Oral care composition including exothermic reaction

Abstract

The present invention relates to a thermoresponsive oral composition, and more specifically, comprises as active ingredients a thermogenic component including a thermogenic anhydrous salt; and a pharmacological component having pharmacological activity, wherein the pharmacological component comprises one or more of myrrh tincture, ratania tincture, chamomile tincture, and centella quantitative extract. According to the present invention, there is an advantage in that blood circulation in the gums is promoted by a sensation of heat through the interaction between the thermogenic component and the pharmacological component, and the absorption of the pharmacological component having anti-inflammatory and tissue regeneration activities is enhanced, thereby effectively improving periodontal diseases such as periodontitis and gingivitis.

Description

Technology Field

[0001] The present invention relates to a thermoresponsive oral composition, and more specifically, to a thermoresponsive oral composition that induces a thermoreactive reaction upon contact with saliva in the oral cavity by including a thermogenic component. Background Technology

[0003] For a long time, oral health compositions have been dominated by oral hygiene-focused products such as toothpaste, mouthwash, and oral gel; however, these compositions have been limited to superficial and short-term functions, such as cleaning, cavity prevention, and bad breath removal. In particular, technologies that provide substantial physiological and pharmacological improvements for chronic inflammatory diseases occurring within the gums, such as periodontitis and gingivitis, are relatively lacking.

[0004] Some technologies have proposed toothpaste compositions that provide a warm sensation upon use by utilizing moisture-reactive exothermic ingredients such as anhydrous salts. However, there is a disadvantage in that safe use in the oral cavity is difficult because it is difficult to control the intensity and duration of the exothermic reaction, resulting in excessive or irregular heat generation. Additionally, due to the characteristics of exothermic anhydrous salts, it is difficult to establish a stable formulation, and there are disadvantages such as poor long-term shelf life due to the occurrence of early exothermic reactions.

[0005] Furthermore, conventional heat-generating toothpaste compositions do not go beyond the level of general fluoride-based toothpastes for hygiene, and no concept has been presented to utilize the thermal response for the purpose of physiological improvement or assisting in the treatment of periodontal tissues.

[0006] Therefore, there is a need to develop a new concept of oral thermotherapy composition that can directly contribute to the improvement of oral diseases while efficiently controlling the fever response. Prior art literature

[0008] (Patent Document 0001) KR 10-2006-0089892 A The problem to be solved

[0009] The objective of the present invention is to provide a thermoresponsive oral composition that enhances the action of pharmacological components by improving their penetration and absorption into gum tissue, by inducing a thermogenic reaction within the oral cavity through the inclusion of a thermogenic component and a pharmacological component having functionalities such as anti-inflammatory and antibacterial properties.

[0010] Another objective of the present invention is to provide a thermoresponsive oral composition that induces a safe and continuous thermoreactive response by additionally including a control component for controlling the exothermic performance, has excellent storage stability so that there is no premature heating or performance degradation even during long-term storage, and is easy to manufacture into various formulations.

[0011] Another objective of the present invention is to provide a thermoresponsive oral composition that maximizes the preventive or improving effect of any one of periodontitis, gingivitis, gum pain, gum bleeding, bad breath, and gum sensitivity through the interaction of a thermogenic agent and a pharmacological component. means of solving the problem

[0013] The thermogenic oral composition of the present invention for achieving the above-mentioned purpose comprises, as active ingredients: a thermogenic component comprising a thermogenic anhydrous salt; and a pharmacological component having pharmacological activity, wherein the pharmacological component comprises one or more of myrrh tincture, ratania tincture, chamomile tincture, and centella quantitative extract.

[0014] The above active ingredient further comprises a control ingredient that controls the exothermic temperature and duration of the exothermic ingredient, wherein the control ingredient comprises 2,3-butanediol.

[0015] The above-mentioned exothermic anhydrous salt is characterized as being anhydrous magnesium sulfate (MgSO4).

[0016] Based on 100% by weight of the above oral composition, the active ingredients are characterized by containing 0.1 to 10% by weight of a pharmacological component, 0.1 to 5% by weight of a control component, and 0.1 to 5% by weight of a control component.

[0017] The above oral composition is characterized by further including a wetting agent and a viscosity modifier.

[0018] The above oral composition is characterized by further including an abrasive, a flavoring agent, and a sweetener.

[0019] The above oral composition is characterized by a thermal reaction of 37 to 42°C that lasts for 180 seconds upon contact with saliva in the oral cavity.

[0020] The above oral composition is characterized by being formulated in the form of a paste-type toothpaste.

[0021] The above oral composition is characterized by being formulated as any one of the following: gel type, liquid type, powder type, tablet type, gargle type, mouthwash type, oral spray type, oral foam type, aerosol type, adhesive type, oral film type, oral patch type, oral sheet type, lozenge type, and oral medical aid type.

[0022] The above-mentioned pharmacological component and pharmacological component are stored separately, characterized by being stored separately through one of the following packaging structures: a separate storage type packaging structure, a multi-chamber type packaging structure, a capsule-embedded type packaging structure, or a microcapsule type packaging structure.

[0023] The above oral composition is for the prevention or improvement of any one of periodontitis, gingivitis, gum pain, gum bleeding, bad breath, and gum sensitivity, and is characterized as being a cosmetic composition, a quasi-drug composition, or a pharmaceutical composition. Effects of the invention

[0025] According to the present invention, there is an advantage in that periodontal diseases such as periodontitis and gingivitis can be effectively improved by promoting blood circulation in the gums through a warming sensation via the interaction of a thermal component and a pharmacological component, and by enhancing the absorption of pharmacological components having anti-inflammatory and tissue regeneration activities. In addition, there is an advantage in that a thermal reaction in the range of 37 to 42°C is induced for a certain period of time. Furthermore, there is an advantage in that a novel thermal-based oral care platform can be established by having excellent long-term storage stability and being easy to formulate into various formulations. Specific details for implementing the invention

[0027] The present invention will be described in detail below.

[0028] The most significant feature of the present invention is that by including both a thermogenic component and a pharmacological component, it induces a thermal response in the oral environment, thereby improving the delivery of pharmacological activity of the pharmacological component and biological response. In other words, it enhances the physiological response of periodontal tissues through a thermogenic oral composition. Furthermore, it is characterized by ensuring a stable and continuous thermal response through the use of a control component.

[0030] The thermoresponsive oral composition of the present invention comprises, as active ingredients: a thermogenic component comprising a thermogenic anhydrous salt; and a pharmacological component having pharmacological activity.

[0031] Hereinafter, the weight % used in the present invention is based on 100 weight % of the oral composition.

[0033] First, the exothermic component is a component that causes an exothermic reaction upon contact with moisture and includes an exothermic anhydrous salt. Furthermore, it is most preferable to use anhydrous magnesium sulfate (MgSO4) as the exothermic anhydrous salt. This is because, while anhydrous magnesium sulfate generates heat through a hydration reaction upon contact with water or saliva—similar to other conventional exothermic salts—it is easier to precisely control the intensity and duration of the exothermic reaction using a control component.

[0034] The above-mentioned pyrogen is included in the composition in an amount of 0.1 to 10 weight percent. This is because if the content is less than 0.1 weight percent, the pyrogen reaction is insufficient, and if it exceeds 10 weight percent, it becomes an excess amount, which induces an excessive reaction and can irritate the mucous membrane.

[0036] In addition, the above pharmacological component provides pharmacological effects in the oral cavity by having one or more physiological activities among antibacterial, anti-inflammatory, and tissue regeneration, and uses one or more, preferably two or more, and most preferably all four of myrrh tincture, rhatany tincture, chamomile tincture, and Centella asiatica standardized extract. Since these four types of natural extracts are already sufficiently known in the field to which this technology belongs, further explanation regarding them is omitted.

[0037] The above-mentioned natural extract has physiological activities such as anti-inflammatory, astringent, soothing, antioxidant, and tissue-protective properties, and exhibits excellent effects in alleviating symptoms of periodontal disease, stomatitis, and tooth sensitivity through synergistic effects with increased blood circulation and enhanced tissue penetration promoted by the thermal reaction of the pyrogenic component.

[0038] The above natural extract is included in the composition at 0.1 to 5 weight percent. This is because if the content is less than 0.1 weight percent, the pharmacological effect is insufficient, and even if it exceeds 5 weight percent, no further enhanced effect is observed, resulting in reduced economic feasibility.

[0040] The oral composition according to the present invention must include the two essential components described above in the compositional ratios described above, and the remainder may be an auxiliary component described below, or a formulation component required for formulation generally used in the field to which this technology belongs, and most simply, purified water.

[0042] As previously explained, the oral composition described above has the advantage of improving the delivery of pharmacological activity of pharmacological components and biological responses through the thermothermal reaction of the pharmacological component.

[0043] However, since it may be difficult to control the intensity and duration of the exothermic reaction if only the exothermic component and the pharmacological component are included as active ingredients, it is preferable in the present invention to further include a control component as an active ingredient that controls the exothermic temperature and duration of the exothermic component.

[0044] The above-mentioned control component is intended to control the exothermic temperature and duration of the above-mentioned exothermic component and includes 2,3-butanediol. Since the 2,3-butanediol forms a multiple hydrogen bond network centered on two adjacent hydroxyl groups (vicinal diol) structures, through this multiple hydrogen bond network, it mitigates the hydration rate of the exothermic anhydrous salt, disperses the exothermic reaction over time, suppresses excessive heat peaks, forms a soft and continuous warmth, and increases the sensation of retention in the oral cavity, thereby contributing to the improvement of the duration, usability, and stability of the warming sensation.

[0045] It is preferable that such control components be included in the composition at a concentration of 0.1 to 5 weight percent. If the content is less than 0.1 weight percent, the formation of a multiple hydrogen bond network by 2,3-butanediol is insufficient, which fails to control the rapid hydration reaction of the pyrogenic anhydrous salt, thereby causing a risk of burns to the oral mucosa or shortening the duration of the heat. Conversely, if it exceeds 5 weight percent, excessive hydration inhibition may delay the time to reach the target effective heat range (37 to 42°C) or lower the maximum temperature, resulting in insufficient enhancement of the penetration of pharmacological components. Furthermore, this is because a high concentration of butanediol may compromise formulation stability by rapidly reducing the viscosity of the composition through interaction with viscosity modifiers in the formulation, making it difficult to maintain the shape of paste formulations such as toothpaste, or causing layer separation during long-term storage.

[0047] In addition, it is preferable that the oral composition of the present invention further includes a viscosity modifier and a wetting agent.

[0048] The above viscosity modifier maintains the components within the composition uniformly, controls the rate of the hydration reaction to prevent the sudden occurrence of a warming sensation, and provides persistence. One or more of sodium carboxymethylcellulose (CMC-Na), xanthan gum, sodium alginate, hydroxyethylcellulose (HEC), and carbomer are used as such viscosity modifiers.

[0049] The above viscosity modifier is included in the composition at 0.1 to 3 weight percent. This is because if the content is less than 0.1 weight percent, it is difficult to control the rate of the hydration reaction, and if it exceeds 3 weight percent, it becomes an excess amount, which reduces economic efficiency.

[0050] The above humectant is used to maintain moisture in the formulation, control the exothermic reaction, and improve the feel of use; it suppresses the early reaction of pyrogenic anhydrous salts and contributes to the formation of a more uniform exothermic environment and a stable formulation structure by imparting viscosity and moisturizing properties. One or more of D-sorbitol solution, glycerin, and polyethylene glycols such as PEG-8 and PEG-12 are used as the humectant.

[0051] It is preferable that the above wetting agent be used in an amount of 20 to 60 weight percent in the composition.

[0053] In addition, the oral composition of the present invention may further include an abrasive, a flavoring agent, and a sweetener.

[0054] The above abrasive is intended to improve tooth surface cleaning power and remove plaque, and when combined with a thermal reaction, it provides both tooth surface cleaning power and a warm sensation of use. As such an abrasive, one or more of the conventionally known precipitated calcium carbonate, calcium carbonate, tricalcium phosphate, hydrated silica, dental-type silica, and sodium bicarbonate may be used.

[0055] The above abrasive is preferably included in the composition in an amount of 5 to 25 weight percent, but is not limited thereto.

[0056] One or more of the above-mentioned flavorings are mint oil, spearmint oil, piperita oil, and menthol, and one or more of the above-mentioned sweeteners are xylitol and steviol glycosides, and a pleasant oral sensation that harmonizes with the warming sensation is achieved by complementing the taste and aroma of the composition.

[0057] It is preferable that the above flavoring and sweeteners be included in the composition in an amount of 0.1 to 1 weight percent each, but this is not limited thereto.

[0059] The oral composition of the present invention provides synergy to the effects of pharmacological components in improving periodontal disease, stomatitis, and tooth sensitivity by maintaining a thermal reaction of 37 to 42°C for 180 seconds upon contact with saliva in the oral cavity. In addition, by controlling the heat intensity and duration, the user experience is improved, and stable storage of the thermal component is possible, resulting in excellent long-term storage stability.

[0061] Furthermore, the oral composition of the present invention may be used for the prevention or improvement of any one of periodontitis, gingivitis, gum pain, gum bleeding, bad breath, and gum sensitivity, but is not limited thereto.

[0062] In addition, it is most preferable for the oral composition to be implemented in a paste-type toothpaste formulation. However, the oral composition of the present invention may also be formulated as any one of a gel type, liquid type, powder type, tablet type, gargle type, mouthwash type, oral spray type, oral foam type, aerosol type, adhesive type, oral film type, oral patch type, oral sheet type, lozenge type, or oral medical aid type, and any formulation is acceptable as long as it is for the prevention or improvement of any one of periodontitis, gingivitis, gum pain, gum bleeding, bad breath, and gum sensitivity.

[0064] The composition according to the present invention may be a quasi-drug composition for the prevention or improvement of any one of periodontitis, gingivitis, gum pain, gum bleeding, bad breath, and gum sensitivity. In addition, it may be a pharmaceutical composition. Furthermore, the components included in the pharmaceutical or quasi-drug composition of the present invention may include, in addition to the components described above, components commonly used in oral quasi-drug compositions or oral pharmaceutical compositions, such as binders, foaming agents, preservatives, flavoring agents, coloring agents, solvents, thickeners, solubilizers, or pH adjusters.

[0065] The oral quasi-drug or pharmaceutical composition of the present invention can be manufactured in any formulation conventionally produced in the art.

[0067] The composition according to the present invention may be a cosmetic composition for preventing or improving any one of periodontitis, gingivitis, gum pain, gum bleeding, bad breath, and gum sensitivity.

[0068] The cosmetic composition of the present invention may be prepared by including a cosmetically effective amount of the aforementioned ingredients and a cosmetically acceptable carrier. In this specification, the cosmetically effective amount refers to an amount sufficient to achieve the antibacterial efficacy of the composition of the present invention described above. Furthermore, the form of the cosmetic composition contains a cosmetically or dermatologically acceptable medium or base. This includes any formulation suitable for topical application and does not limit its implementation.

[0070] Meanwhile, although the present invention can control early fever through a control component using a pyogenic component and a pharmacological component, it is obvious that the pyogenic component and the pharmacological component may be stored separately as needed.

[0071] In the present invention, the separation storage is achieved by a packaging structure, and is implemented through any one of the following packaging structures: a separation storage type packaging structure such as a pouch, a multi-chamber type packaging structure, a capsule-embedded type packaging structure, or a microcapsule type packaging structure. When packaging in the capsule-embedded type, microcapsule type, etc., the component packaged inside the capsule may be a pharmacological component or a pharmacological component, and is not limited thereto.

[0073] The present invention will be explained in more detail below through examples.

[0074] (Example 1)

[0075] A paste-type toothpaste composition was prepared with the composition shown in Table 1 below. After mixing the above-mentioned exothermic component, control component, and humectant, a viscosity modifier, pharmacological component, abrasive, flavoring, sweetener, and solvent were mixed therein to prepare the toothpaste composition.

[0077] Composition of Example 1 division weight% pyrogen Pyrogenic anhydrous magnesium sulfate 5 Control component 2,3-butanediol 2.5 Pharmacological components Myrrh tincture 0.5 Ratania Tincture 0.5 Chamomile Tincture 0.5 Centella quantitative extract 0.5 humectant Sorbitol liquid 40 abrasive silicon dioxide 10 viscosity modifier Xanthan sword 1.5 spices menthol 0.5 sweetener xylitol 0.5 menstruum purified water to 100

[0079] (Test Example 1)_Evaluation of Heat Generation Characteristics

[0080] In order to confirm whether the above Example 1 exhibits a stable and constant thermal response in the oral cavity, the heat-generating properties were evaluated under artificial saliva conditions.

[0081] After contacting 1 g of the sample with 1 mL of artificial saliva maintained at 37°C, the temperature change was measured using a micro-temperature sensor for 0 to 180 seconds. As a control group, regular toothpaste without a heating function was measured under the same conditions. The results are shown in Table 2 below.

[0084] Results of Test Example 1 Time (sec) Example 1 control group 0 37.0℃ 37.0℃ 15 38.9℃ 37.1℃ 30 40.6℃ 37.1℃ 60 40.1℃ 37.2℃ 120 39.0℃ 37.1℃ 180 38.5℃ 37.0℃

[0085] As can be seen in Table 2 above, Example 1 of the present invention generated a gentle warmth in the range of approximately 39–41°C immediately after application and exhibited a stable temperature profile that continued gradually for about 3 minutes or more. On the other hand, no significant temperature increase was observed with ordinary toothpaste.

[0086] These exothermic characteristics were interpreted as the result of the exothermic rate and peak temperature being controlled by the hydration reaction of anhydrous magnesium sulfate and a sustained control matrix structure combined with a wetting agent, a viscosity modifier, and 2,3-butanediol.

[0088] (Test Example 2)_Evaluation of Bactericidal Effect on Causative Bacteria of Periodontitis

[0089] In order to confirm whether Example 1 of the present invention exhibits a bactericidal effect against Porphyromonas gingivalis, a major causative agent of periodontitis, a test was conducted in accordance with the “Guidelines for the Efficacy Evaluation of External Disinfectants (Quasi-drugs) (Ministry of Food and Drug Safety, 2014).”

[0090] Test bacteria with adjusted bacterial counts were placed in the test group and control group (PBS) and stirred at room temperature. After 24 hours, the mixture was centrifuged at 13,000 rpm to remove the supernatant, and washed twice with PBS. Next, the test group and control group were serially diluted, inoculated into the culture medium, and the CFU counted to calculate the reduction rate.

[0091] The culture conditions were as follows.

[0092] P. gingivalis: 37°C, anaerobic conditions, 14-day culture, 5% Blood TSA + H / M medium

[0094] Test strain Initial dose (CFU / mL) Control group (CFU / mL) Test group (CFU / mL) Decrease rate (%) P. gingivalis 1.42×10 5 84,300 ND (Not Detected) 99.9

[0095] As shown in Table 3 above, Example 1 of the present invention showed 4 to 6 times higher inhibitory power against periodontal bacteria compared to the control group, which is a regular toothpaste.

[0097] (Test Example 3)_Storage Stability

[0098] A stability test was performed under accelerated conditions to confirm whether the anhydrous magnesium sulfate in Example 1 of the present invention does not react prematurely and whether the formulation characteristics do not change even during long-term storage. At this time, as a comparative example, toothpaste was prepared with the same composition as Example 1, but without using 2,3-butanediol, which is a heat control component.

[0099] Storage conditions

[0100] 40℃±2℃ (accelerated test conditions), 75% RH, 4 weeks

[0101] Shading conditions

[0102] chest

[0103] Measurement items

[0104] Appearance (phase separation, color change, etc.)

[0105] Viscosity change (% rate of change)

[0106] pH change

[0107] Assessment of potential for fever reaction (presence of fever upon contact with artificial saliva)

[0108] Changes in odor and uniformity

[0109] All measurements were taken at weeks 0, 2, and 4.

[0111] Changes in appearance division 0 weeks 2 weeks 4 weeks Example 1 No change No change No change Comparative example No change Weak separation Deepening separation (layer separation) control group No change No change No change

[0112] As shown in Table 4 above, it was confirmed that Example 1 of the present invention and the control group showed no change for 4 weeks. On the other hand, in the comparative example, weak separation was observed starting from 2 weeks, and layer separation was observed after 4 weeks.

[0114] Viscosity change division 0 weeks 4 weeks Viscosity change rate Example 1 100% 97% -3% Comparative example 100% 82% -18% control group 100% 98% -2%

[0115] As shown in Table 5 above, it was confirmed that Example 1 of the present invention and the control group were stable with almost no change in viscosity, but it was confirmed that the comparative example had a large decrease in viscosity, which increased the risk of separation.

[0117] pH change division 0 weeks 4 weeks Example 1 6.75 6.72 Comparative example 6.76 6.48 control group 6.80 6.78

[0118] As shown in Table 6 above, Example 1 of the present invention was confirmed to have excellent stability with almost no change in pH.

[0120] Early onset of fever (no contact with artificial saliva) division 1 week 2 weeks 4 weeks Example 1 No fever No fever No fever Comparative example No fever Fine heat traces Increase in contact surface temperature control group No fever No fever No fever

[0121] As shown in Table 7 above, Example 1 of the present invention confirmed that there were no early, hydration, or fever reactions when artificial saliva was not in contact. On the other hand, the comparative example confirmed that local fever occurred in a certain area after 4 weeks.

[0123] Results of pyrogenic response measurement after 4 weeks of storage division Highest temperature Duration Example 1 40.2℃ Maintain for 180 seconds Comparative example 37.8℃ Hold for 90 seconds control group No change doesn't exist

[0124] As shown in Table 8 above, Example 1 of the present invention maintained a maximum temperature of 40.2°C and a duration of 180 seconds, maintaining the same heating performance as before storage, whereas Comparative Example 1 showed a maximum temperature of 37.8°C, which was 2.2°C lower than before storage, indicating a decrease in heating performance, and also a duration of 90 seconds, which was reduced by more than 50%.

[0126] As can be confirmed through the aforementioned test examples, the oral composition of the present invention induces a stable thermothermal response within the oral cavity through the interaction of the pharmacological component, the pharmacological component, and the control component. By enhancing the mucosal penetration and pharmacological activity of the pharmacological component, it was confirmed that the oral composition exhibits superior efficacy in improving oral diseases compared to conventional oral compositions. Furthermore, it was confirmed that there are no issues regarding premature heating of the pharmacological component or performance degradation even during long-term storage.

[0128] Foregoing, specific parts of the present invention have been described in detail. It will be apparent to those skilled in the art that such specific descriptions are merely preferred embodiments and do not limit the scope of the invention. Accordingly, the actual scope of the invention is defined by the appended claims and their equivalents.

Claims

Claim 1 A thermogenic oral composition characterized by comprising, as active ingredients: a thermogenic component; a pharmacological component having pharmacological activity; and a control component controlling the thermogenic temperature and duration of the thermogenic component, wherein the thermogenic component is anhydrous magnesium sulfate (MgSO4), the pharmacological component comprises one or more of myrrh tincture, ratania tincture, chamomile tincture, and centella quantitative extract, and the control component is 2,3-butanediol. Claim 2 delete Claim 3 A thermoreactive oral composition according to claim 1, characterized in that, based on 100% by weight of the oral composition, it comprises 0.1 to 10% by weight of anhydrous magnesium sulfate as the active ingredient, 0.1 to 5% by weight of a pharmacological ingredient, and 0.1 to 5% by weight of 2,3-butanediol. Claim 4 A thermoresponsive oral composition according to claim 1, characterized in that the oral composition further comprises a wetting agent and a viscosity modifier. Claim 5 A thermoresponsive oral composition according to claim 1, characterized in that the oral composition further comprises an abrasive, a flavoring agent, and a sweetener. Claim 6 A thermoresponsive oral composition according to any one of claims 1, 3 to 5, characterized in that the oral composition sustains a thermoreactive reaction of 37 to 42°C for 180 seconds upon contact with saliva in the oral cavity.

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