Inhalable composition for enhancing arousal and vitality and inhalable composition supply device comprising same

Abstract

An embodiment relates to an inhalable composition for enhancing arousal and vitality, comprising: caffeine; and an enhancer including at least one selected from glucose and magnesium.

Description

Inhalable composition for enhancing wakefulness and vitality and inhalable composition supply device comprising the same

[0001] The embodiments relate to an inhalable composition for enhancing wakefulness and energy comprising a relatively low content of caffeine and a device for delivering an inhalable composition comprising the same.

[0002] Caffeine is widely used as a substance known to increase alertness and vitality by acting on the central nervous system. However, it has the disadvantage of relaxing the lower esophageal sphincter and stimulating the secretion of gastric acid, thereby irritating the esophagus. Therefore, development is underway to develop an inhaled drug administered through the respiratory tract rather than orally.

[0003] However, inhaling caffeine through the respiratory system can affect the body at a much faster rate than consuming it through food, etc., and excessive consumption can cause side effects such as headaches, dizziness, sleep disturbances, palpitations, and muscle cramps, which is problematic.

[0004] Various embodiments provide an inhalable composition for enhancing wakefulness and vitality and an inhalable composition supply device comprising the same, which can solve the problems of the prior art described above.

[0005] Examples may enhance wakefulness and energy benefits while lowering caffeine content.

[0006] The problems to be solved through the examples are not limited to the problems described above, and problems not mentioned can be clearly understood by a person having ordinary skill in the technical field to which the examples belong from this specification and the attached drawings.

[0007] An inhalable composition for enhancing wakefulness and vitality according to one embodiment may include: caffeine; and an enhancer comprising at least one selected from glucose and magnesium.

[0008] An inhalation composition supply device according to one embodiment may include a storage container containing the inhalation composition described above and an inhaler to which the storage container is coupled.

[0009] The inhalable composition for enhancing wakefulness and vitality and the inhalable composition supply device comprising the same according to the embodiments have excellent wakefulness and vitality enhancing effects even at relatively low caffeine contents, thereby minimizing side effects caused by caffeine.

[0010] The effects of the embodiments are not limited to the effects described above, and effects not mentioned can be clearly understood by a person having ordinary skill in the art to which the embodiments belong from this specification and the attached drawings.

[0011] Figures 1a to 1d are graphs showing the results of general behavioral experiments on inhalable compositions of comparative examples and examples.

[0012] The terms used in the examples are selected from widely used, common terms, taking into account the functions within the examples. However, these terms may vary depending on the intentions of those skilled in the art, precedents, the emergence of new technologies, etc. Furthermore, in certain cases, terms may be arbitrarily selected by the applicant, in which case their meanings will be described in detail in the description of the relevant invention. Therefore, the terms used in the examples should not be defined simply based on their names, but rather based on their meaning and the overall content of the examples.

[0013] When a part of the specification is said to "include" a component, this does not exclude other components, but rather implies the inclusion of other components, unless otherwise specifically stated. Furthermore, terms such as "-unit" and "-module" used in the specification refer to a unit that processes at least one function or operation, which may be implemented in hardware, software, or a combination of hardware and software.

[0014] As used herein, when an expression such as "at least one" precedes an array of elements, it modifies the entire array of elements, not just each individual element. For example, the expression "at least one of a, b, and c" should be interpreted to include a, b, c, or a and b, a and c, b and c, or a and b and c.

[0015] Below, with reference to the attached drawings, embodiments of the present invention are described in detail so that those skilled in the art can easily implement the invention. However, the present invention may be implemented in various different forms and is not limited to the embodiments described herein.

[0016] Throughout this specification, embodiments are used as arbitrary distinctions to facilitate the description of the invention, and each embodiment is not necessarily exclusive of the others. For example, configurations disclosed in one embodiment may be applied and / or implemented in other embodiments, and may be modified and applied and / or implemented without departing from the scope of the present disclosure.

[0017] Additionally, the terminology used in this disclosure is for the purpose of describing embodiments and is not intended to limit the embodiments. In this disclosure, singular forms also include plural forms unless specifically stated otherwise.

[0018] According to an embodiment, an inhalable composition for enhancing wakefulness and vitality may be provided.

[0019] An inhalable composition for enhancing wakefulness and vitality according to one embodiment may include caffeine; and an enhancer including at least one selected from glucose and magnesium, to provide an awakening and vitality enhancing effect with a relatively low caffeine content.

[0020] For example, caffeine may be present in an amount of no more than 15% by weight based on the total weight of the inhalable composition. Alternatively, caffeine may be present in an amount of no more than 8% by weight based on the total weight of the inhalable composition. Exceeding the above amounts of caffeine can cause adverse effects, such as headaches, dizziness, sleep disturbances, palpitations, and muscle cramps, which can be problematic.

[0021] In one embodiment, the stimulant may be one or more selected from glucose and magnesium. The stimulant may be included in the inhalable composition together with caffeine to enhance the wakefulness and energy-enhancing effects.

[0022] The above-mentioned enhancer may include glucose or magnesium, or may include both glucose and magnesium. When both glucose and magnesium are included as enhancers, the awakening and vitality-enhancing effects of the inhalable composition according to the embodiment may be further enhanced.

[0023] An inhalable composition for enhancing wakefulness and vitality according to one embodiment may further comprise, in addition to the caffeine and enhancer described above, vitamin B3 and a solvent.

[0024] As an example, caffeine and vitamin B3 may be included in a weight ratio of 2:1 to 2:3. If the amount of vitamin B3 is less than the above range, caffeine may not be sufficiently dissolved in the inhalation composition, and if the amount of vitamin B3 is more than the above range, the effect of increasing the solubility of caffeine may be minimal.

[0025] According to one embodiment, an inhalable composition for enhancing wakefulness and vitality may comprise 2 to 15 wt% of the caffeine; 1 to 15 wt% of the vitamin B3; 1 to 20 wt% of the enhancer; and 45 to 96 wt% of the solvent, based on the total weight of the composition.

[0026] In one embodiment, the solvent dissolves the caffeine, vitamin B3, and enhancer, and may be included in an amount equal to the remainder of the total weight of the composition, excluding the caffeine, vitamin B3, and enhancer. In one embodiment, the solvent may be included in an amount of 45 to 96 wt% based on the total weight of the inhalable composition. In one embodiment, the solvent may be included in an amount of 55 to 85 wt% based on the total weight of the inhalable composition. In one embodiment, the solvent may be included in an amount of 70 to 80 wt% based on the total weight of the inhalable composition.

[0027] The solvent included in the inhalable composition according to one embodiment may include one or more of water, alcohol, propylene glycol, and vegetable glycerin. The solvent may dissolve caffeine, vitamin B3, and a booster.

[0028] According to one embodiment, the inhalable composition may further comprise sodium chloride in the solvent. For example, the solvent may comprise water and sodium chloride. The sodium chloride may be present in an amount of 0.5 to 1.5 wt% based on the total weight of water. Additionally, the sodium chloride may be present in an amount of 0.85 to 0.95 wt% based on the total weight of water.

[0029] As an example, the solvent included in the inhalable composition may include 98.5 to 99.5 wt% water and 0.5 to 1.5 wt% sodium chloride, based on the total weight of the solvent.

[0030] Meanwhile, in the inhalation composition according to the embodiment, the enhancer may include 1 to 20 wt% of glucose based on the total weight of the composition. Alternatively, the enhancer may include 1 to 20 wt% of magnesium based on the total weight of the composition.

[0031] Additionally, the enhancer may comprise 1 to 20 wt% of glucose and magnesium based on the total weight of the composition. When the enhancer comprises both glucose and magnesium, it may comprise 1 to 10 wt% of glucose and 1 to 10 wt% of magnesium. Additionally, it may comprise 1 to 8 wt% of glucose and 1 to 8 wt% of magnesium, or it may comprise 1 to 5 wt% of glucose and 1 to 5 wt% of magnesium.

[0032] The inhalable composition according to the embodiment may further comprise additives usable as an inhalable composition. For example, the inhalable composition may further comprise one or more flavoring agents or flavoring ingredients. As another example, when the inhalable composition is to be used in a metered dose inhaler, the inhalable composition may further comprise a propellant. However, the present invention is not limited thereto.

[0033] Meanwhile, according to an embodiment, an inhalation composition supply device may be provided, including a storage container 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 may be provided with an opening or the like for refilling the inhalation composition.

[0034] The inhalable composition for enhancing wakefulness and vitality according to one embodiment may be in a form that can be inhaled through an inhaler. The inhaler may take various forms, such as a metered-dose inhaler, a dry powder inhaler, or a nebulizer.

[0035] The inhalable composition may be in the form of a solid, a liquid, or a mixture of solid and liquid. For example, the inhalable composition may be a solid powder mixture of caffeine and a potent agent. Alternatively, the composition may be a solid powder in which caffeine, vitamin B3, and a potent agent are dissolved in a solvent, and the solvent is dried. The solid composition may be prepared as a dry powder that can be inhaled using a dry powder inhaler.

[0036] As another example, the inhalable composition may be in a liquid form, containing caffeine, vitamin B3, and a stimulant dissolved in a solvent. In one embodiment, the inhaler may be a nebulizer. The nebulizer can atomize the liquid inhalable composition, and the atomized composition can be administered to the respiratory tract of a person. In one embodiment, by inhaling the atomized inhalable composition, a wakefulness and energy-enhancing effect can be achieved.

[0037] In one embodiment, the inhaler may include an atomizer for atomizing an inhalable composition, a battery for powering the atomizer, and a supply port for supplying the atomized composition to the atomizer. As an example, an inhaler comprising an atomizer, a battery, and a supply port as described above may be a mist inhaler.

[0038] For example, the atomizer may be a jet type that uses compressed air to atomize the liquid composition, an ultrasonic type that uses high-frequency sound waves to atomize the liquid composition, a vibration type that applies vibration to a mesh to pass the liquid composition through the mesh to form fine particles, or a heating type that atomizes the liquid composition through heating.

[0039] Additionally, the inhaler according to one embodiment may include a heating element, which may control the rate of vaporization by operating the heating element. The heating element may be controlled by, but is not limited to, a separate switch provided externally to the inhalation composition delivery device.

[0040] In one embodiment, the atomized inhalable composition can be administered to a human respiratory tract through a delivery port. The delivery port may include a mouthpiece or mask positioned adjacent to the delivery port. The mouthpiece or mask may be physically connected to the delivery port.

[0041] As an example, the supply port may be connected to a separate mouthpiece, or the portion extending from the supply port may be the mouthpiece. As 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.

[0042] Hereinafter, the present invention will be described in more detail through examples and experimental examples. These examples are provided solely for illustrative purposes, and it will be apparent to those skilled in the art that the present invention is not limited by these examples.

[0043]

[0044] <Example>

[0045] An inhalable composition was prepared and its arousal and vitality-enhancing effects were measured. Specifically, the inhalable composition was administered orally or by inhalation to experimental animals, and its arousal and vitality-enhancing effects were measured through general behavioral tests and forced swimming ability tests.

[0046] 1. Experiment preparation

[0047] (1) Preparation of experimental animals

[0048] Experimental animals were C57BL / 6 male mice (10 weeks old) purchased from KOATECH after receiving approval from the Institutional Animal Care and Use Committee (IACUC). After acclimatization for one week in the breeding room of the KT&G Bio-Efficacy Evaluation Center (temperature 23±2℃, humidity 50±10%, 12-h light / dark cycle), they were used in the experiment.

[0049] (2) Verification of the effects of caffeine through oral administration

[0050] Caffeine was dissolved in 0.9% saline and administered orally to mice using a zonde at a dosage of 10 ml / kg, and then general behavioral experiments were conducted. C57BL / 6 mice were orally administered the samples of Experimental Examples 1 to 3 below, and then the number of movements, movement speed (mm / s), movement distance (meter), and movement time (sec) were measured for 1 hour using a LABORAS behavioral device.

[0051] Experimental Example 1 served as a control group, and only 10 ml / kg of 0.9% saline was administered orally. Experimental Example 2 involved administering 5 mg / kg of caffeine dissolved in 0.9% saline orally using a sonde. Experimental Example 3 involved administering 30 mg / kg of caffeine dissolved in 0.9% saline orally using a sonde. For each of Experimental Examples 1 to 3, the stimulating effect of caffeine was verified through general behavioral experiments, and the results are shown in Table 1 below.

[0052]

[0053] As a result of the measurement, it was confirmed that in Experimental Example 2, where caffeine was orally administered at a concentration of 5 mg / kg, there was almost no effect, and in Experimental Example 3, where caffeine was orally administered at a concentration of 30 mg / kg, an awakening effect was observed.

[0054]

[0055] 2. General behavioral tests on inhalation compositions

[0056] Inhalation compositions of comparative examples and examples were prepared and administered to mice by inhalation by spraying with a mist generator. The inhalation time (min) for the efficacy of each composition was measured, and the compositions were collected for 10 minutes using a sampling pump and Cambridge filter, and the TPM (Total Particulate Matter) concentration was calculated gravimetrically.

[0057] The inhalable compositions of Comparative Examples 1 to 5 and Examples 1 to 3 in Table 2 below were administered by inhalation to C57BL / 6 mice, and then the number of movements, movement speed (mm / s), movement distance (meter), and movement time (sec) for 1 hour were measured using a LABORAS behavioral device. All substances included in the inhalable compositions of Comparative Examples and Examples were dissolved in 0.9% saline solution and used.

[0058] Meanwhile, the control group for each comparative example and embodiment was 0.9% saline solution sprayed with a mist generator and administered to mice by inhalation.

[0059]

[0060] (1) Comparative Example 1

[0061] An inhalation composition (Comparative Example 1) containing 2 wt% caffeine was prepared by dissolving caffeine in 0.9% 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 effect compared to the control group.

[0062] (2) Comparative examples 2 to 4

[0063] Vitamin B3 was dissolved in 0.9% saline solution to prepare an inhalation composition containing 10 wt% of vitamin B3 (Comparative Example 2). In addition, glucose was dissolved in 0.9% saline solution to prepare an inhalation composition containing 10 wt% of glucose (Comparative Example 3), and magnesium was dissolved in 0.9% saline solution to prepare an inhalation composition containing 10 wt% of magnesium (Comparative Example 4).

[0064] The compositions of Comparative Examples 2 to 4 were sprayed using a mist generator and administered to mice by inhalation for 20 to 60 minutes. As a result of observing general behavior, it was confirmed that there was no significant difference in effect compared to the control group.

[0065] (3) Comparative Example 5

[0066] Caffeine and vitamin B3 were dissolved in 0.9% saline solution to prepare an inhalation composition (Comparative Example 5) containing 8 wt% caffeine and 10 wt% 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 the effect was observed when inhaled for more than 30 minutes.

[0067] (4) Example 1

[0068] Caffeine, vitamin B3, and glucose were dissolved in 0.9% saline solution to prepare an inhalation composition (Example 1) containing 8 wt% caffeine, 10 wt% vitamin B3, and 5 wt% glucose. 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 the effect appeared when inhaled for 10 minutes or longer.

[0069] (5) Example 2

[0070] Caffeine, vitamin B3, and magnesium were dissolved in 0.9% saline solution to prepare an inhalation composition (Example 2) containing 8 wt% caffeine, 10 wt% vitamin B3, and 5 wt% magnesium. 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 the effect appeared when inhaled for 20 minutes or longer.

[0071] (6) Example 3

[0072] Caffeine, vitamin B3, glucose, and magnesium were dissolved in 0.9% saline solution to prepare an inhalation composition (Example 3) containing 8 wt% caffeine, 10 wt% vitamin B3, 5 wt% glucose, and 5 wt% magnesium. 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 the effect appeared when inhaled for more than 5 minutes.

[0073]

[0074] 3. General behavioral tests and forced swimming tests for inhalation compositions

[0075] General behavioral experiments and forced swimming experiments were conducted on the inhalable compositions of the control group, comparative example 5, and examples 1 to 3. Each composition was sprayed with a mist generator and inhaled for 15 minutes to compare and examine the efficacy under the same conditions.

[0076] General behavioral experiments were conducted in the same manner as described in Section 2. General Behavioral Experiment Method above. For 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 tank and allowed to acclimate for 10 minutes. Then, 24 hours later, each composition was inhaled for 15 minutes, and the mice were placed in the 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.

[0077]

[0078] As a result, in both the general behavioral experiment and the forced swimming experiment, it was confirmed that the compositions containing glucose or magnesium (Examples 1 and 2) had superior efficacy compared to Comparative Example 5, and the composition containing both glucose and magnesium (Example 3) had very superior efficacy.

[0079] Among these, the results for the general behavioral experiment are shown in Figure 1. Using the LABORAS behavioral device, measurements were made for 1 hour. 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 of movement. At the top of the graphs for each comparative example 5 and examples 1 to 3, the increase rate compared to the control group is indicated.

[0080] Referring to Figure 1, it can be seen that in the overall general behavioral experiment results, the degree of increase in the effect of Comparative Example 5 is minimal compared to the control group, but the increase in effect of Examples 1 and 2 is large, and the increase in effect of Example 3 is even greater.

[0081] In particular, as can be seen from the results of the forced swimming experiment, the immobility time was somewhat shortened in Examples 1 and 2, but in the case of Example 3, the immobility time was significantly shortened to about 175 seconds, confirming that the effect of increasing awakening and vitality was excellent.

[0082] The results of the general behavioral experiment and the forced swimming experiment confirmed the awakening and vitality enhancing effects of the inhalable compositions of Examples 1 to 3.

[0083] The description of the above-described embodiments is merely illustrative, and those skilled in the art will understand that various modifications and equivalent other embodiments are possible from this. The above-described embodiments can still achieve appropriate results even if the described techniques are performed in a different order than the described method, and / or the described components are combined or combined in a different form than the described method, or are replaced or substituted with other components or equivalents. Accordingly, all differences that fall within the scope of equivalents to the content described in the claims should be construed as being included within the scope of protection defined by the claims.

Claims

1. In an inhalation composition for enhancing awakening and vitality, caffeine; and An inhalable composition comprising an enhancer comprising at least one selected from glucose and magnesium.

2. In paragraph 1, An inhalation composition, wherein the caffeine is contained in an amount of 15% by weight or less based on the total weight of the inhalation composition.

3. In paragraph 1, An inhalation composition, wherein the caffeine is contained in an amount of 8 wt% or less based on the total weight of the inhalation composition.

4. In paragraph 1, The above inhalable composition is, Vitamin B3; and An inhalation composition further comprising at least one solvent selected from the group consisting of water, alcohol, propylene glycol, and vegetable glycerin.

5. In paragraph 4, A composition for inhalation, wherein the caffeine and the vitamin B3 are contained in a weight ratio of 2:1 to 2:

3.

6. In paragraph 4, Based on the total weight of the above inhalable composition, The caffeine is 2 to 15 wt%; The above vitamin B3 is 1 to 15% by weight; The promoter is 1 to 20 wt%; and A composition for inhalation, wherein the solvent is contained in an amount of 45 to 96 wt%.

7. In paragraph 4, An inhalation composition, wherein the solvent comprises 98.5 to 99.5 wt% of water and 0.5 to 1.5 wt% of sodium chloride based on the total weight of the solvent.

8. In paragraph 6, An inhalable composition, wherein the enhancer comprises 1 to 10 wt% of glucose and 1 to 10 wt% of magnesium, based on the total weight of the inhalable composition.

9. A storage container in which an inhalation composition is stored, comprising caffeine; and an enhancer comprising at least one selected from glucose and magnesium; and An inhalation composition supply device comprising an inhaler to which the storage container is coupled.

10. In paragraph 9, An inhalation composition delivery device, wherein the inhaler is a metered-dose inhaler, a dry powder inhaler, or a nebulizer.

11. In paragraph 9, The above inhalable composition further comprises vitamin B3; and at least one solvent selected from the group consisting of water, alcohol, propylene glycol, and vegetable glycerin; An inhalation composition supply device, wherein the inhaler comprises an atomizer that atomizes the inhalation composition.

12. In paragraph 11, The above-mentioned atomizer is an inhalation composition supply device that atomizes the inhalation composition by a jet method, an ultrasonic method, a vibration method, or a heating method.

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