Toothpaste containing saffron extract

Abstract

An oral care composition, the composition at least containing saffron extract, water, a polyol and lecithin.

Description

[0001] TOOTHPASTE CONTAINING SAFFRON EXTRACT

[0002] Description

[0003] The invention relates to a dental care composition, a toothpaste, and a tube containing the composition. The invention further relates to the use of the composition and the use of chlorophyll for coloring a toothpaste.

[0004] In the cosmetics and dental care sectors, customer demands and regulatory requirements increasingly require sustainable products containing naturally occurring ingredients. One goal is to avoid microplastics. At the same time, there is still a need for dental care formulations that enable effective cleaning and care of teeth and gums.

[0005] The present invention is based on the objective of providing an improved composition for effectively cleaning and caring for teeth and gums. The composition should contain the most sustainable and naturally occurring ingredients possible, be as digestible as possible, and be positively received by humans both psychologically and physiologically.

[0006] According to the invention, this object is achieved by a composition according to claim 1.

[0007] The invention is based on the idea of ​​providing a composition for dental care which contains at least one saffron extract, water, a polyol and lecithin.

[0008] The term “dental care” includes the care and cleaning of both the gums and the teeth.

[0009] Using sustainable and, wherever possible, naturally occurring ingredients, a microbiologically and thermodynamically stable composition is created that can effectively care for and clean teeth and gums. The composition according to the invention is particularly well-tolerated, both physiologically and psychologically. The composition also does not need to be spit out or rinsed out, allowing the ingredients to work longer. The composition according to the invention can deliver hydrophilic and lipophilic active ingredients to the site of action, as well as absorb hydrophilic and lipophilic contaminants and remove them from teeth and gums.

[0010] Saffron extract can inhibit harmful germs and thus helps care for gums and teeth. Saffron extract is an extract from the saffron plant (Crocus sativus), preferably a saffron flower extract. The extract can be obtained, for example, by macerating dried flowers of the Crocus sativus plant. The pistils are preferably removed beforehand. A mixture of 30% 1,3-propanediol and 70% water can be used as an extraction agent.

[0011] Water and polyol provide the basis for a polar phase and serve as carriers for hydrophilic active ingredients, capable of removing impurities removed during the intended application. The composition according to the invention can also contain one or more lipids that form a non-polar phase. The lipids can be active ingredients or carriers for lipophilic active ingredients and can remove lipophilic impurities removed during the intended application. The emulsifier lecithin can be positioned between the polar and non-polar phases. The composition according to the invention can deliver lipophilic and hydrophilic active ingredients to the site of action simultaneously. Thus, in addition to the physical cleansing action, the composition according to the invention allows saffron extract, ubiquinone-10, or ubiquinol, for example, to exert their beneficial effect at the site of action and care for gums and teeth.

[0012] The polyol contributes to preservation, and no additional preservatives are required. This eliminates the need for synthetic or allergenic preservatives. The polyol also has a beneficial effect on taste and mouthfeel. Lecithin is a preparation containing phosphatidylcholines as its main ingredient. Phosphatidylcholines are l,2-diacyl-sn-glycero-3-phosphocholines, phospholipids in which phosphoric acid is esterified with diacylglycerol and choline. Lecithin is approved for foodstuffs in general (except for certain foodstuffs) under the number E 322 according to the Food Additives Approval Ordinance (ZZulV 1998).

[0013] Emulsifiers other than lecithin are not required in the composition according to the invention. Lecithin can be used in small amounts compared to the substances to be emulsified. For example, the mass of lecithin can be as little as 5% of the mass of the lipid to be emulsified. A further advantage is that lecithins are of natural origin. Thus, no synthetic surfactants are required.

[0014] The composition according to the invention preferably contains 0.1 g to 4 g of lecithin per 100 g of the composition. The lecithin has a phosphatidylcholine content of 30 wt.% to 100 wt.%. In other words, the composition preferably contains 0.03 g to 4 g of phosphatidylcholine per 100 g of the composition. Deoiled lecithin fractions are preferably used as lecithin. This means that the lecithin is preferably substantially free of non-polar lipids such as fatty acids and triglycerides. The content of non-polar lipids such as fatty acids and triglycerides is preferably less than 3 wt.%. The lecithin contains a proportion of polar lipids (acetone-insoluble substance) of 90 wt.% to 100 wt.%. The lecithin may come from a source selected from soy, sunflower, rapeseed, fish, milk, eggs and mixtures thereof, with non-animal sources such as soy, sunflower and rapeseed being particularly preferred.In addition to the main component phosphatidylcholine, lecithin can contain phosphatidylethanolamine, phosphatidylinositol, phosphatidylserine, sterols, fats, and oils, depending on its origin. For example, a lecithin from soy can contain 40-50% by weight phosphatidylcholine, approximately 10% by weight phosphatidylethanolamine, approximately 5% by weight phosphatidylinositol, approximately 1-2% by weight phosphatidylserine, and also sterols, fats, and oils. Lecithin obtained from egg yolks, on the other hand, consists essentially of phosphatidylcholine. Embodiments within this document can be combined with one another as desired, unless the subject matter and description of the embodiments clearly indicate otherwise.

[0015] The verbs "to contain" and "to encompass" and their conjugations also include the verb "to consist of" and its conjugations.

[0016] Preferred embodiments of the invention are also specified in the subclaims.

[0017] Preferably the composition is a toothpaste.

[0018] In this dosage form, the composition can ideally unfold its cleansing effect.

[0019] The composition preferably contains a gelling agent. In one embodiment, xanthan gum is preferred as the gelling agent. In this embodiment, the composition contains 0.5% to 2% xanthan gum, based on the total weight of the composition.

[0020] The gelling agent promotes the formation of a toothpaste. Furthermore, the gelling agent increases the thermodynamic stability of the composition.

[0021] In a preferred embodiment, the composition has a viscosity at 20°C of between 3000 mPa s and 100,000 mPa s. The viscosity referred to herein is the dynamic viscosity, measured according to the method of the European Pharmacopoeia 7.0, 2011, using a cone-and-plate type rotational viscometer.

[0022] This viscosity can be adjusted by the composition of the composition according to the invention, with polyol, optional lipid, and optional gelling agent, in particular, being able to determine the viscosity. Gelling agent and a high amount of lipid lead to a higher viscosity. A higher viscosity extends the residence time of the composition at the site of action. In a preferred embodiment, the composition contains a compound selected from ubiquinone-10 and ubiquinol, in particular ubiquinone-10. Ubiquinone-10 can also be formed in the composition if ubiquinol is added to the composition. The composition particularly preferably contains 0.1% to 1% by weight of ubiquinone-10, based on the total weight of the composition.

[0023] The inventors have found that ubiquinone-10 and ubiquinol can contribute to healthy gums and inhibit gum inflammation. The combination of saffron extract and ubiquinone-10 is particularly effective. A disadvantage is that these compounds lead to a yellowing of the toothpaste, which is perceived as unappealing, which can lead to insufficient compliance and poor dental care.

[0024] In a preferred embodiment, the composition contains chlorophyll.

[0025] The inventors have discovered that the natural product and renewable raw material chlorophyll results in a toothpaste with an appealing color. This means that dyes or pigments, which often have a poor reputation and / or adverse properties, can be dispensed with. This improves compliance and oral health. Another advantage is that chlorophyll is able to mask the yellowing of the toothpaste caused by ubiquinone-10 and ubiquinol. Accordingly, the present invention also provides the use of chlorophyll to color a toothpaste.

[0026] In a preferred embodiment, the composition contains copper.

[0027] The inventors have found that chlorophyll is unstable in a toothpaste. The inventors have further found that copper can stabilize chlorophyll in a toothpaste. Accordingly, in a preferred embodiment, the composition contains a copper-chlorophyll complex, preferably a copper(II)-chlorophyll complex, particularly preferably chlorophyllin. Particularly preferably, the composition contains 0.05 wt.% to 0.6 wt.% of the copper-chlorophyll complex, based on the total weight of the composition. In a preferred embodiment, the composition contains silica, preferably spherical silica. The silica can be precipitated silica. The spherical silica preferably has a particle size of 1 μm to 50 μm, in particular of about 11 μm. For example, silica with CAS No. 112926-00-8 is suitable.

[0028] The inventors have determined that this natural product is a suitable abrasive for cleaning teeth and has good cleaning performance. Silica, especially spherical silica, can effectively remove plaque but has low abrasive properties to protect tooth enamel and dentin.

[0029] In a preferred embodiment, the composition contains a compound selected from cellulose and cellulose derivatives, preferably cellulose, particularly preferably cellulose abrasive particles.

[0030] The inventors have determined that this natural product and renewable raw material is a suitable abrasive for tooth cleaning and has a cleaning performance comparable to that of polyethylene or silica. In particular, cellulose is effective at removing plaque while exhibiting low abrasion to protect tooth enamel and dentin. Cellulose is biodegradable.

[0031] The composition preferably contains, based on the total weight of the composition, 5 wt.% to 25 wt.% or up to 30 wt.% of a compound selected from cellulose, silica, and mixtures thereof. In a preferred embodiment, the composition contains 5 wt.% to 25 wt.% or up to 30 wt.% of a mixture of cellulose and silica in a ratio (w / w) of 1:2 to 2:1, preferably about 1:1.

[0032] In a preferred embodiment, the composition contains a carrier selected from liposomes and nanosomes. With the help of liposomes and nanosomes, the saffron extract and ubiquinone-10 or ubiquinol can be transported particularly effectively to the site of action.

[0033] Liposomes can be formed, in particular, if the composition contains more lecithin / phosphatidylcholine than is needed to emulsion existing lipids. The emulsifier molecules (lecithin) not required to stabilize the lipids (e.g., in the form of fat droplets) can then form liposomal structures in the polar phase. These liposomal structures can serve as a special carrier system for water-soluble, hydrophilic substances or impurities. If the composition according to the invention contains at least one lipid, two carrier systems are present: fat droplets for lipophilic active ingredients and impurities, and liposomes for hydrophilic active ingredients and impurities. The formation of liposomes can be assisted by using high-pressure homogenizers during production of the composition.

[0034] Nanosomes can be formed by the interaction of water, polyol, lecithin and lipophilic compounds and can transport lipophilic active ingredients in particular.

[0035] In a preferred embodiment, the composition contains 0.1 wt% to 5 wt% saffron extract based on the total weight of the composition.

[0036] In a preferred embodiment, the composition contains, based on the total weight of the composition, 15% to 40% by weight of water, 30% to 65% by weight of polyol, 0.1% to 4% by weight of lecithin, 0.2% to 5% by weight of lipid and 0.1% to 5% by weight of saffron extract.

[0037] In this composition, the composition according to the invention is a stable and particularly effective drug carrier system for improving the mouthfeel, the condition of the teeth, the condition of the gums and for removing plaque.

[0038] The polyol is preferably selected from sorbitol, glycerin, xylitol, pentylene glycol, erythritol, fructose, and mixtures thereof. More preferably, the polyol comprises sorbitol. More preferably, the composition according to the invention contains 30% to 60% by weight of sorbitol.

[0039] Sorbitol is particularly suitable for stabilizing the composition and improving mouthfeel, and is non-cariogenic. In a preferred embodiment, the composition contains 20% to 40% water by weight, based on the total weight of the composition.

[0040] In a preferred embodiment, the composition contains 0.1 wt.% to 5 wt.% triacylglycerols, preferably medium-chain triglyceride, based on the total weight of the composition. Triacylglycerols can serve as carriers for lipophilic substances and impurities.

[0041] In a preferred embodiment, the composition contains pentylene glycol.

[0042] In a preferred embodiment, the composition contains a compound selected from an amino acid and an amide of an amino acid and a fatty acid. Cocoyl glutamate, the amide of gutamate and lauric acid, is preferred.

[0043] Preferably, the composition does not contain polyethylene.

[0044] Polyethylene is commonly used as an abrasive in toothpastes. However, polyethylene is not a natural product and is not a sustainable raw material.

[0045] In one embodiment, the composition does not contain silicate.

[0046] Silicate is used in toothpastes as an abrasive in the state of the art.

[0047] Preferably, the composition does not contain any synthetic surfactant. The term "no" is to be understood as meaning that the concentration of the compound is so low that no significant effect is to be expected. In other words, the concentration is outside the range in which the compound is normally used. Synthetic surfactants within the meaning of the invention are ethoxylated surfactants, macrogol and derivatives thereof (e.g. macrogolglycerol fatty acid esters such as macrogolglycerol ricinoleate,

[0048] Macrogol fatty acid esters such as macrogol oleate, macrogol fatty alcohol ethers such as polyoxyethylene cetyl ether), propylene glycol and derivatives thereof, polyoxypropylene-polyoxyethylene block polymers, benzalkonium, benzethonium, cetylalkonium, cetylpyridinium, cetyltrimethylammonium, dequalinium, sodium dodecyl sulfate, sodium cetyl sulfate, sodium stearyl sulfate, ethylene glycol monostearate, partial fatty acid esters of sorbitan (e.g. sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, sorbitan tristearate, sorbitan monooleate, sorbitan sesquioleate, sorbitan trioleate, polysorbates (polyoxyethylene sorbitan fatty acid esters), fatty acid esters of sucrose, fatty acid esters of polyglycerol and da-tocopheryl 1000 succinate.

[0049] Preferably, the composition contains no artificial preservative. The term "no" is to be understood as meaning that the concentration of the compound is so low that no significant effect is to be expected. In other words, the concentration is outside the range at which the compound is normally used. Artificial preservatives within the meaning of the invention include 4-hydroxybenzoic acid esters (e.g., methyl 4-hydroxybenzoate and propyl 4-hydroxybenzoate), chlorocresol, chlorobutanol, sorbic acid (E 200), potassium sorbate (E 202), calcium sorbate (E 203), sodium edetate, glycerol triacetate, benzalkonium, benzethonium, cetylalkonium, cetylpyridinium, cetyltrimethylammonium, cetrimonium, chlorhexidine, dequalinium, and organic mercury compounds.

[0050] Preferably, the composition contains no artificial sweetener. The term "no" is to be understood as meaning that the concentration of the compound is so low that no significant effect is to be expected. In other words, the concentration is outside the range at which the compound is normally used. Artificial sweeteners within the meaning of the invention are considered to be acesulfame (E 950), advantame (E 969), aspartame (E 951), aspartame-acesulfame salt (E 962), cyclamate (E 952), neohesperidin (E 959), neotame (E 961), saccharin (E 954), and sucralose (E 955).

[0051] Preferably, the composition does not contain monohydric alcohol.

[0052] In a particularly preferred embodiment, the composition contains, based on the total weight of the composition

[0053] - 5 wt.% to 25 wt.% or to 30 wt.% of a compound selected from cellulose, silica and mixtures thereof,

[0054] - 30% to 50% by weight sorbitol, - 20% to 35% by weight water,

[0055] - 1% by weight to 10% by weight of xylitol,

[0056] - 0.5% to 2% by weight xanthan,

[0057] - 1 wt% to 10 wt% pentylene glycol,

[0058] - 0.05 wt% to 0.6 wt% copper chlorophyll complex,

[0059] - 0.1% to 4% by weight lecithin,

[0060] - 0.1 wt% to 1 wt% ubiquinone-10,

[0061] - 0.1% to 5% by weight medium chain triglyceride,

[0062] - 0.1% to 5% by weight saffron extract and

[0063] - 1% to 5% by weight of an amide of an amino acid and a fatty acid, preferably cocoyl glutamate.

[0064] The present invention further provides a tube containing the composition or toothpaste according to the invention.

[0065] A tube is the preferred form of toothpaste.

[0066] The present invention further provides the use of a composition according to the invention as a toothpaste.

[0067] The present invention further provides the use of a composition according to the invention for achieving at least one effect selected from i) improvement of the mouthfeel, ii) improvement of the condition of the teeth, iii) improvement of the condition of the gums and iv) removal of plaque.

[0068] The inventors have found that the present composition is particularly well suited for this purpose.

[0069] The present invention further provides the composition according to the invention as a medicament, in particular for the prevention and / or treatment of a clinical picture selected from caries and periodontitis.

[0070] The inventors have found that the present composition is particularly well suited for this purpose.

[0071] The invention is further based on the idea of ​​providing a process for producing a composition according to the invention. The process for producing a composition according to the invention preferably comprises the following steps:

[0072] - stirring a mixture of water, polyol, optionally cellulose and / or silica, optionally xylitol, optionally xanthan and optionally pentylene glycol to homogeneity to obtain phase A;

[0073] - Optionally stirring a mixture of optionally a copper(II) chlorophyll complex and optionally sodium cocoylglutamate to homogeneity to obtain phase B;

[0074] - Stirring a mixture of saffron extract, lecithin, optionally ubiquinone-10 and optionally medium-chain triglyceride and high pressure homogenization to obtain phase C;

[0075] - Initially introduce phase A and optionally stir in phase B to obtain phase D;

[0076] - Add Phase D to Phase C and stir.

[0077] The processing temperature is preferably adjusted to the lecithin. For hydrogenated lecithins, processing temperatures between 40 °C and 80 °C are preferred; for unsaturated lecithins, processing can be carried out at room temperature. Processing above the melting point of lipophilic ingredients is preferred.

[0078] Homogenization is preferably carried out using a high-pressure homogenizer, ultrasound, and / or a rotor-stator mixer, in particular a high-pressure homogenizer. A high-pressure homogenizer reliably ensures that the composition contains liposomes.

[0079] Preferably, the process, in particular the stirring and homogenization under high pressure, is carried out under inert gas.

[0080] For further embodiments, advantages, and explanations, reference is made to the statements regarding the composition according to the invention. Another invention relates to a dental care composition containing at least one copper-chlorophyll complex and a compound selected from ubiquinone-10 and ubiquinol.

[0081] For embodiments, advantages and explanations, please refer to the above statements.

[0082] The invention is illustrated below using three examples.

[0083] In a first example, 15.0 g of cellulose, 43.0 g of sorbitol, 27.9 g of water, 3.0 g of xylitol, 1.0 g of xanthan and 5.0 g of pentylene glycol are mixed and stirred until homogeneous (= phase A).

[0084] 0.2 g chlorophyllin and 2.4 g sodium cocoylglutamate are mixed and stirred until homogeneous (= phase B).

[0085] 1.0 g saffron extract, 0.4 g lecithin, 0.5 g ubiquinone-10 and 0.6 g medium-chain triglycerides are mixed and processed under high pressure homogenization until homogeneous (= phase C).

[0086] Then Phase A is added and Phase B is stirred in. The mixture is added to Phase C and stirred in.

[0087] The obtained product contains 15.0 g cellulose, 43.0 g sorbitol, 27.9 g water, 3.0 g xylitol, 1.0 g xanthan gum, 5.0 g pentylene glycol, 0.2 g chlorophyllin, 2.4 g sodium cocoyl glutamate, 1.0 g saffron extract, 0.4 g lecithin, 0.5 g ubiquinone-10 and 0.6 g medium chain triglycerides.

[0088] The product received was tested in a study.

[0089] Implementation:

[0090] The study included 20 adult subjects with healthy oral mucosa who used the product as toothpaste twice daily (morning and evening) for three minutes each time over a period of four weeks. On day 0 and day 28, the gingival index and plaque index were determined for each subject. In addition, each subject completed a questionnaire on day 28.

[0091] Oral hygiene can be assessed by determining various indices, such as the presence of plaque (microbial plaque) and signs of inflammation of the gums (gingiva).

[0092] The plaque index provides a snapshot of the most recent cleaning procedures. Plaque can be visualized and assessed using staining methods (Mira-Z-Ton®, Hager & Werken GmbH & Co. KG; plaque staining tablets). The plaque index is calculated from the number of plaque-positive surfaces in relation to the total number of surfaces. The plaque index was recorded by a qualified professional.

[0093] The degree of gingival inflammation provides an insight into long-term oral hygiene, as inflammation develops only over a specific period of time. The degree of inflammation was classified according to the bleeding at the gingival margin (gingival index). A periodontal probe was inserted into the gingival pocket to a maximum depth of 0.5 mm. After provocation, the presence of bleeding was assessed, and its intensity was graded.

[0094] The gingival index is calculated as the total number of measured degrees divided by the total number of all measured interdental spaces. The gingival index was determined by a qualified professional.

[0095] The values ​​of the individual measurements were averaged, and the differences between the before and after values, as well as the relative change in the mean values, were calculated. The data sets were tested for normal distribution (chi-square test, Kolmogorov-Smirnov test). The data were compared using a parametric test (Student's t-test). P < 0.05 was accepted as significant, and P < 0.01 as highly statistically significant.

[0096] Result: The gingival index determined on day 28 was on average 91.5% (P = 1.7 x ICT 6 ) lower than the gingival index on day 0. The condition of the gums therefore improved significantly during the study period.

[0097] The plaque index determined on day 28 was on average 42.3% (P = 0.0015) lower than the plaque index on day 0. Thus, the condition of the teeth improved significantly during the study period and plaque was effectively removed.

[0098] The product was very well tolerated and did not cause any dermatologically relevant mucosal changes in the oral cavity in any of the test subjects.

[0099] The questionnaire completed by each subject on day 28 shows that the majority of subjects attested to the product's improvement in their oral health, particularly in their teeth and gums. The majority of subjects also attested to reduced sensitivity in their teeth and gums, a long-lasting feeling of freshness, good cleaning effect, good taste, and an improvement in the condition of their teeth and gums.

[0100] In a second example, 15.0 g of spherical silica with a particle size of approximately 11 pm was used instead of 15.0 g of cellulose. In a study, the product showed similar results to the product containing cellulose.

[0101] In a third example, the procedure was as in the first example, the product obtained containing 10.0 g of cellulose, 10.0 g of silica, 40.0 g of sorbitol, 25.9 g of water, 3.0 g of xylitol, 1.0 g of xanthan gum, 5.0 g of pentylene glycol, 0.2 g of chlorophyllin, 2.4 g of sodium cocoyl glutamate, 1.0 g of saffron extract, 0.4 g of lecithin, 0.5 g of ubiquinone-10 and 0.6 g of medium-chain triglycerides.

[0102] The product obtained was tested in a study as in the first example.

[0103] The gingival index determined on day 28 was on average 89.2% lower than the gingival index on day 0. Thus, the condition of the gums improved significantly during the study period. The plaque index determined on day 28 was on average 57.9% lower than the plaque index on day 0. Thus, the condition of the teeth improved significantly during the study period, and plaque was effectively removed.

[0104] The product was very well tolerated and did not cause any dermatologically relevant mucosal changes in the oral cavity in any of the test subjects.

[0105] The product reduced tooth staining by up to 6.7%.

[0106] The questionnaire completed by each subject on day 28 shows that the majority of subjects attested to an improvement in the feeling in the mouth, especially in the teeth and gums. The majority of subjects also attested to a reduced sensitivity of the teeth and gums.

[0107] Gums, a long-lasting feeling of freshness, a good cleaning effect, a good taste and an improvement in the condition of teeth and gums.

Claims

Claims 1. Composition for dental care, wherein the composition comprises at least - a saffron extract, - Water, - a polyol and - Contains lecithin.

2. Composition according to at least claim 1, characterized in that the composition is a toothpaste.

3. Composition according to at least claim 1 or 2, characterized in that the composition contains a gelling agent.

4. Composition according to at least one of the preceding claims, characterized in that the composition contains ubiquinone-10.

5. Composition according to at least one of the preceding claims, characterized in that the composition contains chlorophyll.

6. Composition according to at least one of the preceding claims, characterized in that the composition contains copper.

7. Composition according to at least one of the preceding claims, characterized in that the composition contains a compound selected from cellulose, cellulose derivatives, silica and mixtures thereof.

8. Composition according to at least one of the preceding claims, characterized in that the composition contains a carrier form selected from liposomes and nanosomes.

9. Composition according to at least one of the preceding claims, characterized in that the composition, based on the total weight of the composition - 15% to 40% by weight water, - 30 wt% to 65 wt% polyol, - 0.1% to 4% by weight lecithin, - 0.2 wt% to 5 wt% triglyceride and - Contains 0.1% to 5% w / w saffron extract.

10. Composition according to at least one of the preceding claims, characterized in that the polyol is selected from sorbitol, glycerin, xylitol, pentylene glycol and mixtures thereof and preferably comprises sorbitol.

11. A tube containing a composition according to at least one of claims 1 to 10.

12. Use of a composition according to at least one of claims 1 to 10 as a toothpaste.

13. Use of a composition according to at least one of claims 1 to 10 for achieving at least one effect selected from i) improvement of the mouthfeel, ii) improvement of the condition of the teeth, iii) improvement of the condition of the gums and iv) removal of plaque.

14. Use of chlorophyll to color a toothpaste.

15. Composition according to at least one of claims 1 to 10 for the prevention and / or treatment of a clinical picture selected from caries and periodontitis.