Oral moisturizing spray as well as preparation method and application thereof

Abstract

The invention relates to an oral cavity moisturizing spray which is characterized by comprising the following components in percentage by mass: 3-5% of an inducer, 1-5% of a preservative and the balance of water. 0.1 to 0.3 percent of accelerant; 0.2%-0.5% of a humectant; 2-3% of mucopolysaccharide; and the balance of water. Through scientific compatibility of the four functional components of the inducer, the accelerant, the humectant and the mucopolysaccharide compound, a synergistic effect chain of induced permeation, absorption promotion, long-acting water locking and film-forming protection is formed; in addition, glycerol is used as a permeation inducer, and oral mucosa intercellular spaces are quickly opened by utilizing the small molecule characteristic (molecular weight is 92Da) of glycerol, so that subsequent active ingredients are easier to permeate. Compared with the traditional polyethylene glycol inducer, the glycerol has higher biocompatibility and mucous membrane affinity.

Description

Technical Field

[0001] The invention relates to the technical field of oral moisturizers, and in particular to an oral moisturizing spray and a preparation method and application thereof. Background Art

[0002] In the existing technology, there is no special oral moisturizer product for alleviating the symptoms of dry mouth caused by water abstinence in patients with Sjogren's disease and perioperative period.

[0003] Currently, the most common way to relieve dry mouth for patients with Sjogren's disease is to drink water frequently, but this can only provide temporary relief and has limited effect on patients with severe symptoms and severe lack of saliva secretion. In addition, some patients will use some ordinary lip balm to apply on their lips to prevent chapped lips, but this has no effect on dryness inside the mouth.

[0004] For patients who suffer from dry mouth due to water abstinence during surgery, nursing staff usually wipe their lips with wet gauze. Although this can bring a slight sense of moisture, it cannot penetrate deeply into the mouth to relieve dryness. In addition, the moisture of wet gauze evaporates quickly and has a short moisturizing effect. Some patients also try to gargle with a small amount of water, but due to the strict requirements of the surgery, this approach carries a certain risk of aspiration and may cause serious postoperative complications. These existing methods have limitations and cannot effectively and safely solve the dry mouth problem of the target population.

[0005] Currently, no effective solution has been proposed for the problems of short moisturizing time, aspiration or postoperative complications existing in the relevant technologies. Summary of the invention

[0006] The purpose of the present invention is to provide an oral moisturizing spray and a preparation method and application thereof in view of the deficiencies in the prior art, so as to solve the problems existing in the related art such as short moisturizing time and the possibility of causing aspiration or postoperative complications.

[0007] To achieve the above object, the technical solution adopted by the present invention is:

[0008] An oral moisturizing spray, comprising the following components by weight:

[0009] Inducer 3-5%;

[0010] Accelerator 0.1-0.3%;

[0011] Moisturizer 0.2-0.5%;

[0012] Mucopolysaccharide 2-3%;

[0013] The balance is water.

[0014] In an embodiment of the present invention, the inducer is any one or more of polyethylene glycol 300, polyethylene glycol 400, polyethylene glycol 600, polyethylene glycol 1000, glycerol, butanediol, propylene glycol, pentanediol, and hexanediol.

[0015] Further, the inducer is 3-5% glycerol.

[0016] In an embodiment of the present invention, the promoter is any one or more of menthol, cineole, camphor, and spearmint oil.

[0017] Further, the promoter is 0.1-0.3% menthol.

[0018] In an embodiment of the present invention, the humectant is any one or more of sodium hyaluronate, ceramide, and trehalose.

[0019] Further, the humectant is a mixture of sodium hyaluronate and ceramide, and the mixing ratio is 0.2-0.5:0.05.

[0020] In an embodiment of the present invention, the mucopolysaccharide complex is any one or more of dextran, collagen, and chitosan.

[0021] Further, the mucopolysaccharide is 2-3% dextran.

[0022] A preparation method of an oral moisturizing spray, comprising the following steps:

[0023] First step, mixing the humectant and the water at a mixing temperature of 30°C - 50°C, and standing to obtain a first mixed solution;

[0024] Second step, sequentially adding the inducer and the mucopolysaccharide into the first mixed solution, and stirring evenly at a rotation speed of 150-250 rpm and a stirring time of 20-40 minutes to obtain a second mixed solution;

[0025] Third step, cooling the second mixed solution to 15°C - 25°C, adding the promoter, and stirring evenly to obtain a third mixed solution;

[0026] Fourth step, filtering the third mixed solution to obtain the oral moisturizing spray product.

[0027] In a preferred embodiment of the present invention, the standing time is 1.5-3 hours.

[0028] In a preferred embodiment of the present invention, the filtration is performed using a 0.15-0.5 μm sterile filter membrane.

[0029] In a preferred embodiment of the present invention, the oral moisturizing spray has a pH value of 6.5 - 7.5 and an osmotic pressure of 250 - 350 mOsm / L.

[0030] An application of an oral moisturizing spray, said application being for intraoperative treatment and postoperative care, wherein the intraoperative treatment is for xerosis treatment or adjuvant oral treatment;

[0031] The postoperative care is for relieving dry mouth symptoms after surgery.

[0032] The present invention adopts the above technical solutions. Compared with the prior art, it has the following technical effects:

[0033] 1. Through the scientific compatibility of four types of functional components of the inducer (glycerol), promoter (menthol), moisturizer (sodium hyaluronate + ceramide) and mucopolysaccharide complex (dextran) of the present invention, a synergistic action chain of "inducing penetration - promoting absorption - long - term water locking - film - forming protection" is formed.

[0034] 2. Glycerol (3 - 5%) as an osmotic inducer, using its small - molecule characteristics (molecular weight 92 Da) to quickly open the intercellular space of oral mucosal cells, making subsequent active ingredients more easily penetrate. Compared with traditional polyethylene glycol - based inducers, glycerol has higher biocompatibility (LD 50 > 10 g / kg) and mucosal affinity (contact angle reduced by 20%).

[0035] 3. Menthol (0.1 - 0.3%) stimulates the reflex secretion of salivary glands (clinical trials show that the secretion volume increases by 15 - 20%) by activating the TRPM8 cold - sensing receptor, and its microcirculation - promoting effect (capillary blood flow velocity increases by 8 - 12%) can accelerate the absorption of moisturizing components.

[0036] 4. Sodium hyaluronate (0.2 - 0.5%) and ceramide (0.05%) form a two - phase moisturizing system: sodium hyaluronate forms a three - dimensional network structure through intermolecular hydrogen bonds (water - holding capacity up to 1000 times its own weight), and ceramide fills the lipid bilayer of the stratum corneum (penetration depth up to 50 - 80 μm). The two work together to reduce the water evaporation rate on the mucosal surface by more than 40%.

[0037] 5. Dextran (2 - 3%) as a mucopolysaccharide complex forms a bioadhesive film through β - 1,3 / 1,6 glycosidic bonds (adhesion force ≥ 0.8 N / cm 2 ) and can maintain effective adhesion for more than 2 hours in the dynamic oral environment. Detailed implementation manners

[0038] To make the objectives, technical solutions and advantages of this application clearer and more understandable, the following describes and explains this application in combination with embodiments. It should be understood that the specific embodiments described herein are only used to explain this application and are not used to limit this application. Based on the embodiments provided in this application, all other embodiments obtained by those of ordinary skill in the art without creative efforts belong to the scope of protection of this application.

[0039] Referring to "embodiments" in this application means that specific features, structures or characteristics described in combination with embodiments can be included in at least one embodiment of this application. The appearance of this phrase in various positions in the specification does not necessarily refer to the same embodiment, nor is it an independent or alternative embodiment mutually exclusive with other embodiments. Those of ordinary skill in the art explicitly and implicitly understand that the embodiments described in this application can be combined with other embodiments without conflict.

[0040] The components used in the embodiments of the present invention are as follows:

[0041] The inducer is glycerol. Glycerol (3-5%) is used as a penetration inducer. Utilizing its small molecule characteristics (molecular weight 92 Da), it can quickly open the intercellular spaces of oral mucosal cells, making it easier for subsequent active ingredients to penetrate. Compared with traditional polyethylene glycol-based inducers, glycerol has higher biocompatibility (LD 50 > 10 g / kg) and mucosal affinity (contact angle reduced by 20%).

[0042] The promoter is menthol. Menthol (0.1-0.3%) activates the TRPM8 cold receptor, stimulates the reflex secretion of salivary glands (clinical trials show that the secretion volume increases by 15-20%), and at the same time its microcirculation promoting effect (capillary blood flow rate increases by 8-12%) can accelerate the absorption of moisturizing ingredients.

[0043] The moisturizer is composed of sodium hyaluronate (0.2-0.5%) and ceramide (0.05%) to form a biphasic moisturizing system: sodium hyaluronate forms a three-dimensional network structure through intermolecular hydrogen bonds (water holding capacity reaches 1000 times its own weight), and ceramide fills the lipid bilayer of the stratum corneum (penetration depth reaches 50-80 μm). The two work together to reduce the water evaporation rate on the mucosal surface by more than 40%.

[0044] The mucopolysaccharide is dextran. Dextran (2-3%) is used as a mucopolysaccharide complex and forms a bioadhesive film through β-1,3 / 1,6 glycosidic bonds (adhesive force ≥ 0.8 N / cm 2 ), and can maintain effective adhesion for more than 2 hours in the dynamic oral environment.

[0045] Example 1

[0046] This embodiment relates to the oral moisturizing spray in the present invention.

[0047] In this embodiment, the formula of the oral moisturizing spray is as follows:

[0048] The mass fraction of glycerol is 4%.

[0049] The mass fraction of menthol is 0.2%.

[0050] The mass fraction of sodium hyaluronate is 0.3%.

[0051] The mass fraction of ceramide is 0.05%.

[0052] The mass fraction of dextran is 2.5%.

[0053] The balance is water.

[0054] The preparation method of this embodiment is as follows:

[0055] Add the moisturizer to water and let it stand to obtain the first mixed solution. The water temperature is 35°C and the standing time is 2 hours.

[0056] Add the inducer and mucopolysaccharide to the first mixed solution in sequence and stir evenly to obtain the second mixed solution. The stirring speed is 200 rpm and the stirring time is 30 minutes.

[0057] After controlling the temperature of the second mixed solution, add the promoter and stir evenly to obtain the third mixed solution. The temperature control is 20°C - 25°C.

[0058] Filter the third mixed solution with a 0.3μm sterile filter membrane.

[0059] The pH value of the oral moisturizing spray in Example 1 is 7.2, and the osmotic pressure is 300 mOsm / L.

[0060] In this embodiment, the following advantages are available:

[0061] 1. The pH value of the moisturizing spray highly matches the natural pH of saliva (6.6 - 7.1), avoiding mucosal damage caused by acid-base imbalance (the apoptosis rate of cells < 5%).

[0062] 2. Through the osmotic compensation effect of glycerol and sodium hyaluronate, it precisely matches the plasma osmotic pressure (285 mOsm / L), eliminating the risk of tissue dehydration caused by hypertonic solutions.

[0063] Example 2

[0064] Compared with Example 1, the proportion of ceramide in the present invention is relatively low.

[0065] In this embodiment, the formula of the oral moisturizing spray is as follows:

[0066] The mass fraction of glycerol is 3%.

[0067] The mass fraction of menthol is 0.1%.

[0068] The mass fraction of sodium hyaluronate is 0.2%.

[0069] The mass fraction of ceramide is 0.02%.

[0070] The mass fraction of dextran is 2%, and the balance is water.

[0071] The preparation method of this example is the same as that of Example 1.

[0072] The pH value of the oral moisturizing spray of Example 2 is 7.2, and the osmotic pressure is 300 mOsm / L.

[0073] Ceramide is an important lipid component in the skin stratum corneum, and its main functions are to maintain the skin barrier, moisturize and anti-inflammation.

[0074] Compared with Example 1, the proportion of ceramide in the present invention is relatively low.

[0075] If the content of ceramide in the mouthwash is relatively low, it may lead to insufficient moisturizing performance of the mouthwash, and a dry feeling may occur in the mouth after use. If a mouthwash with a low ceramide content is used for a long time, it may indirectly cause chronic oral mucosal problems, such as repeated inflammation or mucosal desquamation.

[0076] Example 3

[0077] Compared with Example 1, the proportion of ceramide in the present invention is relatively high.

[0078] In this example, the formula of the oral moisturizing spray is as follows:

[0079] The mass fraction of glycerol is 5%.

[0080] The mass fraction of menthol is 0.3%.

[0081] The mass fraction of sodium hyaluronate is 0.5%.

[0082] The mass fraction of ceramide is 0.1%.

[0083] The mass fraction of dextran is 3%.

[0084] The balance is water.

[0085] The preparation method of this example is the same as that of Example 1.

[0086] The pH value of the oral moisturizing spray of Example 3 is 7.2, and the osmotic pressure is 300 mOsm / L.

[0087] Ceramide is an important lipid component in the stratum corneum of the skin, and its main functions are to maintain the skin barrier, moisturize, and have anti-inflammatory effects.

[0088] Compared with Example 1, the proportion of ceramide in the present invention is relatively high.

[0089] After use, there may be a "film feeling of oil" remaining in the oral cavity, which affects the freshness, and even makes people feel "not rinsed clean", reducing the usage experience. An appropriate amount of ceramide is helpful for mucosal health, but an excessive amount may change the oral environment. An overly high amount of ceramide may hinder its penetration and reduce the bactericidal / anti-inflammatory effect. In addition, too much lipid may interfere with the normal secretion of saliva or the microbial balance, and in the long term, it may affect the oral self-cleaning function and even indirectly promote the growth of certain anaerobic bacteria.

[0090] The technical features of the above-described embodiments can be combined arbitrarily. For the sake of brevity of description, not all possible combinations of the technical features in the above embodiments are described. However, as long as there is no contradiction in the combination of these technical features, it should be considered as the scope described in this specification.

[0091] The above-described embodiments only represent several implementation manners of the present application. The description is relatively specific and detailed, but it should not be construed as a limitation on the scope of the invention patent. It should be noted that for those of ordinary skill in the art, without departing from the concept of the present application, several modifications and improvements can still be made, and these all belong to the protection scope of the present application. Therefore, the protection scope of the patent of the present application shall be subject to the appended claims.

Claims

1. An oral moisturizing spray, characterized in that, By mass fraction, it includes the following components: Inducing agent 3 - 5%; Accelerating agent 0.1 - 0.3%; Humectant 0.2 - 0.5%; Mucopolysaccharide 2 - 3%; The balance is water.

2. An oral moisturizing spray as described in claim 1, characterized in that The inducing agent is any one or more of polyethylene glycol 300, polyethylene glycol 400, polyethylene glycol 600, polyethylene glycol 1000, glycerol, butanediol, propylene glycol, pentanediol, hexanediol; The accelerating agent is any one or more of menthol, cineole, camphor, spearmint oil.

3. An oral moisturizing spray as described in claim 2, characterized in that The inducing agent is 3 - 5% glycerol; The accelerating agent is 0.1 - 0.3% menthol.

4. An oral moisturizing spray as described in claim 1, characterized in that The humectant is any one or more of sodium hyaluronate, ceramide, trehalose.

5. An oral moisturizing spray as described in claim 4, characterized in that The humectant is a mixture of sodium hyaluronate and ceramide, and the mixing ratio is 0.2 - 0.5:0.

05.

6. An oral moisturizing spray as described in claim 1, characterized in that The mucopolysaccharide complex is any one or more of dextran, collagen, chitosan.

7. An oral moisturizing spray as described in claim 6, characterized in that The mucopolysaccharide is 2 - 3% dextran.

8. The preparation method of an oral moisturizing spray according to any one of claims 1-7, characterized in that, It includes the following steps: The first step is to mix the humectant and the water at a mixing temperature of 30°C - 50°C, and let it stand to obtain the first mixed solution; The second step is to sequentially add the inducing agent and the mucopolysaccharide into the first mixed solution, and stir evenly at a rotation speed of 150 - 250 rpm and a stirring time of 20 - 40 minutes to obtain the second mixed solution; The third step is to cool the second mixed solution to 15°C - 25°C, then add the accelerating agent, and stir evenly to obtain the third mixed solution; The fourth step is to filter the third mixed solution to obtain the oral moisturizing spray product.

9. A preparation method of an oral moisturizing spray as described in claim 8, characterized in that The standing time is 1.5 - 3 hours. The filtration is carried out by filtering with a 0.15 - 0.5 μm sterile filter membrane. The pH value of the oral moisturizing spray is 6.5 - 7.5, and the osmotic pressure is 250 - 350 mOsm / L.

10. Use of an oral moisturizing spray as described in claims 1-7, characterized in that, The application is for intraoperative treatment and postoperative care. The intraoperative treatment is for the treatment of xerosis or auxiliary oral treatment; The postoperative care is for the care of relieving dry mouth symptoms after surgery.