Agent for application to skin areas of a human for increasing the power of muscles of the human that are under the skin areas in the event of anaerobic stress

Abstract

The invention relates to an agent for application to skin areas of a human for increasing the power of muscles of the human under the skin areas in the event of anaerobic stress, in particular for reducing a lactate concentration in muscles under the skin areas. The agent expediently has a beta-alanine content of between 5.00 vol.% and 20.00 vol.% and a water content of between 20.00 vol.% and 95.00 vol.%. Overall, the claimed content of beta-alanine leads to a low-side-effect increase in power of those muscles that lie below skin areas treated with an agent according to the invention. In one embodiment of the invention, the agent additionally comprises water-soluble magnesium salt, wherein a content of the water-soluble magnesium salt is between 3.00 vol.% and 6.00 vol.%, and wherein the water-soluble magnesium salt is selected from the group consisting of magnesium chloride, magnesium sulfate, magnesium acetate, magnesium citrate, magnesium glycinate and magnesium gluconate.

Description

[0001] Description:

[0002] "A substance for application to the skin of a person to increase the performance of muscles located under the skin of a person during anaerobic exercise"

[0003] The invention relates to a means for application to skin areas of a person to increase the performance of muscles located under the skin areas of the person during anaerobic exercise, in particular to reduce a lactate concentration in muscles located under the skin areas.

[0004] Furthermore, the invention relates to the transdermal use of an agent according to the invention for increasing the performance of muscles located beneath the skin by applying the agent to the skin. This achieves both a reduction in the amount of lactate in muscle cells located beneath the skin and a reduction in the lactate concentration in the blood compared to activity without applying an agent according to the invention to skin areas above the muscles, which overall leads to an increase in performance.

[0005] A composition according to the invention is intended exclusively for transdermal application.

[0006] Anaerobic exercise is a high-intensity activity in which the body obtains the necessary energy with little or no oxygen consumption. In this state, the body's oxygen demand exceeds the available oxygen, leading to an oxygen debt. The body can no longer meet the energy requirements through aerobic metabolism (with oxygen) and must instead work anaerobically.

[0007] The transition from aerobic to anaerobic energy production is determined by the so-called anaerobic threshold, the value of which can be measured by the lactate level in the blood. In performance diagnostics, the lactate concentration in the blood is measured during increasing exercise intensity. The point at which the lactate concentration rises sharply is the anaerobic threshold.

[0008] Products for application to skin are known to be used as lotions, creams, or gels, which are applied to the skin areas to be treated, for example, during a massage. These usually contain nourishing or cooling ingredients that support the massage effect.

[0009] Beta-alanine, also spelled β-alanine, is a non-essential amino acid that combines with the amino acid histidine to form the dipeptide carnosine. Carnosine is stored in muscles and acts as an intracellular buffer, reducing the accumulation of lactic acid during anaerobic exercise; that is, it can reduce lactate concentration during anaerobic exercise.

[0010] It is known that a daily oral dose of four to six grams of beta-alanine over a period of two to four weeks increases the training performance of an endurance athlete (see E. Trexler; “International Society of Sports Nutrition position paper: Beta-

[0011] Alanine"; Journal of the International Society of Sports Nutrition, Vol. 12, 2015, p. 1 -14; DOI: 10.1 186 / sl 2970-015-0090-y).

[0012] Furthermore, it is known that oral administration of beta-alanine at the aforementioned dosage leads to paresthesia as a very common side effect, manifesting in particular as a constant tingling sensation throughout the entire body and nervous states, i.e., an unpleasant agitation. This side effect can cause, for example, competitive athletes taking beta-alanine to overlook underlying medical conditions, masking them with the side effect of the medication.

[0013] Dietary supplements containing beta-alanine are known from EP 1 883 406 B1 and US 2016 / 0303177 A1. Beta-alanine is known from WO 2012 / 02461 1 A1 for the treatment of sarcopenia in the elderly. US 2015 / 0283163 A1 describes a composition for the treatment of muscle cramps, muscle pain, or spasms, which may contain beta-alanine. Beta-alanine for enhancing anaerobic performance in athletes is not known from either WO 2012 / 024611 A1 or US 2015 / 0283163 A1.

[0014] WO 2007 / 073398 discloses a composition for administering beta-alanine, either orally, as a patch or as a topical dermatological compound, to reduce acidosis during high-performance exercise.

[0015] US 2001 / 0005579 and WO 2004 / 091497 describe compositions for increasing the anaerobic performance of muscles. The composition contains beta-alanine and can be administered orally or by injection. Use by topical application is not disclosed.

[0016] US 11,491,225 describes a formulation for the transdermal administration of therapeutics. Among other things, beta-alanine is described as a therapeutic agent. In Example 10 (column 40), a cream containing beta-alanine is used to enhance muscle performance. The described cream contains 1% by weight of beta-alanine.

[0017] WO 201 1 / 019348 describes a composition containing beta-alanine, for oral use only.

[0018] The present invention is based on the objective of creating a means of the type mentioned above, which is applied locally to skin areas and by which an increase in the performance of muscles lying under the treated skin areas is achieved.

[0019] The invention also aims to create a means by which transdermal use makes it possible to increase performance during anaerobic exercise, which until now has only been possible through oral intake of beta-alanine.

[0020] Furthermore, the invention aims to create a means of the type mentioned above, the use of which does not cause whole-body paresthesia as a side effect of beta-alanine application. In particular, no persistent tingling or burning sensation occurs in large, untreated areas of skin. Side effects such as persistent, unpleasant agitation can also be effectively prevented with a local, transdermal application of a means according to the invention.

[0021] According to the invention, the problem is solved by the agent having a proportion of beta-alanine between 5.00 vol% and 20.00 vol% and a proportion of water between 20.00 vol% and 95.00 vol%.

[0022] The proportions of the individual components in VoL-% are based on the total volume of all components contained in the product before they are combined to manufacture the product.

[0023] The total volume is the volume occupied by the components before they are combined. Combining the components can, for example, create a mixture.

[0024] A composition according to the invention contains at least beta-alanine and water.

[0025] It is understood that the sum of all components of the mixture is 100.00 vol%. The conversion between vol% and wt% is carried out taking into account the respective densities of the components at room temperature, and, in the case of powdered solids, their bulk densities, if applicable.

[0026] A product containing 5.00 vol% beta-alanine and 95.00 vol% water has a beta-alanine content of 7.04 wt% and a water content of 92.96 wt%.

[0027] A product containing 20.00 vol% beta-alanine and 80.00 vol% water has a beta-alanine content of 26.47 wt% and a water content of 73.53 wt%.

[0028] The inventors have determined through numerous elaborate experiments that a beta-alanine content of less than 5.00 VoL-% has no effect at all, as not enough beta-alanine reaches the muscles for which the beta-alanine is intended.

[0029] Furthermore, the inventors have determined that a proportion of more than 20.00 VoL-% no longer results in an increase in performance, but leads to unpleasant local side effects on treated skin areas, in particular a tingling or burning sensation, as is known from touching stinging nettles.

[0030] The inventors further discovered that, surprisingly, no increase in muscle performance was achieved with a water content of less than 20.00 vol% or above 95.00 vol%. Below 20 vol%, there is insufficient water to act as a solvent for beta-alanine; above 95 vol%, the water content is too high to transport enough beta-alanine through the skin. The inventors determined that, for a composition according to the invention, an increase in performance occurred across all muscles relevant to the human musculoskeletal system.

[0031] Overall, the claimed proportion of beta-alanine between 5.00 VoL-% and 20.00 VoL-% leads to a low-side-effect increase in performance of those muscles that lie below skin areas treated with a product according to the invention.

[0032] For example, in the case of football players or cyclists, the inventors treated the legs of test subjects, circumferentially from the hip to the ankle, with a composition according to the invention containing water and beta-alanine for 10 minutes before physical exertion. The composition according to the invention was applied as a spray.

[0033] In one embodiment of the invention, the agent has a water content of between 20.00 vol% and 80.00 vol%.

[0034] In a further embodiment of the invention, the agent has a water content of between more than 80.00 vol% and 95.00 vol%.

[0035] In one embodiment of the invention, the agent additionally comprises a water-soluble magnesium salt, wherein the proportion of the water-soluble magnesium salt is between 3.00 vol% and 6.00 vol%, and wherein the water-soluble magnesium salt is selected from the group consisting of magnesium chloride, magnesium sulfate, magnesium acetate, magnesium citrate, magnesium glycinate and magnesium gluconate.

[0036] A water-soluble magnesium salt is a salt that is completely soluble in water at room temperature, that is to say, in particular, completely soluble in the amount of water used to produce a composition according to the invention.

[0037] Magnesium chloride can be used as a pure substance or as magnesium chloride hexahydrate.

[0038] The water-soluble magnesium salt provides magnesium ions to a stressed muscle, thereby preventing or at least reducing muscle cramps and muscle pain.

[0039] The inventors recognized that adding a water-soluble magnesium salt could further enhance performance. The muscles beneath the treated skin areas receive an additional supply of magnesium ions, so that cramps and pain are only felt under higher exertion levels. Using lactate measurements, a technique known from performance diagnostics, the inventors observed that by adding a water-soluble magnesium salt, such as magnesium chloride or magnesium citrate, test subjects in an ergometer performance test, on average across several subjects, exhibited lactate levels significantly lower than those achieved with a spray containing only beta-alanine, even at workloads as low as 150 watts. This result was surprising.This demonstrated that magnesium ions can not only be absorbed through beverages, but can also be effectively and specifically supplied to muscles through a transdermal application of a substance according to the invention.

[0040] The inventors also found that adding less than 3.00 vol% of the water-soluble magnesium salt has no effect, while adding more than 6.00 vol% does not result in any further increase in performance.

[0041] The inventors have further determined that the type of water-soluble magnesium salt has little influence on performance enhancement, with magnesium chloride being preferred due to its particularly good skin compatibility.

[0042] In one embodiment of the invention, the agent additionally comprises urea, wherein the proportion of urea is between 5.00 vol% and 12.00 vol%.

[0043] Urea, also known as urea in cosmetic applications, acts as a humectant, drawing water into the skin and binding it, thus keeping the skin hydrated and soft. Urea can also serve as a penetration enhancer, weakening but maintaining the integrity of the skin barrier and improving the transdermal absorption of active ingredients. This use of urea is already known from moisturizing face, hand, or foot creams, where it restores suppleness to treated, dry skin areas.

[0044] The inventors recognized that using urea in the claimed quantity can lead to increased absorption of beta-alanine. Surprisingly, not only does the skin barrier become more permeable to beta-alanine, but also the tissue between the skin and muscles.

[0045] For concentrations below 5.00 vol%, the beneficial effect could not be observed at all; for concentrations above 12.00 vol%, no further increase in performance could be determined. In a further embodiment of the invention, the agent additionally comprises arnica tincture, with the proportion of arnica tincture being between 3.00 vol% and 6.00 vol%.

[0046] Arnica tincture (Arnica Montana Flower Extract) within the meaning of this invention is a tincture made from arnica flowers [ratio of drug to extraction solvent 1 :10], wherein ethanol 70% (V / V) is used as the extraction solvent.

[0047] Arnica is known for its anti-inflammatory, antibacterial and analgesic effects when applied topically.

[0048] The inventors discovered that arnica, in combination with beta-alanine, further enhances performance, meaning that, on average across multiple test subjects, it can lead to a higher maximum power output during an ergometer performance test. For example, a majority of test subjects were able to reach the next higher power level of 300 watts instead of the previous maximum of 250 watts.

[0049] The inventors attribute the positive effect of arnica to its ability to penetrate deep into the muscle, where it can exert its pain-relieving effect. As a result, a test subject perceives less pain and can perform at a higher level. This finding is surprising, as arnica can apparently penetrate deep into the muscle and act locally. This was not foreseeable given its previous primary use as an active ingredient in creams for treating only superficial skin injuries such as bruises and contusions.

[0050] A concentration of 3.00 vol.% is a threshold that must be reached for arnica to have any effect in a composition according to the invention. Above 6.00 vol.%, a large number of test subjects no longer experience any performance improvements, but rather significant skin irritation.

[0051] In one embodiment of the invention, the agent additionally comprises a water-soluble magnesium salt selected from the group consisting of magnesium chloride, magnesium sulfate, magnesium acetate, magnesium citrate, magnesium glycinate and magnesium gluconate, as well as urea and arnica tincture, wherein the proportion of water-soluble magnesium salt is between 3.00 vol% and 6.00 vol%, the proportion of urea is between 5.00 vol% and 12.00 vol%, and the proportion of arnica tincture is between 3.00 vol% and 6.00 vol%.

[0052] The inventors have surprisingly discovered that by using these three additional components in the aforementioned composition, a particularly good permeability of the skin to beta-alanine is achieved, while at the same time no or only very minor side effects such as skin irritation of the treated skin areas occurred in test subjects.

[0053] It has been found that for a product containing these three additional components, in addition to beta-alanine, particularly low lactate concentrations were measured across all test subjects in a standardized ergometer performance test.

[0054] The inventors attribute this to the fact that the use of these three components in the aforementioned proportions leads to a particularly high absorption of beta-alanine into a muscle located beneath a treated area of ​​skin.

[0055] In a further embodiment of the invention, the agent additionally contains ubiquinone-10 (coenzyme Q10), wherein the proportion of ubiquinone-10 is between 2.50 vol% and 6.00 vol%.

[0056] The inventors have surprisingly discovered that adding ubiquinone-10, also known as coenzyme Q10, can improve performance. While it is known that ubiquinone-10 is involved in the respiratory chain in the mitochondria, the powerhouses of human cells, and in the production of ATP (adenosine triphosphate), the main energy carrier of human cells, it has not previously been described that ubiquinone-10, as a component of a transdermal product, can penetrate to muscle cells beneath the treated area of ​​skin and exert a local effect there.

[0057] The product conveniently also contains glycerin, with a glycerin content between 14.00 vol% and 25.00 vol%.

[0058] The inventors discovered that the high glycerin content makes the skin particularly permeable to beta-alanine, thus providing more beta-alanine to stressed muscles than without glycerin. Therefore, the inventors found that using glycerin could reduce the amount of beta-alanine and still improve performance. However, this performance increase was only observed at levels between 14.00% and 25.00% vol. The inventors attribute this to the fact that saturation occurs above 25.00% vol. , preventing further improvement, while at least 14.00% vol. is required to achieve any improvement in the skin's permeability to beta-alanine.In one embodiment of the invention, the agent additionally comprises a water-soluble magnesium salt selected from the group consisting of magnesium chloride, magnesium sulfate, magnesium acetate, magnesium citrate, magnesium glycinate and magnesium gluconate, as well as ubiquinone-10 (coenzyme Q10) and glycerol, wherein the proportion of water-soluble magnesium salt is between 3.00 vol% and 6.00 vol%, the proportion of ubiquinone-10 is between 2.50 vol% and 6.00 vol%, and the proportion of glycerol is between 14.00 vol% and 25.00 vol%.

[0059] This composition has proven to be particularly effective in increasing performance, especially when the users of a product according to the invention were high-performance athletes.

[0060] The inventors attribute the performance-enhancing effect in highly trained elite athletes to the fact that this combination can supply stressed muscles particularly well with beta-alanine and other performance-relevant substances despite transdermal application.

[0061] For proportions below the claimed proportions, the performance increase was less pronounced, while for proportions above the claimed proportions, no further performance increase was found. The inventors attribute this to the fact that a threshold value is required, whereas once saturation is reached, no further performance increase is possible.

[0062] The agent is preferably an oil-in-water emulsion, a water-in-oil emulsion, or an aqueous solution.

[0063] Advantageously, a composition according to the invention is suitable for many different applications. For example, an oil-in-water emulsion can be a cream, while a water-in-oil emulsion can be a lotion, each of which can be used, for example, for simultaneous skin care and regeneration after exertion. An aqueous solution can be a gel in the form of a massage gel, which can be applied before exertion.

[0064] An aqueous solution can also be a spray for quick use before an unplanned stress, as it can be sprayed on by the user himself immediately before use and without external assistance.

[0065] Due to its transdermal application, the product in the aforementioned dosage forms is particularly suitable for endurance athletes, as effective use before, after, or even during a competition is possible. In one embodiment of the invention, the product comprises at least one further additional component, wherein this at least one further additional component is selected from the list consisting of ethylhexyl stearate, cetearyl alcohol, isopropyl palmitate, glyceryl monostearate, phenoxyethanol, citric acid, panthenol, sodium stearoyl glutamate, sea salt, sweet almond oil (Prunus Amygdalus Dulcis Oil), wheat germ oil (Triticum Vulgare Germ Oil), lavender oil (Lavandula Angustifolia Oil), linalool, almond oil, shea butter, and jojoba oil.

[0066] The inventors have recognized that at least one of the other components results in a particularly skin-nourishing product containing beta-alanine. This can significantly reduce or even completely prevent side effects such as skin irritation or redness, especially in sensitive individuals.

[0067] In particular, the addition of this further component can create a performance-enhancing agent suitable for continuous and regular use.

[0068] In one embodiment of the invention, the agent contains 7.00 wt.% to 27.00 wt.% beta-alanine.

[0069] An agent according to the invention is intended for transdermal use to enhance the performance of muscles located beneath the skin by applying the agent to the skin area and reduces lactate formation in muscles located beneath the skin area to which the agent has been applied. In particular, the agent is especially suitable for use in reducing lactate formation in muscles located beneath the skin area to which the agent has been applied during anaerobic exercise.

[0070] The inventors have even found that, on average across several test subjects, the lactate concentration in muscles located below the skin areas to which an inventive agent was applied can be reduced by at least 15% compared to the lactate concentration in the same muscles located below the same skin areas and not treated with an inventive agent.

[0071] In the ergometer performance test, this 15% reduction refers to a decrease in the lactate concentration in the blood of a test subject at a power output of 150 watts, 200 watts and 250 watts.

[0072] The agent according to the invention is advantageously suitable for use by endurance athletes such as cyclists, soccer players, runners, or triathletes. An inventive method for increasing the performance of muscles located under the skin during anaerobic exercise is characterized in that an agent according to the invention is applied to the skin.

[0073] Advantageously, a simple procedure is created that can be carried out by laypersons even without prior medical knowledge.

[0074] The invention is explained in more detail below with reference to exemplary embodiments and the accompanying drawings relating to these embodiments. The drawings show:

[0075] Fig. 1 A diagram showing lactate concentration as a function of performance in a standardized performance test using a first agent according to the invention.

[0076] Fig. 2 A diagram showing lactate concentration as a function of performance in a standardized performance test using several other means according to the invention,

[0077] Fig. 3 A diagram showing lactate concentration as a function of performance in a standardized performance test using several other means according to the invention,

[0078] Fig. 4 A diagram showing lactate concentration as a function of performance in a standardized performance test using several other means according to the invention.

[0079] Example 1:

[0080] An agent according to the invention as shown in Example 1 is a spray with the following composition:

[0081] - 17.00% by volume beta-alanine (22.77% by weight)

[0082] - 83.00 vol% water (77.23 wt%) To prepare the spray according to Example 1, beta-alanine was added to water at room temperature, with the relative volumes of the two starting materials being 17 vol% and 83 vol%. The relative volume fractions are based on the total volume of water and beta-alanine before they were mixed to prepare the spray according to Example 1.

[0083] Expressed in weight percent, this corresponds to 22.77 wt% beta-alanine and 77.23 wt% water.

[0084] The technical effect for all the examples mentioned was demonstrated on 22 test subjects, with whom a baseline state was determined in a first performance test. In a second performance test, which took place two weeks later, some received a placebo, while others were administered a composition according to Example 1 for transdermal application.

[0085] A standardized performance diagnostic procedure was used as the performance test. In this procedure, a test subject pedaled on a bicycle ergometer at a constant wattage and a predetermined cadence between 70 and 90 revolutions per minute. The test began at 50 watts. Every five minutes, the power output was increased by one increment, i.e., by 50 watts. After each increase in power output, a lactate measurement was taken within 30 seconds using a blood sample taken from the fingertip. The lactate concentration in the blood was measured in millimoles per liter (mmol / l), providing information about the level of exertion during this standardized performance test.

[0086] To evaluate the performance test, lactate concentration is plotted as a function of the achieved power output, a so-called lactate curve. It is known that the lactate concentration in the blood rises sharply above 100 watts, which indicates that the so-called anaerobic threshold has been reached. On average, across all test subjects, during a performance test without the use of a substance according to the invention (“reference” in Figs. 1 to 4), they reached their subjectively perceived point of exhaustion at approximately 250 watts and ended the test.

[0087] To demonstrate the influence of beta-alanine on performance in the aforementioned performance test, lactate curves were determined and compared for those test subjects who received a product according to the invention, both with and without the use of such a product. The product according to Example 1 was a spray and was applied to the entire surface of the legs and rubbed in five minutes before the start of the performance test.

[0088] Mean values ​​were calculated from the data of all test subjects who were administered a substance with a composition according to Example 1, which are shown in the diagram according to Fig.

[0089] Figure 1 is shown as a function of the ergometer power output in watts. The curve labeled "Reference" shows the mean values ​​without the application of a compound according to the invention, while "Example 1" shows the mean values ​​when applying a compound according to the invention with the composition according to Example 1.

[0090] In all diagrams, the curve labelled “Example X” shows the mean values ​​when using an agent according to the invention with the composition according to Example X.

[0091] It is clearly evident that the application of a spray according to the invention as described in Example 1 leads to a lower lactate concentration in a standardized test upon reaching the anaerobic threshold. For example, at 150 watts, the lactate concentration is approximately 6.04 mmol / l, compared to 4.21 mmol / l after administration of beta-alanine. A reduction in lactate concentration from 6.04 mmol / l to 4.21 mmol / l corresponds to a decrease of 30.28%.

[0092] At 250 watts, the reduction in lactate concentration is still 18.5%, from 1.88 mmol / l at the reference to 9.69 mmol / l according to Example 1.

[0093] Although not shown in any of the figures 1 to 4, the inventors found that when using a spray according to the invention, a performance test had to be stopped on average only at 300 watts, whereas in the reference test a personal limit of the test subjects was already reached at 250 watts.

[0094] Although not shown in Figures 1 to 4, no performance improvement could be detected in the subjects who received a placebo. The corresponding reference curves and that of a placebo trial were identical within the margin of measurement uncertainty.

[0095] Comparable results were found for the means according to examples 2 to 13 below.

[0096] Example 2: - 14.50 vol% beta-alanine (19.23 wt%)

[0097] - 6.50 vol% urea (8.00 wt%)

[0098] - 79.00 vol-% water (72.77 wt.%)

[0099] Example 3:

[0100] - 19.00% by volume beta-alanine (24.69% by weight)

[0101] - 8.75 vol% urea (10.56 wt%)

[0102] - 4.75 vol-% arnica tincture (tincture made from arnica flowers [ratio of drug to extraction solvent])

[0103] 1:10], using 70% (v / v) ethanol as the extraction solvent.) (3.82 wt.% at a determined density of 0.89 g / cm³ 3 )

[0104] - 67.50 vol-% water (60.92 wt.%)

[0105] Example 4:

[0106] - 16.50% by volume beta-alanine (20.35% by weight)

[0107] - 9.00 vol% urea (10.31 wt%)

[0108] - 4.50 vol-% arnica tincture (tincture made from arnica flowers [ratio of drug to extraction solvent])

[0109] 1:10], using 70% (v / v) ethanol as the extraction solvent.) (3.44 wt% at a determined density of 0.89 g / cm³ 3 )

[0110] - 5.25 vol% magnesium chloride (10.45 wt%)

[0111] - 64.75% vol water (55.45% wt.)

[0112] Fig. 2 shows the lactate curves for a reference measurement as well as when using a means according to the invention as shown in Examples 2 to 4.

[0113] It is clearly evident that the addition of urea, arnica tincture and magnesium chloride resulted in a lower average lactate concentration across all test subjects.

[0114] At 250 watts, a further reduction in lactate concentration from 9.69 mmol / l to 8.88 mmol / l is observed between the agents according to Examples 1 and 4, which corresponds to a further reduction of approximately 9%. Compared to the reference, the reduction when using an agent according to the invention at 250 watts is even approximately 25%, from 11.93 mmol / l to 8.88 mmol / l.

[0115] It was also found that the products in examples 1 to 4 did not cause any skin irritation, meaning their use was free of side effects.

[0116] Example 5:

[0117] - 6.00% by volume beta-alanine (8.31% by weight)

[0118] - 7.00 vol% urea (9.00 wt%)

[0119] - 4.50 vol-% arnica tincture (tincture made from arnica flowers [ratio of drug to extraction solvent])

[0120] 1:10], using 70% (v / v) ethanol as the extraction solvent.) (3.86 wt%)

[0121] - 4.00 vol% magnesium chloride (8.94 wt%)

[0122] - 28.40 vol-% water (27.31 wt.%)

[0123] - 0.10 vol% polysorbate 60 as emulsifier (0.10 wt%)

[0124] - 30% vol. jojoba oil (24.94% wt.)

[0125] - 20% vol. almond oil (17.53% wt.)

[0126] An oil-in-water emulsion according to Example 5 had a comparable effect on the lactate concentration of a test subject in an ergometer performance test as a spray according to Example 4.

[0127] Example 6:

[0128] - 8.00% by volume beta-alanine (10.77% by weight)

[0129] - 7.00 vol% urea (8.76 wt%)

[0130] - 4.50 vol-% arnica tincture (tincture made from arnica flowers [ratio of drug to extraction solvent])

[0131] 1:10], using 70% (v / v) ethanol as the extraction solvent.) (3.75 wt%)

[0132] - 4.00 vol% magnesium chloride (8.69 wt.%)

[0133] - 28.40 vol-% water (26.56 wt.%)

[0134] - 0.10 vol% lecithin as emulsifier (0.10 wt%)

[0135] - 48 vol% Shea Butter (41.37 wt%) A water-in-oil emulsion according to Example 6 had a comparable effect on the lactate concentration of a subject in an ergometer performance test as a spray according to Example 4 and an oil-in-water emulsion according to Example 5.

[0136] The two products of the composition shown in examples 5 and 6 are particularly suitable for long-term use, as they contain a high proportion of skin-conditioning substances.

[0137] Example 7:

[0138] - 11.00% by volume beta-alanine (14.29% by weight)

[0139] - 4.50 vol% magnesium chloride (MgCl2) (9.44 wt%)

[0140] - 84.50 vol-% water (76.26 wt.%)

[0141] Example 8:

[0142] - 12.00% by volume beta-alanine (16.45% by weight)

[0143] - 4.00% by volume ubiquinone-10 (coenzyme Q10) (3.59% by weight)

[0144] - 84.00 vol-% water (79.96 wt.%)

[0145] Example 9:

[0146] - 8.00% by volume beta-alanine (10.59% by weight)

[0147] - 20.00 vol% glycerin (23.21 wt%)

[0148] - 72.00 vol-% water (66.20 wt.%)

[0149] Example 10:

[0150] - 10.00% by volume beta-alanine (13.00% by weight)

[0151] - 5.00 vol% magnesium chloride (MgCl2) (10.50 wt%)

[0152] - 5.00% by volume ubiquinone-10 (coenzyme Q10) (4.25% by weight)

[0153] - 80.00 vol-% water (72.25 wt.%)

[0154] Example 1 1 :

[0155] - 15.00% by volume beta-alanine (18.31% by weight)

[0156] - 5.00 vol% magnesium chloride (MgCl2) (9.85 wt%)

[0157] - 18.00 vol% glycerin (19.27 wt%)

[0158] - 62.00 vol-% water (52.57 wt.%) Example 12:

[0159] - 12.50% by volume beta-alanine (16.29% by weight)

[0160] - 4.50% by volume ubiquinone-10 (coenzyme Q10) (3.84% by weight)

[0161] - 20.00 vol% glycerin (22.85 wt%)

[0162] - 63.00 vol-% water (57.02 wt.%)

[0163] Example 13:

[0164] - 9.00% by volume beta-alanine (1 1.33% by weight)

[0165] - 5.00 vol% magnesium chloride (MgCl2) (10.17 wt%)

[0166] - 3.00% by volume ubiquinone-10 (coenzyme Q10) (2.47% by weight)

[0167] - 15.00 vol% glycerin (16.56 wt%)

[0168] - 68.00 vol-% water (59.47 wt.%)

[0169] All of Examples 7 to 13 were sprays, for the production of which the respective volume fractions of the individual components were combined to produce a composition according to the invention as described in the respective example. The relative volume fractions refer to the total volume of all components contained in the composition before their combination to produce the composition.

[0170] The experimental procedure for determining the lactate curves in Fig. 3 and Fig. 4 was analogous to the experimental procedure described for Fig. 1 and Fig. 2.

[0171] Figs. 3 and 4 show further lactate curves for the aforementioned reference measurement and when using a means according to the invention as described in Examples 7 to 13, wherein the results for Examples 7, 9, 11 and 13 are shown in Fig. 3 for clarity and the results for Examples 8, 10 and 12 are shown in Fig. 4 for clarity.

[0172] In both Fig. 3 and Fig. 4, the reference curve shown in Figs. 1 and 2 and the curve belonging to Example 1 have been added to clarify the results.

[0173] Figure 3 clearly shows, for example, that by adding 4.50 vol% magnesium chloride (MgCl2) as in Example 7, a reduction in lactate concentration at 150 watts from 6.04 mmol / l (reference) to 4.00 mmol / l is possible. At 200 watts, a reduction in lactate concentration from 10.77 mmol / l (reference) to 6.52 mmol / l was determined.

[0174] Even when comparing the lactate values ​​for example 1 with those for example 7, a reduction from 4.21 mmol / l (example 1 at 150 watts) to 4.00 mmol / l and from 9.67 mmol / l (example 1 at 250 watts) to 9.20 mmol / l (example 7 at 250 watts) is evident.

[0175] Reductions in lactate concentrations were also found for compositions according to Examples 9, 11 and 13 and are also shown in Fig. 3.

[0176] The greatest effect was observed in Example 13, where a significant reduction in lactate concentration occurred at 200 watts and 250 watts. At 200 watts, this concentration was 5.02 mmol / l, and at 250 watts, it was 8.62 mmol / l. This confirms that a substance like the one in Example 13 enables a particularly high increase in performance.

[0177] Figure 4 also clearly shows that by adding ubiquinone-10 (coenzyme Q10) as in Example 8, a reduction in lactate concentration is possible even at 100 watts compared to the use of Example 1. Thus, the additional addition of ubiquinone-10 has a positive technical effect that enables a further increase in performance.

[0178] A comparable effect was found for the lactate curves determined for examples 10 and 12. Example 10 shows that a further increase in performance is possible by adding magnesium chloride (MgCl2) and ubiquinone-10 (coenzyme Q10) to beta-alanine.

[0179] A further increase in performance is possible if a composition according to Example 12 is used, that is, if ubiquinone-10 and glycerol are added in addition to beta-alanine.

[0180] The test subjects praised the skin compatibility of the products according to examples 7 to 13 and even described the product according to examples 1 to 13 as a skin care product.

[0181] Similar results to those obtained for the agents in Examples 1 to 13 were found for the further Examples 14 to 32, the composition of which is shown in Table 1 below:

[0182] When using water-soluble magnesium salts other than magnesium chloride, comparable results were found to those obtained for the products in Examples 1 to 32, which contain magnesium chloride. The exemplary compositions of Examples 33 to 37 are shown in Table 2 below.

[0183] Overall, the inventors have been able to demonstrate that an increase in performance is possible through beta-alanine, and that a further increase in performance is possible by adding suitable additional components, one of which is an improvement in the permeability of the skin on which an inventive agent is applied to beta-alanine.

Claims

Patent claims:

1. A composition for application to the skin of a person to enhance the performance of muscles located under the skin during anaerobic exercise, in particular to reduce the lactate concentration in muscles located under the skin, characterized in that the composition has a proportion of beta-alanine between 5.00 vol% and 20.00 vol% and a proportion of water between 20.00 vol% and 95.00 vol%.

2. Composition according to claim 1, characterized in that the composition additionally comprises a water-soluble magnesium salt, wherein the proportion of the water-soluble magnesium salt is between 3.00 vol% and 6.00 vol%, and wherein the water-soluble magnesium salt is selected from the group consisting of magnesium chloride, magnesium sulfate, magnesium acetate, magnesium citrate, magnesium glycinate and magnesium gluconate.

3. Composition according to claim 1 or 2, characterized in that the composition additionally comprises urea, wherein the proportion of urea is between 5.00 vol% and 12.00 vol%.

4. Composition according to any one of claims 1 to 3, characterized in that the composition additionally comprises arnica tincture, wherein the proportion of arnica tincture is between 3.00 vol% and 6.00 vol%.

5. Composition according to claim 1, characterized in that the composition additionally comprises a water-soluble magnesium salt selected from the group consisting of magnesium chloride, magnesium sulfate, magnesium acetate, magnesium citrate, magnesium glycinate and magnesium gluconate, as well as urea and arnica tincture, wherein a proportion of water-soluble magnesium salt is between 3.00 vol% and 6.00 vol%, and a proportion of urea is between 5.00 vol% and 12.00 vol%, and a proportion of arnica tincture between 3.00 vol% and 6.00 vol%.

6. Composition according to any one of claims 1 to 5, characterized in that the composition additionally comprises ubiquinone-10 (coenzyme Q10), wherein the proportion of ubiquinone-10 is between 2.50 vol% and 6.00 vol%.

7. Composition according to any one of claims 1 to 6, characterized in that the composition additionally comprises glycerin, wherein the proportion of glycerin is between 14.00 vol% and 25.00 vol%.

8. Composition according to claim 1, characterized in that the composition additionally comprises a water-soluble magnesium salt selected from the group consisting of magnesium chloride, magnesium sulfate, magnesium acetate, magnesium citrate, magnesium glycinate and magnesium gluconate, as well as ubiquinone-10 (coenzyme Q10) and glycerol, wherein a proportion of water-soluble magnesium salt is between 3.00 vol% and 6.00 vol%, a proportion of ubiquinone-10 is between 2.50 vol% and 6.00 vol%, and a proportion of glycerol is between 14.00 vol% and 25.00 vol%.

9. Composition according to any one of claims 1 to 8, characterized in that the composition is an oil-in-water emulsion, a water-in-oil emulsion or an aqueous solution.

10. Composition according to any one of claims 1 to 9, characterized in that the composition comprises at least one further additional component, wherein this at least one further additional component is selected from the list consisting of ethylhexyl stearate, cetearyl alcohol, isopropyl palmitate, glyceryl monostearate, phenoxyethanol, citric acid, panthenol, sodium stearoyl glutamate, maris sal, sweet almond oil (Prunus Amygdalus Dulcis Oil), wheat germ oil (Triticum Vulgare Germ Oil), lavender oil (Lavandula Angustifolia Oil), linalool, almond oil, shea butter and jojoba oil are selected.

11. A composition according to any one of claims 1 to 10 for transdermal use to enhance the performance of muscles located beneath a skin area of ​​a person by applying the composition to the skin area.

12. A composition according to claim 11 for transdermal use to reduce the formation of lactate in muscles located below the area of ​​skin to which the composition has been applied, during anaerobic exercise.

13. A composition according to claim 1 or 12 for transdermal use to reduce the lactate concentration in muscles located below the area of ​​skin to which the composition has been applied, by at least 15% compared to the lactate concentration in the same muscles located below the same area of ​​skin and which have not been treated with a composition according to any one of claims 1 to 10.

14. Method for increasing the performance of muscles located under skin areas of a person during anaerobic exercise, characterized in that a means according to one of claims 1 to 13 is applied to the skin areas.

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