awakening and vitality enhancement is in the form of inhalation through an inhaler. Inhalers come in various forms, such as metered-dose inhalers, dry powder inhalers, and nebulizers.

[0030] Inhalation compositions are in the form of a solid, a liquid, or a mixture of a solid and a liquid. For example, an inhalation composition may be a mixture of solid powders of caffeine and a stimulant. Alternatively, it may be a solid obtained by dissolving caffeine, vitamin B3, and a stimulant in a solvent and then drying the solvent. Solid compositions can be produced as dry powders for inhalation using a dry powder inhaler.

[0031] As another example, the inhalation composition is a liquid in which caffeine, vitamin B3, and a stimulant are dissolved in a solvent. In one embodiment, the inhaler is a fume inhaler, i.e., a nebulizer. The nebulizer atomizes the liquid inhalation composition, and the atomized composition can be administered to the human respiratory system. In one embodiment, an awakening and vitality-enhancing effect can be obtained by inhaling the atomized inhalation composition.

[0032] According to one embodiment, the inhaler may include an atomizer for atomizing an inhalation composition, a battery for supplying power to the atomizer, and a supply port for supplying the atomized composition to the atomizer. As an example, as described above, an inhaler including an atomizer, a battery, and a supply port is a fume inhaler.

[0033] For example, atomizers include jet atomizers that use compressed air to atomize liquid compositions, ultrasonic atomizers that use high-frequency sound waves to atomize liquid compositions, vibration atomizers that apply vibration to a mesh to atomize liquid compositions by passing them through the mesh, and heating atomizers that atomize liquid compositions through heating.

[0034] Furthermore, the inhaler according to one embodiment includes a heating element, and the atomization rate can be adjusted by activating the heating element. The heating element is controlled by a separate switch located outside the inhalation composition supply device, but is not limited to this.

[0035] According to one embodiment, an inhalation composition atomized in a atomizer can be administered to a human respiratory system through a supply port. The supply port may include a mouthpiece or mask positioned adjacent to the supply port. The mouthpiece or mask may be physically connected to the supply port.

[0036] For example, the supply port may include a mouthpiece, which is connected to or extends from the supply port as an integral part of the supply port. In another example, the supply port may include an inhalation mask connected to the supply port. The inhalation mask may have a shape that fits snugly against the face.

[0037] The invention will be further explained below through examples and experimental examples. It will be clear to those with ordinary skill in the art that these examples are merely illustrative and that the invention is not to be construed as being limited by these examples.

[0038] [Examples] Inhalation compositions were prepared, and their awakening and vitality-enhancing effects were measured. Specifically, after preparing the inhalation compositions and administering them orally or by inhalation to experimental animals, the awakening and vitality-enhancing effects were measured through general behavioral experiments and forced swimming ability experiments.

[0039] 1. Experiment preparation (1) Preparation of experimental animals The experimental animals were C57BL / 6 mice (male, 10 weeks old), purchased from KOATECH after approval from the Animal Experiment Ethics Committee (IACUC). They were purified for one week in the KT&G Bio-Efficacy Evaluation Center's breeding room (temperature 23±2℃, humidity 50±10%, light-dark cycle 12 hours) before being used in the experiments.

[0040] (2) Verification of the effects of caffeine through oral administration Caffeine was dissolved in 0.9% physiological saline and administered orally to mice using a tube at a dose rate of 10 ml / kg, after which general behavioral experiments were conducted. After orally administering the samples from Experimental Examples 1 to 3 below to C57BL / 6 mice, the number of movements, movement speed (mm / s), distance moved (meter), and movement time (sec) over a one-hour period were measured using the LABORAS behavioral apparatus.

[0041] Experimental Example 1 involved the oral administration of only 10 ml / kg of 0.9% physiological saline as a control group. Experimental Example 2 involved the oral administration of caffeine at a dose of 5 mg / kg dissolved in 0.9% physiological saline using a feeding tube. Experimental Example 3 involved the oral administration of caffeine at a dose of 30 mg / kg dissolved in 0.9% physiological saline using a feeding tube. The stimulating effect of caffeine was examined for each of Experimental Examples 1 to 3 through general behavioral experiments, and the results are shown in Table 1 below.

[0042] [Table 1]

[0043] The measurement results showed that in Experiment 2, where caffeine was orally administered at a concentration of 5 mg / kg, there was almost no effect, while in Experiment 3, where caffeine was orally administered at a concentration of 30 mg / kg, a stimulating effect was observed.

[0044] 2. General behavioral experiments on inhalation compositions Inhalation compositions for comparative examples and examples were prepared and administered to mice by inhalation using a mist generator. The inhalation time (min) at which efficacy was observed for each composition was measured, and the compositions were collected for 10 minutes using a sampling pump and Cambridge filter. The TPM (Total Particulate Matter) concentration was calculated by gravimetric analysis.

[0045] C57BL / 6 mice were administered the inhalation compositions of Comparative Examples 1 to 5 and Examples 1 to 3 shown in Table 2 below by inhalation. The number of movements, movement speed (mm / s), distance moved (meter), and movement time (sec) were then measured over a one-hour period using a LABORAS behavioral device. All substances contained in the inhalation compositions of the comparative examples and examples were dissolved in 0.9% physiological saline before use.

[0046] On the other hand, the control group for each comparative example and example was administered by inhaling 0.9% physiological saline solution sprayed using a mist generator into mice.

[0047] [Table 2]

[0048] (1) Comparative Example 1 A caffeine inhalation composition containing 2% by weight of caffeine (Comparative Example 1) was prepared by dissolving caffeine in 0.9% physiological saline. The composition of Comparative Example 1 was sprayed using a mist generator and administered to mice by inhalation for 50 minutes. General behavior was observed, and it was confirmed that there was no significant difference in efficacy compared to the control group.

[0049] (2) Comparative Examples 2 to 4 A comparative example (Comparative Example 2) was prepared by dissolving vitamin B3 in 0.9% physiological saline to produce an inhalation composition containing 10% by weight of vitamin B3. In addition, a comparative example (Comparative Example 3) was prepared by dissolving glucose in 0.9% physiological saline to produce an inhalation composition containing 10% by weight of glucose, and a comparative example (Comparative Example 4) was prepared by dissolving magnesium in 0.9% physiological saline to produce an inhalation composition containing 10% by weight of magnesium.

[0050] The compositions of Comparative Examples 2 to 4 were administered to mice by inhalation for 20 to 60 minutes by spraying them using a mist generator, and their general behavior was observed. The results confirmed that there was no significant difference in efficacy compared to the control group. (3) Comparative Example 5 Caffeine and vitamin B3 were dissolved in 0.9% physiological saline to prepare an inhalation composition (Comparative Example 5) containing 8% by weight of caffeine and 10% by weight of vitamin B3. The composition of Comparative Example 5 was sprayed using a mist generator and administered to mice by inhalation for 10 to 30 minutes. General behavior was observed, and it was confirmed that an effect was observed when the mice inhaled for 30 minutes or more.

[0051] (4) Example 1 An inhalation composition (Example 1) containing 8% by weight of caffeine, 10% by weight of vitamin B3, and 5% by weight of glucose was prepared by dissolving caffeine, vitamin B3, and glucose in 0.9% physiological saline. The composition of Example 1 was sprayed using a mist generator and administered to mice by inhalation for 5 to 15 minutes. General behavior was observed, and it was confirmed that an effect was observed when the mice inhaled the composition for 10 minutes or more.

[0052] (5) Example 2 An inhalation composition (Example 2) containing 8% by weight of caffeine, 10% by weight of vitamin B3, and 5% by weight of magnesium was prepared by dissolving caffeine, vitamin B3, and magnesium in 0.9% physiological saline. The composition of Example 2 was sprayed using a mist generator and administered to mice by inhalation for 5 to 30 minutes. General behavior was observed, and it was confirmed that an effect was observed when the mice inhaled the composition for 20 minutes or more.

[0053] (6) Example 3 An inhalation composition (Example 3) containing 8% by weight of caffeine, 10% by weight of vitamin B3, 5% by weight of glucose, and 5% by weight of magnesium was prepared by dissolving caffeine, vitamin B3, 10% by weight of vitamin B3, 5% by weight of glucose, and 5% by weight of magnesium in 0.9% physiological saline. The composition of Example 3 was sprayed using a mist generator and administered to mice by inhalation for 5 to 15 minutes. General behavior was observed, and it was confirmed that an effect was observed when the mice inhaled the composition for 5 minutes or more.

[0054] 3. General behavioral experiments and forced swimming experiments on inhalation compositions General behavioral experiments and forced swimming experiments were conducted on the control group, Comparative Example 5, and the inhalation compositions of Examples 1 to 3. The efficacy of each composition was compared under identical conditions by spraying it using a mist generator and inhaling it for 15 minutes.

[0055] The general behavioral experiment was conducted in the same manner as described in Section 2, "General Behavioral Experiment Methods." In the case of the forced swimming experiment, a transparent cylinder with a diameter of 8 cm and a height of 25 cm was filled with water at a temperature of 25°C, and the mice were placed in the water and allowed to adapt for 10 minutes. After 24 hours, each composition was inhaled for 15 minutes, and then the mice were placed in a water tank for 6 minutes. The immobility time (sec) during the last 4 minutes was measured. The measurement results are shown in Table 3 below.

[0056] [Table 3]

[0057] As a result, in both general behavioral experiments and forced swimming experiments, it was confirmed that compositions containing glucose and magnesium (Examples 1 and 2) showed superior efficacy compared to Comparative Example 5, and that the composition containing both glucose and magnesium (Example 3) showed extremely superior efficacy.

[0058] The results for the general behavior experiment are shown in Figure 1. Measurements were taken over one hour using the LABORAS behavior device. Figure 1A shows the number of movements, Figure 1B shows the speed of movement, Figure 1C shows the distance moved, and Figure 1D shows the time spent moving. In the upper part of the graphs for each Comparative Example 5 and Examples 1 to 3, the percentage increase is shown compared to the control group.

[0059] Referring to Figure 1, in the overall general behavioral experiment results, Comparative Example 5 showed only a slight increase in effect compared to the control group, while Examples 1 and 2 showed a significant increase, and Example 3 showed an even greater increase.

[0060] In particular, as can be seen from the results of the forced swimming experiment, the immobility time was shortened somewhat in Examples 1 and 2, but in Example 3, the immobility time was remarkably short at around 175 seconds, confirming that the awakening and vitality-enhancing effect was excellent.

[0061] Through general behavioral experiments and forced swimming experiments, the awakening and vitality-enhancing effects of the inhalation compositions of Examples 1 to 3 can be confirmed. The descriptions relating to the embodiments described above are merely illustrative, and a person with ordinary skill in the art will understand that a variety of modifications and equivalent other embodiments are possible therefrom. The embodiments described above may achieve satisfactory results even if the described techniques are performed in a different order than described, and / or if the described components are combined or combined in a different manner than described, or substituted or replaced by other components or equivalents. Therefore, all differences that fall within the scope equivalent to those described in the claims should be construed as being within the scope of protection defined by the claims.

Claims

1. In an inhalation composition for awakening and enhancing vitality, Caffeine and, An inhalation composition comprising a enhancer containing one or more selected from glucose and magnesium.

2. The inhalation composition according to claim 1, wherein the caffeine is contained in an amount of 15% by weight or less, based on the total weight of the inhalation composition.

3. The inhalation composition according to claim 1, wherein the caffeine is contained in an amount of 8% by weight or less, based on the total weight of the inhalation composition.

4. The aforementioned inhalation composition is Vitamin B3 and The inhalation composition according to claim 1, further comprising one or more solvents selected from the group consisting of water, alcohol, propylene glycol, and vegetable glycerin.

5. The inhalation composition according to claim 4, wherein the caffeine and the vitamin B3 are contained in a weight ratio of 2:1 to 2:

3.

6. Based on the total weight of the aforementioned inhalation composition, The caffeine is present in an amount of 2 to 15% by weight, The aforementioned vitamin B3 is present in an amount of 1 to 15% by weight, The aforementioned enhancing agent is present in an amount of 1 to 20% by weight, The inhalation composition according to claim 4, wherein the solvent is present in an amount of 45 to 96% by weight.

7. The inhalation composition according to claim 4, wherein the solvent comprises 98.5 to 99.5% by weight of water and 0.5 to 1.5% by weight of sodium chloride, based on the total weight of the solvent.

8. The inhalation composition according to claim 6, wherein the enhancer comprises 1 to 10% by weight of glucose and 1 to 10% by weight of magnesium, based on the total weight of the inhalation composition.

9. A storage container for storing an inhalation composition containing an enhancer selected from one or more of caffeine, glucose, and magnesium, An inhalation composition supply device comprising an inhaler to which the aforementioned storage container is attached.

10. The inhalation composition supply device according to claim 9, wherein the inhaler is a metered-dose inhaler, a dry powder inhaler, or a nebulizer.

11. The inhalation composition further comprises vitamin B3 and one or more solvents selected from the group consisting of water, alcohol, propylene glycol, and vegetable glycerin. The inhalation composition supply device according to claim 9, wherein the inhaler includes an atomizer for atomizing the inhalation composition.

12. The inhalation composition supply device according to claim 11, wherein the atomizer atomizes the inhalation composition using a jet method, an ultrasonic method, a vibration method, or a heating method.

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