Use of a co 2-absorbing formulation, and ergogenic food supplement, in particular energy drink or sports drink
The integration of a CO2-absorbing formulation into energy or sports drinks addresses the need for improved performance and reduced fatigue by effectively absorbing CO2 from the body, enhancing acid-base balance and extending endurance.
Patent Information
- Application Number
- PCT/EP2024/083240
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-03-14
- Filing Date
- 2024-11-22
- Publication Date
- 2025-05-30
AI Technical Summary
Existing energy and sports drinks do not effectively address the need for a formulation that can absorb CO2 from the body, leading to improved performance and reduced fatigue during physical activities.
A CO2-absorbing formulation is integrated into an ergogenic food supplement, specifically designed for energy or sports drinks, using a CO2-absorber embedded in a carrier matrix or shell that prevents the release of the absorber, allowing it to effectively absorb CO2 in the gastrointestinal tract.
The formulation reduces CO2 content in the blood, leading to improved performance, delayed fatigue, and enhanced acid-base balance, thereby extending endurance and aiding in faster recovery from physical exertion.
Smart Images

Figure EP2024083240_30052025_PF_FP_ABST
Abstract
Description
[0001] Use of a CO2-absorbing formulation, as well as ergogenic food supplement, in particular energy drink or sports drink
[0002] The present invention provides a highly effective, innovative performance-enhancing energy drink or sports drink, wherein the energy drink or sports drink may contain a dietary supplement of fiber and minerals.
[0003] In detail:
[0004] The present invention relates to the use of a CO2-absorbing formulation for the preparation of an ergogenic food supplement and in particular a drink, especially a sports drink or energy drink.
[0005] The invention also relates to an ergogenic food supplement, and in particular to a non-carbonated drink, especially an energy or sports drink, containing the CO2-absorbing formulation.
[0006] An ergogenic dietary supplement (NEM) is a dietary supplement containing ergogenic substances. Substances that enhance a person's performance in everyday life, especially in sports, are referred to as ergogenic substances in the context of this application. Numerous ergogenic substances are known from the state of the art, particularly from the market, such as L-carnitine, taurine, creatine, or caffeine.
[0007] In the physical form of the dietary supplement envisaged in the practical implementation of the invention, it can be administered as a food, especially as a beverage, also referred to here synonymously as a drink. For the purposes of the present patent application, a beverage / drink should primarily be selected from the group of: liquid food, gel-like food, pasty food, food in the form of a suspension, food in the form of a dispersion, or food in the form of an emulsion.
[0008] The present invention relates in particular to the technical field of beverages and the specifications specified in the preceding paragraph, specifically the technical field of energy drinks or sports drinks, which naturally can also be present in the specifications specified in the preceding paragraph. The term "energy drink" refers to beverages as referred to as "energy drinks" or "energy drinks" according to the "Fruit Juice and Soft Drinks Ordinance of May 24, 2004 (Federal Law Gazette I p. 1016), most recently amended by Article 3 of the Ordinance of April 26, 2023 (Federal Law Gazette 2023 I No. 115)."
[0009] The term “sports drink” refers to a functional drink that is designed or optimized for use during physical exertion and serves to supply water during sporting activity and as an energy supplier during endurance or acute performance.
[0010] Energy drinks commonly available on the market usually contain several of the following ingredients: water, sugar or, in the case of sugar-free versions, sweetener, carbon dioxide, caffeine, taurine, glucuronolactone, vitamins, often from the B vitamin group, inositol, minerals, natural, nature-identical or synthetic flavorings, and colorings.
[0011] An energy drink is known from the state of the art comprising the ingredients: water, acidifier (citric acid), taurine (0.4%), carbon dioxide, acidity regulator (sodium citrates), flavorings, Panax ginseng root extract (0.08%), sweeteners (sucralose, acesulfame K), caffeine (0.03%), preservatives (sorbic acid, benzoic acid), L-carnitine L-tartrate (0.015%), vitamin mixture (nicotinamide, pantothenic acid, vitamin B6, vitamin B12), salt, glucuronolactone, guarana seed extract (0.002%), inositol.
[0012] In addition, the inventors are aware of an energy drink comprising the following ingredients: water, sucrose, glucose, acidifier (citric acid), carbon dioxide, taurine (0.4%), acidity regulators (sodium carbonates, magnesium carbonates), caffeine (0.03%), vitamins (niacin, pantothenic acid, B6, B12), flavorings, colorings (caramel, riboflavins).
[0013] The inventors are aware of a drink based on green tea, with the following ingredients: 93% green tea (water, green tea leaves), sugar, 3% mango juice from mango juice concentrate, natural flavoring, acidifier citric acid.
[0014] The inventors are also aware of a beverage powder comprising the ingredients: isomaltulose, acidifier: citric acid, sea salt, natural lemon flavor.
[0015] In the field of the present invention, there is increasing consumer interest in ergogenic dietary supplements and, in particular, beverages with a perceived pleasantly invigorating effect. There is also increasing consumer interest in ergogenic dietary supplements and beverages that exhibit an invigorating effect and develop this effect as evenly as possible and over the longest possible period. There is also interest in ergogenic dietary supplements and energy drinks that contribute to the non-therapeutic improvement of psychomotor performance and coordination.
[0016] The present invention is based on the object of improving the state of the art or of offering an alternative.
[0017] According to a first aspect of the present invention, the stated object is achieved by the use of a CO2-absorbing formulation for producing an ergogenic dietary supplement, in particular for producing a formulation for producing an ergogenic dietary supplement.
[0018] The following terminology is used to explain this:
[0019] The invention according to the first aspect of the invention uses a CO2-absorbing formulation, i.e. a formulation which, after absorption of the dietary supplement in the organism, absorbs and binds CO2 and thus leads to a reduction of the CO2 content in the blood of the body, wherein the absorbed CO2 is stored in the body for excretion in the form of defecation and, after excretion, reduces the CO2 content of the body.
[0020] A CO2 absorber is preferably provided as the active ingredient in the formulation. The mechanism of action accordingly consists in the v / v uptake of carbon dioxide. In the context of the present invention, v / v uptake of CO2 means the uptake of CO2 by the entire living organism, with an extrapulmonary reduction of carbon dioxide occurring as a result of oral administration. Accordingly, the formulation and the ingredients it contains must also be suitable for food use and preferably already approved.
[0021] A CO2 adsorber can also be used within the scope of the present invention, either together with a CO2 absorber or instead of a CO2 absorber. Whenever an absorber is mentioned in the context of this patent application, an adsorber is expressly understood to be disclosed as an alternative or cumulative. An adsorber has the advantage that no chemical reaction takes place, which, depending on the absorber, could lead to a basic pH. Accordingly, depending on the design, the requirements for the base stability of the matrix can be lower.
[0022] Activated carbon is suggested as an adsorber option.
[0023] Activated carbon is a proven adsorber for organic substances from liquids, including (inorganic) CO2.
[0024] As an alternative to activated carbon, or in the specification of activated carbon, a substance with an open-pore structure and a surface area between 300 and 2,000 m² / g and an iodine value between 500 and 1,200 is proposed as an adsorbent. In particular, activated carbon that meets the requirements of "Regulation (EC) No. 1333 / 2008 of the European Parliament and of the Council of December 16, 2008 on food additives" is considered.
[0025] Although activated carbon has less CO2 absorption capacity than metal hydroxides, it is highly available and has sufficient adsorptive power for many conceivable applications.
[0026] The CO2-absorbing formulation may comprise a CO2 absorber embedded in a carrier matrix or surrounded by a shell.
[0027] In a particular embodiment, the CO2-absorbing formulation consists of the CO2 absorber and the carrier matrix or shell enveloping this absorber.
[0028] In a preferred embodiment, the carrier matrix or the shell of the formulation is designed such that it substantially prevents release of the CO2 absorber during in vivo application. "Substantially" means that during in vivo application of the formulation, at most 5 wt.%, preferably at most 4 wt.%, more preferably at most 3 wt.%, and more preferably at most 1 wt.% of the CO2 absorber is released from the formulation.
[0029] Many CO2 absorbers cause undesirable side effects upon release in the gastrointestinal tract. With calcium hydroxide, as a strong base, the release would lead to a significant increase in pH. With magnesium hydroxide, excessive release could be associated with muscle weakness and diarrhea. According to the invention, the CO2-absorbing formulation is a formulation that serves exclusively to absorb CO2 from the organism; release of the CO2 absorber, whether as a CO2-free reactant or a CO2-containing product, should be prevented as far as possible. In this sense, the carrier matrix or shell is a semipermeable or selectively permeable barrier that allows CO2 from the organism to pass through, allowing absorption by the CO2 absorber within the formulation, but is impermeable to the CO2 absorber and preferably also impermeable to its absorption product(s).
[0030] Accordingly, the shell or the carrier matrix is impermeable to the CO2 absorber and preferably its absorption product(s), even for the duration of the in vivo application.
[0031] In an alternative preferred embodiment, the carrier matrix or the shell of the formulation is designed such that, when used in v / vo, it prevents release of the CO2 absorber in the gastrointestinal tract to such an extent that the concentration of the CO2 absorber in the intestinal lumen is less than 1 mmol / L intestinal content, preferably less than 100 pmol / L, further preferably less than 10 pmol / L and particularly preferably less than 1 pmol / L.
[0032] This minimized release can also be determined using an in vitro test. Both the European Pharmacopoeia (Ph. Eur.) and the American Pharmacopoeia (USP) define precise procedures and equipment for in vitro drug release studies. The European Pharmacopoeia names the equipment according to the dosage form. For example, Chapter 2.9.3 "Drug Release from Solid Dosage Forms" lists the following defined equipment: rotating basket apparatus (USP); rotating paddle apparatus (USP); or flow-through cell (USP). Those skilled in the art are familiar with reaction temperatures and buffers that simulate release of the formulation in the gastrointestinal tract. How the test must be conducted depends on the drug release of the dosage form, and in this case, the delayed release method is selected.
[0033] The present formulation has a selectively permeable shell or carrier matrix, whereby the selective permeability consists in the carrier matrix being permeable to CO2 (and thus the CO2 from the gastrointestinal tract can pass through the shell or carrier matrix to the CO2 absorber and be bound there), and impermeable to the coated CO2 absorber (whether as a CO2-free reactant or a CO2-containing product). The selective permeability of the present formulation persists during the passage of the coated CO2 absorber through the gastrointestinal tract. A physiologically effective amount of CO2 is removed from the human gastrointestinal tract.In this form, the coated CO2 absorber, which is preferably a microcapsule or a microsphere, can pass through the human gastrointestinal tract for a period of at least (about) 30 hours or, in some cases, for a longer period of at least (about) 36 hours or 42 hours or 48 hours.
[0034] The coated CO2 absorber - preferably configured as a microcapsule or microsphere - of any embodiment of the invention is preferably sufficiently robust to persist in the environment of use, for example, to pass through the GI tract or a representative in vitro assay for pharmaceutical applications, without such coated CO2 absorber being significantly degraded and / or preferably without the physical characteristics and / or performance characteristics of the coated CO2 absorber being significantly impaired.In preferred embodiments, the shell or support matrix of the coated CO2 absorber is substantially non-degradable and / or has physical characteristics and / or performance characteristics that are substantially not degraded under physiological conditions of the GI tract (or in vivo representations or mimics thereof) during a period of residence in or during passage through the environment of interest, such as the gastrointestinal tract.
[0035] Preferably, the coated CO2 absorber, which is preferably a microcapsule or a microsphere, and the compositions comprising such a CO2 absorber are not absorbed from the gastrointestinal tract.
[0036] Preferably, the coated CO2 absorber and compositions comprising such coated CO2 absorbers (such as coated calcium hydroxide or magnesium hydroxide particles described herein) bind the CO2 and retain the CO2 in the environment of interest for a significant period of time. For example, in applications involving the binding of CO2 in the gastrointestinal tract, the coated CO2 absorber can bind CO2 in areas of the gastrointestinal tract that have a relatively high concentration of CO2. Such bound CO2 preferably remains bound to the CO2 absorber and is excreted from the body in a sufficient amount such that a physiologically beneficial effect occurs. From an alternative perspective, the coated CO2 absorber does not significantly release the bound CO2 absorber in the environment of interest, for example, the gastrointestinal tract, before a desired beneficial effect is achieved.The coated CO2 absorbers and formulations / compositions described herein are capable of capturing a significant amount of bound CO2. The term "significant amount" as used herein is not intended to imply that the entire amount of bound CO2 is captured. It is preferred that at least a majority of the bound CO2 be captured so that a physiologically beneficial effect occurs.
[0037] The retention period is generally preferably during the time the coated CO2 absorbers or composition are used in the environment of interest. For applications involving the capture of CO2 in the gastrointestinal tract, for example, this time is a period sufficient for a physiologically beneficial effect. In the embodiment in which the composition is used to capture and remove CO2 from the gastrointestinal tract, the retention period can generally be the residence time of the composition in the gastrointestinal tract, and more preferably, the mean residence time in the small intestine and large intestine.
[0038] Advantageously, the permeable selectivity of the coated CO2 absorbers of the invention is sufficiently permanent to produce a beneficial effect, for example, a performance-enhancing or regeneration-promoting effect. The permanent selectivity (e.g., the permanent selective permeability) of the coated CO2 absorbers is particularly advantageous for binding CO2 in the gastrointestinal tract.
[0039] The coated CO2 absorbers of the invention are preferably sufficiently robust to persist in the environment of intended use. In one application, for example, the coated CO2 absorbers are sufficiently robust to pass through the gastrointestinal system (or to pass through an in vitro assay representative thereof) without such coated CO2 absorber being substantially degraded. In preferred embodiments, the coating or support matrix of the CO2 absorber is substantially robust (e.g., it is not degraded, separated, and / or delaminated) under physiological conditions of the gastrointestinal tract (or in vitro representations or mimics thereof) during a period of residence in and passage through the gastrointestinal tract.For example, the CO2 absorber and the shell or support matrix are not substantially decomposed under in vitro conditions, which conditions are preferably selected from the group consisting of (i) an aqueous solution having a pH of (about) 1 for a period of (about) 3 hours, (ii) an aqueous solution having a pH of (about) 3 for a period of (about) 6 hours, (iii) an aqueous solution having a pH of (about) 8 for a period of (about) 10 hours, (iv) an aqueous solution having a pH of (about) 6 for a period of (about) 20 hours, and combinations thereof, each at a temperature of (about) 37°C with stirring.
[0040] In some embodiments, the coated CCL absorbers can be robust in other respects in addition to not degrading, for example, including physical characteristics and / or performance characteristics. Physical characteristics can include particle size, particle size distribution, and / or surface properties, for example, visually assessed using microscopes, such as electron microscopes and / or confocal microscopes. Performance characteristics can include specific binding capacity, selectivity (e.g., selective permeability), and durability or persistence.
[0041] Some preferred in vitro assays that can be used in connection with the determination of robustness, for example for the purpose of modifying or optimizing an encapsulated CO2 absorber in this respect, include the previously listed in vitro drug release studies, where the CO2 absorber as the “active ingredient” is not to be released.
[0042] In some embodiments, the shell or the carrier matrix may impart other properties related to robustness, for example, sufficient resistance to withstand mechanical forces or stresses associated with swelling of the CO2 absorber and / or associated with the formulation (for example, compression occurring during capsule formulation).
[0043] In embodiments of the invention, the shell or carrier matrix can protect the CO2 absorber from the external environment, for example, the gastrointestinal tract. For example, the shell or carrier matrix can bind functional groups (e.g., hydroxyl groups) of the CO2 absorber and prevent their exposure to the gastrointestinal environment.
[0044] Preferably, the CO2 absorbers and compositions comprising such CO2 absorbers are not absorbed by the gastrointestinal tract. The term "unabsorbed" and its grammatical equivalents are not intended to imply that the entire amount of administered CO2 absorber is not absorbed. It is expected that certain amounts of the CO2 absorber may be absorbed. It is preferred that (about) 90% or more of the CO2 absorber is not absorbed, preferably (about) 95% or more is not absorbed, even more preferably (about) 97% or more is not absorbed, and most preferably (about) 98% or more of the CO2 absorber is not absorbed.
[0045] In one embodiment, the carrier matrix comprises a binder that binds the CO2 absorber as a substance for binding other substances, allowing it to continue absorbing CO2. Ideally, the binder can continue to function even after CO2 absorption, which is often accompanied by a chemical reaction forming reactants, such as calcium hydroxide or magnesium hydroxide.
[0046] The carrier material is preferably biodegradable and / or particularly preferably selected from the group comprising: beeswax, paraffin, cellulose, derivatized cellulose, pectin, gelatin, alginate, agarose, latex rubber, dandelion rubber, polyhydroxyalkanoate (PHA), polylactide (PLA) and fibroin, or a combination thereof.
[0047] In one embodiment, the CO2 absorber in combination with the carrier matrix forms a composite active ingredient, which preferably additionally contains fiber and / or minerals.
[0048] Particularly preferably, the CO2 absorber and / or the composite active ingredient including the CO2 absorber can consist predominantly of fiber and CO2 absorbers and / or minerals, wherein the fiber can form a biodegradable, bio-based matrix and / or wherein the minerals can serve as additional or sole CO2 absorbers.
[0049] For the purposes of this patent application, "predominantly" means that the fiber and the CO2 absorbers and / or minerals constitute at least 50% (each wt% and / or mass%) of the composite material and / or the dietary supplement, i.e., in particular, the drink. In particular, they constitute at least 55, 60, 65, 70, 75, 80, 85, and most preferably at least 90, or even at least 95%.
[0050] The proportion of CO2 absorbers is particularly preferably divided between minerals at up to 100, 95, 90, 85, 80, 75, 70, 65, 60, 55, 50, 45, 40, 35, 30, 25, 20, 15, or 10%. Examples of dietary fiber include flaxseeds and chia seeds, cellulose fiber, as well as traces or fibers selected from the following groups: legumes, nuts and seeds, whole grain products, vegetables and fruits such as salsify, artichokes, peppers, rhubarb, berries and pears, as well as porcini mushrooms and chanterelles.
[0051] In another embodiment, the CO2-absorbing formulation contains the CO2 absorber in a flowable carrier matrix. A gel formulation is preferred.
[0052] In one embodiment, the absorbent formulation comprises, as a coated formulation, both a shell consisting of a wall material, wherein the shell is permeable to CO2 and optionally also to water vapor, and a core region comprising at least one CO2 absorber.
[0053] Advantageously, the shell or carrier matrix, preferably permeable to water vapor, is impermeable to water. This is advantageous both for the preparation of the formulation (e.g., as an aqueous suspension) and during consumption. While the shell is permeable to water vapor in one embodiment, allowing controlled moistening of the active ingredient, it prevents water from penetrating the core area or CO2 absorber components from escaping. Reaction with water could cause the core to swell and damage the shell.
[0054] In the context of this application, the term "waterproofness" is synonymous with the term "watertightness." The so-called watertightness of the shell is measured based on the water column, under which pressure the material begins to allow water to pass through. According to DIN EN 343:2019, a membrane is watertight from a value of 1,300 mm upwards.
[0055] An encapsulated drug formulation can be provided in at least one of the following five embodiments: Liquid core comprising the CO2 absorber with a membrane shell to form a liposome or niosome.
[0056] A liposome is generally a spherical structure composed of lipid molecules forming a bilayer. Liposomes are artificially produced vesicles used to transport and typically release active ingredients. The structure of liposomes is similar to that of cell membranes, as they are also composed of lipids. Liposomes can have various sizes and shapes, from small unilamellar (single layer) to larger multilamellar (multiple layers) structures. Their ability to encapsulate both lipophilic (fat-soluble) and hydrophilic (water-soluble) substances makes them effective carrier systems for the delivery of drugs or other active ingredients.
[0057] The areas of application of liposomes are diverse:
[0058] Drug delivery: Liposomes can be used to encapsulate drugs, protect them from degradation, and deliver them to specific cells or tissues. This allows for improved bioavailability and targeted action.
[0059] Food industry: Liposomes can also be used in the food industry to transport and release flavors or nutrients.
[0060] The use of liposomes enables the controlled release of active ingredients and helps improve their stability. This makes them an important tool in the development of pharmaceuticals and other products requiring precise drug delivery.
[0061] However, the present development does not use the potential liposomes for release, but rather for transporting and retaining the CO2-absorbing formulation.
[0062] In one embodiment, the coated drug formulation can therefore be present as a liposome. The advantage of liposomes lies in the high gas permeability of the membrane shell, allowing for high CO2 uptake. Niosomes are microscopically small spheres similar to liposomes, in which a double membrane encloses an interior space. Active ingredients can be incorporated into this interior space. Niosomes are structured similarly to liposomes. However, liposomes contain double membranes formed from phospholipids, whereas the building blocks of the niosome double membrane are derived from sugars or amino acids. Solid core comprising the C02 absorber with a single layer
[0063] Shell. In this embodiment, the solid core is encased in a single-layer shell. Accordingly, it is a simple and inexpensive formulation. Solid core comprising the CCh absorber with a multilayer
[0064] Covering.
[0065] In this embodiment, the solid core is encased in a multilayer shell. This is a complex formulation in which the shell's properties regarding permeability, stability, or biocompatibility can be specifically adjusted or distributed. Thus, an inner shell layer can provide the formulation with the necessary strength, while an outer shell layer can achieve the specified permeability. Microcapsule.
[0066] In this embodiment, the coated active ingredient formulation can also be present as a microcapsule.
[0067] Microcapsules are free-flowing powders with particle diameters ranging from approximately 1 μm to 1,000 μm. They are manufactured using various coating processes for finely divided solid or liquid substances. Polymers are typically used as the shell or wall material. Microcapsules therefore essentially consist of two disparate regions: the core region and the shell region.
[0068] Microcapsules are small, spherical structures consisting of an outer shell (shell or membrane) enclosing an inner core. These tiny capsules can generally enclose a variety of materials, such as liquids, solids, or gases.
[0069] There are various methods for producing microcapsules, including:
[0070] Coacervation: This is a process in which polymers precipitate from a solution and collect around a substance to be encapsulated to form a shell.
[0071] Spray drying: A liquid containing the substance to be encapsulated is atomized into fine droplets. The droplets then dry, and a solid shell forms around the core. This method is particularly suitable for the formation of microcapsules with a diameter of less than 100 μm. Depending on the polymer and the process, the resulting microcapsules have a sponge-like structure. In such cases, an additional coating of the microcapsules is necessary.
[0072] In-situ polymerization: Here, polymerization is carried out directly around the core to form the microcapsule.
[0073] The use of microcapsules allows precise control over the release of ingredients and can help improve the stability and efficiency of various products.
[0074] For the microcapsules to be free-flowing, no adhesive forces must occur between the particles, which could cause the particles to stick together or even agglomerate (“clumping”). Flowability can be determined using DIN standard EN ISO 6186:2023-10, as also described in the European Pharmacopoeia, Chapter 2.9.1 “Flowability.” This standard defines an apparatus used to control and test the flowability of solids in powder or granular form (e.g., plastic granules). The material is poured through a standardized funnel, and the flow time is determined using a stopwatch. This provides information regarding processability and consistent process control in production. Good flowability is important for trouble-free automatic processing. The flowability of materials is primarily influenced by the surface properties of the granules.
[0075] Manufacturing processes suitable for microencapsulation include phase separation processes (simple and complex coacervation), interfacial polymerization processes (polycondensation or polyaddition from dispersions) and mechanical-physical processes (fluidized bed process, spray drying).
[0076] The fundamental disadvantage of conventional microencapsulation is the relatively high manufacturing costs.
[0077] Embodiment 5, if a coating is also understood to include a carrier matrix: solid CO2 absorber particles in a carrier matrix. The carrier matrix can be, in particular, a gel-like and / or otherwise flowable paste, and / or the carrier matrix can have a dynamic viscosity, in particular, in the range of 2,000 mPas (honey-like) to 100,000 mPas (syrup-like), each measured at 20°C. Advantageously, the invention can provide that, in the coated active ingredient formulation, the microcapsule is a microsphere in which the CO2 absorber is incorporated in a polymeric carrier matrix in solid, dispersed form or in dissolved form.
[0078] Microspheres are systems related to microcapsules, but lack a precise separation into core and shell regions. However, in their size of approximately 1 pm to 1,000 pm, microspheres correspond to microcapsules. In microspheres, the embedded active ingredient is incorporated into the carrier matrix in solid, i.e., dispersed, or dissolved form. Microspheres are thus a special form of microcapsule. The carrier matrix is usually made of a polymer.
[0079] Embedding the CO2 absorber in microspheres has the advantage that the carrier matrix provides a continuous spectrum with respect to its "wall thickness" (defined as the shortest distance from the active ingredient to the outside of the microsphere), allowing the penetrating CO2 gas to reach the active ingredient in a staggered manner, starting with the active ingredient inclusions closest to the surface. This results in advantageous CO2 uptake kinetics, which, with an early onset, leads to long-lasting, continuous CO2 uptake.
[0080] There are several methods for producing microspheres, including:
[0081] Extrusion: Here, the solid granular CO2 absorber is processed in an extruder together with a polymer forming the carrier matrix. Melting the polymer in the extruder and intensively mixing the CO2 absorber into the molten polymer stream results in the CO2 absorber being dispersed in the polymer matrix. After extrusion, the mixture is granulated while cooling and then optionally further ground and surface treated.
[0082] Batch extrusion (“melting and grinding”): Here, the solid granular CO2 absorber is melted together with a polymer forming the carrier matrix and, after cooling, ground until the desired particle size is reached.
[0083] Preferably, the CO2-absorbing formulation contains a CO2 absorber.
[0084] The term "absorption" describes the process of carbon dioxide being absorbed or "dissolved" into another phase. This does not involve adsorption on the surface, but rather absorption into the free volume of the absorbing phase. A distinction is made between physical and chemical absorption. In physical absorption, the carbon dioxide is dissolved as a gas in a solvent. Mixing occurs without a chemical reaction.
[0085] In chemical absorption, the carbon dioxide undergoes a chemical reaction with the “solvent” or absorbent, forming a product substance.
[0086] In contrast, “adsorption” refers to the accumulation of carbon dioxide on the surface of a solid.
[0087] Advantageously, it can be provided that in the coated active ingredient formulation, the shell or the carrier matrix has a CO2 permeability of 0.004 to 2,500 x 10 13 cm 3 cm cnr 2 Pa 1 s -1 , preferably from 5 to 500 x 10 13 cm 3 cm cnr 2 Pa 1 s -1 , and particularly preferably from 10 to 300 x 10 -13 cm 3 cm cnr 2 Pa -1 s -1 The shell can, for example, have a CO2 permeability of 0.1, 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 15, 20, 25, 30, 35, 40, 45, 50, 55, 60, 65, 70, 75, 80, 85, 90, 95, 100, 150, 200, 250 or 275 x 10 13 cm 3 cm cnr 2 Pa 1 s~ 1 It has been shown that a shell with such CO2 permeability achieves adequate absorption kinetic profiles.
[0088] A material with high permeability to CO2 is suitably used as the wall material of a shell, preferably a polymer. This enables efficient CO2 absorption in the context of in-vitro applications. Examples of suitable polymers include: polyethylene such as high-density polyethylene (HD-PE) or low-density polyethylene (LD-PE) (although the inventors currently consider these to be less suitable); (bio)degradable PE, including polylactide (PLA), polybutylene adipate terephthalate (PBAT, EcoFlex), thermoplastic polyurethane (TPU), and polyhydroxyalkanoates such as poly[(R)-3-hydroxybutyrate] (PHB).
[0089] The predefined CO2-permeable carrier matrix is preferably the carrier matrix of a microsphere.
[0090] Advantageously, the invention can provide that in the coated active ingredient formulation, the carrier matrix or the shell has a water vapor permeability of 0.009 to 32,000 x 10 13 cm3 cm cnr 2 Pa 1 s -1 , and preferably from 100 to 1500 x 10 13 cm 3 cm cnr 2 Pa 1 s -1 The shell can, for example, have a water vapor permeability of 150, 200, 250, 300, 350, 400, 450, 500, 550, 600, 650, 700, 750, 800, 850, 900, 950, 1000, 1050, 1100, 1150, 1200, 1250, 1300, 1350, 1400 or 1450 x 10 13 cm 3 cm cnr 2 Pa- 1 s" 1 It has been found that a carrier matrix or shell with such a water vapor permeability can moisten the absorber material up to approx.
[0091] 10 wt.% moisture, which is essential for the efficient absorption of CO2, especially with basic absorbers such as calcium hydroxide, since only after the carbon dioxide has been converted to carbonic acid can this carbonic acid react with the calcium hydroxide to form calcium carbonate and water.
[0092] A material, preferably a polymer, with sufficiently high water vapor permeability is suitably used as the wall material for the shell. This enables CO2 absorption via intermediate carbonic acid in the context of in-vitro applications. Examples of suitable polymers include: polyethylene such as high-density polyethylene (HD-PE) or low-density polyethylene (LD-PE), polylactide (PLA), thermoplastic polyurethane (TPU), polybutylene adipate terephthalate (PBAT, EcoFlex), and polyhydroxyalkanoates such as poly[(R)-3-hydroxybutyrate]. According to the inventors' current assessments, it appears particularly advantageous if the polymer is (bio)degradable.
[0093] The predefined water vapor permeable carrier matrix is preferably the carrier matrix of a microsphere.
[0094] In a further embodiment, the shell or carrier matrix can constitute a mass fraction of 10 to 95 wt.%, preferably 40 to 60 wt.%, and particularly preferably 55 to 65 wt.%, in each case based on the weight of the CO2-absorbing formulation. The mass fraction of the shell can be, for example, 42, 44, 46, 48, 50, 52, 54, 56, 58, 60, 62, or 64 wt.%. The carrier matrix is preferably the carrier matrix of a microsphere.
[0095] Furthermore, it is conceivable that the shell or carrier matrix has an average layer thickness of 10 to 500 pm, preferably of 50 to 250 pm and particularly preferably of 100 to 200 pm.
[0096] As has been shown, such layer thicknesses allow sufficient CO2 uptake on the one hand, but are stable enough to prevent the unwanted release of the core material into the organism on the other.
[0097] In the coated formulation, the wall material constituting the shell is preferably a polymer and particularly preferably selected from the group consisting of poly(organo)siloxane; polyolefin; polyester; polybutylene succinate; polybutylene adipate terephthalate (PBAT); polyethylene such as high-density polyethylene (HDPE) or low-density polyethylene (LDPE); thermoplastic polyurethane (TPU), polylactide (PLA), polyhydroxyacetic acid (PGA), and poly(lactide-co-glycolide) (PLGA); lipids such as fatty acids or phospholipids. The wall material is particularly preferably a polyester.
[0098] The use of a polyester has the advantage that it has very good resistance to bases and acids and can be processed in a particularly wide process window.
[0099] A pharmaceutically acceptable material, preferably a polymer, is suitably used as the wall material. This enables a low- or no-side-effect in-vitro application. Examples include the following polymers: polyethylene such as high-density polyethylene (HD-PE) or low-density polyethylene (LD-PE), polylactide (PLA), polybutylene adipate terephthalate (PBAT; EcoFlex), thermoplastic polyurethane (TPU), and polyhydroxyalkanoates such as poly[(R)-3-hydroxybutyrate] (PHB).
[0100] The wall material used is a material (preferably a polymer) that, due to its purity, has a content of so-called "leachables" or "extractables" that is below the permissible limits. This enables a low- or no-side-effect in-vitro application.
[0101] In the coated formulation, the shell is suitably inert towards the CO2-absorbing active ingredient.
[0102] This means that with a basic CO2-absorbing active ingredient, such as calcium hydroxide, the shell is base-stable.
[0103] In addition, the casing should be stable throughout the entire gastrointestinal passage.
[0104] The term "stable" in the context of the present invention, when used to characterize the shell in base, means that the shell remains largely intact after exposure to a saturated calcium hydroxide solution (alternatively: other hydroxide compounds, generally any metal hydroxides) either for one day at 90°C or for 30 days at 40°C. Preferably, the shell remains substantially completely intact under these conditions, and more preferably, the shell remains practically completely intact under these conditions. In the context of acid treatment, the terms "largely, substantially completely, and practically completely" mean that the shell matrix retains at least 90%, at least 95%, and at least 99% of its chemical bonds in the polymer backbone, respectively, after exposure to these conditions.
[0105] This also means that for an acidic CO2-absorbing active ingredient, the shell must be acid-stable. Acid stability is also required for oral administration or gastric transit.
[0106] The term "stable" in the context of the present invention, when used to characterize the shell in acid, means that the shell remains substantially completely intact after exposure to a 20% sulfuric acid solution for either one day at 90°C or 30 days at 40°C. Preferably, the shell remains substantially completely intact under these conditions, and most preferably, the shell remains virtually completely intact under these conditions. In the context of acid treatment, the terms "substantially completely, substantially completely, and virtually completely" mean that the shell matrix retains at least 90%, at least 95%, and at least 99% of its chemical bonds in the polymer backbone, respectively, after exposure to these conditions. For further stability requirements, see the above statements.
[0107] It is also advantageous if the shell of the coated formulation forms a semipermeable barrier, allowing nonpolar molecules such as CO2 gas molecules to pass through the shell and reach the core area of the CO2 absorber. However, as a semipermeable barrier, this shell is impermeable to charged molecules such as salt cations or anions, and accordingly also to protons and hydroxide anions. Thus, the shell represents a selectively permeable shell. This selective permeability can prevent, for example, the release of hydroxide ions into the organism from a strongly basic CO2 absorber such as calcium hydroxide.
[0108] Wall materials that enable the construction of such a selectively permeable shell, as described above, include polyethylene such as high-density polyethylene (HD-PE) or low-density polyethylene (LD-PE), polylactide (PLA), polybutylene adipate terephthalate (PBAT; EcoFlex), thermoplastic polyurethane (TPU) and polyhydroxyalkanoates such as poly[(R)-3-hydroxybutyrate] (PHB).
[0109] Advantageously, the invention can provide that the CO2 absorber is selected from the group consisting of inorganic hydroxide compound, lithium peroxide and mixtures thereof, with lithium hydroxide, sodium hydroxide, potassium hydroxide, calcium hydroxide and magnesium hydroxide, and mixtures thereof, being preferred.
[0110] Advantageously, the invention can provide that the CCL absorber comprises calcium hydroxide.
[0111] According to a further embodiment, the CO2 absorber consists essentially of calcium hydroxide. The calcium hydroxide reacts with the carbon dioxide to form pharmaceutically acceptable calcium carbonate. "Essentially" means that the CO2 absorber contains at most 5 wt.%, preferably at most 4 wt.%, more preferably at most 3 wt.%, and more preferably at most 1 wt.% of other components.
[0112] In an advantageous embodiment, the calcium hydroxide-containing CO2 absorber is substantially free of sodium and potassium hydroxide. "Substantially" means that the CO2 absorber contains at most 4 wt.%, preferably at most 2 wt.%, preferably at most 1 wt.%, more preferably 0.5 wt.% of sodium and potassium hydroxide, and particularly preferably no sodium and potassium hydroxide.
[0113] In one embodiment, the calcium hydroxide-containing compositions described above contain, as an additional optional ingredient, an effective amount of a hygroscopic or deliquescent humectant capable of absorbing carbon dioxide.
[0114] According to a further embodiment, the CO2-absorbing material consists essentially of magnesium hydroxide. Magnesium hydroxide has the advantage of being more easily tolerated during gastrointestinal use due to its lower basicity. Furthermore, its hygroscopic nature facilitates initial moistening of the absorber material, which promotes absorption through the dissolution of the CO2 as carbonic acid, forming the carbonate. Ultimately, it is a cheap substance and has been shown to be particularly suitable for use in the production of microspheres. The magnesium hydroxide reacts with the carbon dioxide to form pharmaceutically acceptable magnesium carbonate. "Essentially" means that the CO2-absorbing material contains no more than 5% by weight, preferably no more than 4% by weight, more preferably no more than 3% by weight, and more preferably no more than 1% by weight of other components.Magnesium hydroxide has the advantage of having a 30% higher CO2 binding capacity than calcium hydroxide. Thus, 100 g of calcium hydroxide (= 1.34 mol) binds 30 liters of CO2, and 100 g of magnesium hydroxide (= 1.71 mol) binds 39 liters of CO2 (assuming a CO2 movolume of 22.4 L / mol under standard physical conditions).
[0115] Magnesium hydroxide has a higher CO2 binding capacity per gram of absorber than Ca(OH)2 due to its lower molecular weight. However, it has slower binding kinetics and affinity. Thus, using these two metal hydrides as examples, albeit preferred examples, the properties of the formulation in the organism can be controlled through targeted formulation composition.
[0116] In an advantageous embodiment, the magnesium hydroxide-containing, CO2-absorbing material is substantially free of sodium and potassium hydroxide. "Substantially" means that the CO2-absorbing material contains at most 4 wt.%, preferably at most 2 wt.%, preferably at most 1 wt.%, more preferably 0.5 wt.% of sodium and potassium hydroxide, and particularly preferably no sodium and potassium hydroxide.
[0117] In one embodiment, the magnesium hydroxide-containing compositions described above contain, as an additional optional ingredient, an effective amount of a hygroscopic or deliquescent humectant capable of absorbing carbon dioxide.
[0118] According to a further advantage, it can be provided that in the formulation according to the invention, the CO2 absorber has a CO2 absorption capacity of more than 10 mg CO2 / g of formulation, preferably more than 40 mg CO2 / g of formulation, particularly preferably more than 50 mg CO2 / g of formulation, and in particular more than 75 mg CO2 / g of formulation. The higher the CO2 absorption capacity, the smaller the amounts of applied formulation are necessary to achieve a relevant ergogenic effect.
[0119] In one embodiment, the ergogenic dietary supplement is selected from the group consisting of bar, gummy candy, dragee, tablet, granule, powder, capsule, gel and drink.
[0120] In a preferred embodiment, the ergogenic dietary supplement is a beverage, in particular an energy drink or a sports drink. In one embodiment, the beverage, especially an energy drink or sports drink, contains one or more of the following substances: caffeine, creatine, beta-hydroxy-beta-methylbutyrate (HMB), carnitine, coenzyme Q10, inositol, glucuronolactone, taurine, branched-chain amino acids (BCAA), glucose, and sweeteners.
[0121] In a preferred embodiment, the drink, especially in a form as an energy drink or sports drink, contains 0.05 to 50 g taurine / l, 0.1 to 10 g glucuronolactone / l, 0.1 to 1 g caffeine / l, 1 to 50 g glucose / l, 10 to 150 g sucrose / l and 20 to 500 mg inositol / l, for the non-therapeutic improvement of psychomotor performance and coordination, wherein preferably further vitamins and / or further auxiliary and / or additives and / or mixtures of these substances are provided in the composition, wherein preferably independently of one another, glucuronolactone in a concentration of 1.2 to 2.4 g / l, caffeine in a concentration of 0.16 to 0.32 g / l, glucose in a concentration of 10 to 25 g / l, sucrose in a concentration of 40 to 100 g / l, and inositol in a concentration of 100 to 200 mg / l.
[0122] In one embodiment, the drink, especially an energy drink or sports drink, contains 20% to 70% calcium hydroxide and / or 20% to 70% magnesium hydroxide and / or other metal hydroxide, with the sum of the components being less than 100%. 30, 35, 40, 45, 50, 55, 60, or 65% may also be relevant for the lower limit of the beneficial range; 65, 60, 55, 50, or 45% may also be relevant for the upper limit of the beneficial range.
[0123] The viscosity can be controlled by the composition of the formulation. The higher the viscosity of the carrier solution, the higher the proportion of meta II hydroxides should be.
[0124] According to a second aspect of the present invention, the stated object is achieved by an ergogenic food supplement containing a CO2-absorbing formulation which is used as described above for the first aspect of the invention.
[0125] In one embodiment, the ergogenic dietary supplement can be used for optimizing acid-base balance through acid elimination after oral administration.
[0126] The following physiological effects are conceivable, especially during sporting activities:
[0127] Prevention of overacidification in overwork Fast regeneration of the body
[0128] • Avoiding muscle soreness
[0129] • Longer performance due to higher buffer capacity
[0130] • Delaying muscular exhaustion
[0131] • Enable prolonged training and more effective muscle building.
[0132] On the occupational physiology background:
[0133] The acid-base balance plays a significant role in coping with sporting and other physical stress conditions. In simplified terms, four phases can be distinguished from a sports physiological perspective: (i) the warm-up phase, in which the athlete must transfer his or her entire circulatory and respiratory situation from the resting phase to the exertion phase. In this process, both the cardiac output (CO) and the respiratory output (AT) are increased and adapted to the sporting activity. Since this adaptation process lags behind the actual sporting activity, there is a short-term accumulation of acid valences in the muscles until the sport reaches (ii) the steady-state phase. Here, CO and AT are adequately balanced for the stress. In this balanced phase, the athlete is capable of engaging in endurance sports. If sporting activity increases beyond this level for a short time (e.g.uphill climb), then (iii) overload occurs in the muscles and, just as in the start-up phase, anaerobic glycolysis (energy production from sugar without sufficient oxygen supply) occurs. This state is caused by an inadequate supply of O2, which is primarily due to a blood flow (CO) that cannot be increased any further. Since acidic waste products are produced during anaerobic glycolysis, the muscles become increasingly over-acidified. This state of overload can be maintained as long as adequate acid buffering from anaerobic glycolysis is possible. Not only the local buffer capacity plays an important role here, but also the buffer capacity of the freshly supplied blood. Thus, the amount of local and supplied buffer capacity as well as the glucose availability define the duration of a possible anaerobic exercise phase.After the end of the physical activity, (iv) the regeneration phase is characterized by the replenishment of muscular energy stores and the removal of local acid valences from the muscles, which are largely responsible for muscle soreness. This regeneration phase can be shortened by an optimized acid-base balance with a higher absorption capacity for acid valences.
[0134] This is where one of the inventive ideas comes in:
[0135] A dietary supplement suggested here, preferably as an energy drink or sports drink, increases the buffering capacity for acids in the blood through the enteral elimination of volatile acid (CO2), thus optimizing the acid-base balance. This delays systemic and local hyperacidity in the muscles and facilitates a faster return to a balanced state (steady state). This results in longer performance under anaerobic conditions (start-up and overload phases) as well as faster regeneration after the anaerobic phase or the end of the sporting activity.
[0136] Under physiological conditions, the respiratory volume (RI) can be increased by a factor of 20 during physical activity. Oxygen uptake plays a subordinate role; instead, the exhalation of CO2 is accelerated. The enteral elimination of CO2 from the blood using the present invention therefore reduces the work of breathing, and the athlete becomes "out of breath" less quickly. As an additional effect, energy consumption is lowered by reducing the work of breathing, making it available for increased performance elsewhere (muscles).
[0137] The accumulation of CO2 in the blood is directly linked to increased fatigue (typical early signs of hypercapnia include yawning and reduced alertness). Enteral CO2 elimination prevents systemic hypercapnia and thus counteracts fatigue, and improved cognitive performance can be expected.
[0138] In one embodiment, the ergogenic dietary supplement can be used to reduce the work of breathing following oral administration.
[0139] The following physiological effects are conceivable, especially during sporting activities:
[0140] Reducing energy consumption
[0141] Increase in performance, particularly in terms of duration In one embodiment, the ergogenic dietary supplement can be used to increase alertness or attention after oral administration.
[0142] The following physiological effects are conceivable, especially during sporting activities:
[0143] • Reduce fatigue by avoiding hypercapnic states
[0144] • Increase cognitive performance.
[0145] In one embodiment, the ergogenic dietary supplement can be used for detoxification following oral administration.
[0146] Definitions
[0147] According to Wikipedia, a "beverage," or "drink," is defined as a liquid intended for consumption, usually processed or prepared. Beverages are consumed either to quench thirst and thus to provide the body with water, as food, or purely as a luxury item. The dynamic viscosity of a beverage, for the applications considered here, can range from 0.75 mPas (water-like) to 100,000 mPas (syrup-like).
[0148] Food supplements (NFS) are considered foods for general consumption. They differ from other foods in that they are offered in small doses, such as tablets, capsules, or portioned drinks. They contain vitamins, minerals, or other nutrients intended to have a nutritional or physiological effect in concentrated form. They may supplement the normal diet but do not have a medicinal effect.
[0149] An ergogenic dietary supplement is defined as a dietary supplement that contains ergogenic substances. Substances that promote a person's performance in everyday life, or particularly in sports or fitness, are referred to as ergogenic substances in the context of this application. Numerous ergogenic substances are known from the prior art, such as L-carnitine, taurine, creatine, or caffeine. The present invention now provides, for the first time, CO2 absorbers as ergogenic substances. The term "cellulose" is defined in the context of this invention as a collective term for fibers made from natural, regenerated, and derivatized cellulose, such as cellulose esters or cellulose ethers.
[0150] A composite material (composite for short) is a mixture of two or more pure basic materials—in this case, a CO2 absorber and a matrix—at least one of which forms a continuous phase. The CO2 absorber and matrix, which comprise a composite material, are bonded together. However, the individual basic materials do not dissolve among each other, or only dissolve superficially.
[0151] The term "polymer" in this document encompasses, on the one hand, a collective of chemically uniform macromolecules that differ in terms of degree of polymerization, molecular weight, and chain length, which were produced by a polyreaction (polymerization, polyaddition, polycondensation). On the other hand, the term also encompasses derivatives of such a collective of macromolecules from polyreactions, i.e., compounds that were obtained by reactions, such as additions or substitutions, of functional groups on given macromolecules and which may be chemically uniform or chemically heterogeneous. The term also encompasses copolymers and so-called prepolymers, i.e., reactive oligomeric pre-adducts whose functional groups are involved in the construction of macromolecules.
[0152] The term "copolymer" in this document refers to a polymer composed of two or more different monomer units. This distinguishes a copolymer from a homopolymer, which is composed of only one (real or imaginary) monomer type and, accordingly, has only one repeating unit. Copolymers can be divided into five classes:
[0153] 1 .) statistical copolymers, in which the distribution of the two monomers in the chain follows a statistical distribution,
[0154] 2.) Gradient copolymers, which are in principle similar to statistical copolymers, but in which the proportion of one monomer increases and the other decreases along the chain,
[0155] 3.) Alternating copolymers, in which the two monomers alternate,
[0156] 4.) Block copolymers and segment copolymers consisting of longer sequences or
[0157] blocks of each monomer, and
[0158] 5.) Graft copolymers, in which blocks of one monomer are grafted onto the backbone of another monomer. In this document, "molecular weight" refers to the molar mass (in grams per mole or in Daltons) of a molecule. "Mean molecular weight" in this document always refers to the number average of the molecular weight distribution M n (Number average). The term "number average molar mass" is also used as a synonym for "average molecular weight."
[0159] The term "solvent" in this document refers to compounds as listed as organic solvents in CD Römpp Chemie Lexikon, 9th edition, version 1.0, Georg Thieme Verlag, Stuttgart 1995. The polyols used in the invention are not covered by this definition, although they act as solvents for the monomers and also the low-molecular polymer formed by radical polymerization.
[0160] In this document, "solid" refers to substances that do not change their shape without external influence or are difficult to deform, but in particular, they are not flowable. "Liquid" refers to substances that can be deformed and are flowable, including highly viscous and pasty substances.
[0161] It should be expressly pointed out that, in the context of this patent application, indefinite articles and indefinite numerical expressions such as "one...", "two...", etc. are generally to be understood as "at least one...", "at least two...", etc., unless the context or the specific text of a particular passage indicates that only "exactly one...", "exactly two...", etc. are intended. Furthermore, all numerical expressions and information on process parameters and / or device parameters are to be understood in the technical sense, i.e., subject to the usual tolerances. Even the explicit specification of the restriction "at least" or "at least" or similar does not imply that the simple use of "one", i.e., without specifying "at least" or similar, means "exactly one."
[0162] If it is stated that AB “has”, this means that A can have C in addition to B, or as a special case, that A consists entirely of B.
[0163] Unless otherwise stated, the percentages in this document are by weight. In the context of this application, the carbon dioxide molecule may be written not only as CO2, but also as CO2. Both notations are to be understood as the same.
[0164] Preferred features for embodiments envisaged by the inventors, as well as previously envisaged embodiments:
[0165] In particular, consider a drink (or other food) with an enteral CO2 absorber that meets the following basic properties:
[0166] Inert gastrointestinal passage: During the entire gastrointestinal passage, the drink is neither attacked nor metabolized by gastric acid (pH 1.3) nor by enzymes (pepsin, bile acid, etc.) of the gastrointestinal tract (acid and enzymatic stability)
[0167] Environmental compatibility: To achieve optimal environmental compatibility, we use only bio-based and biodegradable materials or minerals that biodegrade under normal environmental conditions. Neither the product itself nor its degradation products are toxic or biologically harmless.
[0168] For optimal function, the following properties are necessary: o high gas permeability for CO2o good water vapor permeability o ion / water tightness
[0169] formulation
[0170] The dietary supplement, or the food produced therewith, can preferably be produced both as a suspension and as a flowable matrix absorber composition.
[0171] Suspensions, for example, are an inventive development of previous inventions by the present inventors (microspheres or microspherules). A spherical shape is preferred for an optimal ratio of absorber to microparticle surface, but other shapes (pellets, cuboids, etc.) can also be chosen. The "spherical" shape is to be understood in terms of food or chemical engineering – the decisive factor is not a 100% mathematically precise shape, but the shape should be essentially round. The particles in the suspension should be either dimensionally stable throughout the entire gastrointestinal passage or geometrically flexible (e.g., using a wax matrix) (see also below).
[0172] Flowable matrix absorber formulation: Here, the pure absorber particles are not further encapsulated, but are present as free particles in a flowable, non-resorbable matrix (e.g., wax, gel, etc.). The flowable, surrounding matrix ensures the most complete separation of the CO2 absorber particles from the environment.
[0173] Forms of administration
[0174] The dietary supplement can be administered in various forms, and both color and flavor can be customized to meet user needs.
[0175] In simple terms, the dietary supplement consists of fiber and minerals that can absorb CO2 enterally in a controlled manner.
[0176] The following forms of administration are preferred with the formulations described above:
[0177] Gel stripping packs (similar to Power-Gel™)
[0178] Bar
[0179] drink
[0180] Powder for self-mixing in non-carbonated drinks (users can mix their own individual sports drink)
[0181] Acid-resistant capsules, dragees, coated tablets, but deliberately no pharmaceutical applications
[0182] CO2 traps
[0183] All forms of metal hydroxides (e.g., Ca(OH)2 or Mg(OH)2) are preferred. However, all other CO2 absorbers developed by the inventors in preliminary work are also possible.
[0184] Matrix materials
[0185] Bio-based matrix materials:
[0186] Agarose (beeswax) - Alginates
[0187] Cellulose
[0188] pectin
[0189] Gelatin (currently not favored by the inventors due to questionable acid stability) Latex rubber / dandelion rubber
[0190] - PLA
[0191] - PHA / PHB
[0192] paste
[0193] - Silk
[0194] Combinations and embedding with and in other fibers (e.g., flaxseed, chia seeds, or similar) are also conceivable. Composites, such as PLA (thermoplastic) with cellulose (non-thermoplastic), are also conceivable to ensure optimized enteral passage and degradability.
[0195] Synthetic, biodegradable matrices
[0196] - PEG
[0197] - Ecoflex™ (BASF)
[0198] silicone
[0199] Liposome
[0200] The invention is explained in more detail below with reference to the drawing.
[0201] Fig.1 shows a schematic representation of a first drink and
[0202] Fig.2 shows a schematic representation of a second drink.
[0203] Fig.3 the results of a thermogravimetric analysis (TGA) of C02 absorber particles after an 18-hour intestinal passage
[0204] Fig.4 the results of a thermogravimetric analysis (TGA) of placebo particles after an 18-hour intestinal transit
[0205] Fig.5 the results of a thermogravimetric analysis (TGA) of C02 absorber particles before in vivo application
[0206] Fig. 6 shows a schematic view of a microsphere 1 in section with a polymer carrier matrix 3 containing Ca(OH)2 particles 2A, 2B as CO2 absorber particles. The first drink in Fig. 1 essentially consists of a suspension medium, for example, a low-viscosity liquid, a gel, or a viscous medium such as wax or syrup, with spheres embedded therein. One sphere is shown enlarged and partially sectioned.
[0207] The sphere contains a CO2 absorber in microparticles, which are encased in a shell in the form of a circular polymer matrix.
[0208] The second drink in Fig. 2 also essentially consists of a suspension medium. Unlike the first drink, the second drink should be more viscous than, for example, water. The suspension medium in the second drink is a viscous enveloping matrix in which the CO2 absorber is directly embedded in the form of microparticles.
[0209] Figure 3 shows the results of a thermogravimetric analysis (TGA) of CO2 absorber particles after 18 hours of intestinal transit, with weight loss plotted against heating temperature. The Ca(OH)2-containing microspheres with a low-density polyethylene (LDPE) carrier matrix exhibit an average CO2 content of 8.83 wt.% after intestinal transit (n=3).
[0210] Figure 4 shows the results of a thermogravimetric analysis (TGA) of placebo particles after an 18-hour intestinal transit, with weight loss plotted against heating temperature. The microspheres consisted only of the low-density polyethylene (LDPE) carrier matrix, thus containing no CO2 absorber particles. No CO2 could be detected for these placebo particles after intestinal transit.
[0211] Figure 5 shows the results of a thermogravimetric analysis (TGA) of CO2 absorber particles prior to in vivo application (oral administration with 18-hour intestinal transit), with weight loss plotted against heating temperature. The Ca(OH)2-containing microspheres with a low-density polyethylene (LDPE) carrier matrix exhibit a low CO2 content of 0.43 wt.% (n=3) prior to administration.
[0212] Figure 6 shows a microsphere 1 in perspective view and in partial section. It consists of a polymer carrier matrix 3 with Ca(OH)2 particles as CO2 absorber particles 2A, 2B, with the particles 2A either encased by the carrier matrix or exposed on the surface as partially enclosed particles 2B. List of reference symbols:
[0213] 1 microsphere
[0214] 2A Fully coated CO2 absorber particle
[0215] 2B C02 absorber particle exposed on the surface
[0216] 3 Polymer carrier matrix
[0217] Example 1: Direct measurement of the amount of CO2 absorbed in the gastrointestinal tract using TGA
[0218] Objectives and measurement methods:
[0219] This method quantitatively and directly detects the body's own CO2, which the CO2-absorbing microspheres in the intestine bind and remove from the organism. The actual measurement is performed on the particles recovered after intestinal passage using the thermogravimetric analysis (TGA) method. TGA measures particles that have undergone an 18-hour intestinal passage in animal experiments (German Landrace pigs, weight: approximately 60 kg).
[0220] Thermogravimetric analysis (TGA) is an analytical method that measures the mass change of a sample as a function of temperature and time. The sample is heated in a small crucible in a furnace at a defined heating rate to temperatures up to 1100 °C and decomposed until pyrolysis occurs. The crucible is coupled to a microbalance, which records the mass change during the heating process. Since the components react at a predefined temperature, the mass loss can be directly correlated with the mass fraction if the sample composition is known.
[0221] Overall, five stages of mass loss can be distinguished in microsphere samples under a nitrogen atmosphere: The first stage shows the loss of water. The second and third stages show the loss of organic compounds on the granules (fecal residues). The fourth stage shows the decomposition of the polymeric particle matrix, polyethylene (PE). In the fifth stage, the gas CO2 escapes from the calcium carbonate, which is formed after the body's own CO2 binds to the calcium hydroxide, according to the following reaction equation:
[0222] (i) in vivo CO2 elimination during intestinal transit:
[0223] Ca(OH)2+ C02CaCO3+ H20 (exothermic) (ii) in vitro CO2 release in thermogravimetric analysis (TGA):
[0224] CaCO3CaO + CO2(endothermic)
[0225] Thus, the mass fraction of bound CO2 can be precisely determined via the mass loss in the fifth stage (see Figures 3 to 5).
[0226] Results:
[0227] The test animals were administered a dispersion containing microspheres containing CO2 absorbers. The microspheres contained Ca(OH)2 particles as CO2 absorbers embedded in a low-density polyethylene (LDPE) carrier matrix. As shown in Figure 3, these particles exhibited an average CO2 content of 8.83 wt.% after intestinal passage in the pig (n=3).
[0228] Compared to the administration of the CO2 absorber-containing microspheres in animal experiments, the placebo sample (geometrically identical PE particles without CO2 absorber) showed no CO2 release in the TGA (see Figure 4).
[0229] In the initial sample of the CO2 absorber-containing microspheres (before oral administration), a small amount of CO2 was detected, which was subtracted as a “blank value” from the calculated amount of CO2 absorbed in the intestine (see Figure 5).
[0230] The embodiments shown here are merely examples of the present invention and should therefore not be considered limiting. Alternative embodiments contemplated by those skilled in the art are equally encompassed within the scope of the present invention.
Claims
Patent claims:
1. Use of a C0 2 -absorbing formulation for the preparation of an ergogenic food supplement, in particular for the preparation of a formulation for the preparation of an ergogenic food supplement.
2. Use according to claim 1, characterized in that the CO 2 - absorbing formulation a C0 2 absorber embedded in a carrier matrix or surrounded by a shell.
3. Use according to claim 2, characterized in that the carrier matrix or the shell has a selective permeability for the CO 2 compared to CO 2 - absorber, wherein the selective permeability is at least during the passage of the coated C0 2 -absorber through the gastrointestinal tract persists and / or the carrier matrix or the shell prevents the release of CO 2- absorber in v / vo application is essentially prevented.
4. Use according to claim 2 or 3, characterized in that the carrier matrix comprises a binder which is preferably biodegradable and is particularly preferably selected from the group comprising beeswax, paraffin, cellulose, derivatized cellulose, pectin, gelatin, alginate, agarose, latex rubber, dandelion rubber, polyhydroxyalkanoate (PHA), polylactide (PLA) and fibroin, or a combination thereof.
5. Use according to one of claims 2 to 4, characterized in that the C0 2 -Absorber in combination with the carrier matrix forms a composite material which preferably also contains fiber and / or minerals.
6. Use according to one of claims 2 to 5, characterized in that in the C0 2 -absorbing formulation of the C0 2 absorber is contained in a flowable carrier matrix, whereby the C02 -Absorber preferentially forms a gel with the carrier matrix.
7. Use according to claim 2 or 3, characterized in that the CO 2 - absorbent formulation as a coated formulation has the following: (i) An envelope consisting of a wall material, the envelope being permeable to CO 2 and optionally also for water vapor; (ii) and a core area containing at least one C0 2 absorber, wherein the shell preferably allows the release of the C0 2 -absorber during in vivo application.
8. Use according to one of claims 2 to 7, characterized in that the carrier matrix or the shell is impermeable to water and preferably impermeable to the C0 2 -absorber and its reaction products.
9. Use according to claim 7 or 8, characterized in that the coated active ingredient formulation is selected from the group consisting of: • Liquid core containing the C0 2 -Absorber with a membrane shell to form a liposome or niosome; • Solid core containing the C0 2 -Absorber with a single-layer shell; • Solid core containing the C0 2 -Absorber with a multi-layer shell; • Microcapsule.
10. Use according to claim 9, characterized in that the microcapsule is a microsphere in which the C0 2 -Absorber is incorporated in solid dispersed form or in dissolved form into a polymeric carrier matrix.
11. Use according to one of claims 2 to 10, characterized in that the shell or the carrier matrix, which is preferably the carrier matrix of a microsphere, comprises a CO 2 -Permeability from 0.004 to 2,500 x 10 13 cm 3 cm cnr 2 Pa s -1 , preferably from 5 to 500 x 10 13 cm 3 cm cnr 2 Pa s -1and particularly preferably from 10 to 300 x 10 13 cm 3 cm cnr 2 Pa 1 s -1 has.
12. Use according to one of claims 2 to 11, characterized in that the shell, or the carrier matrix, which is preferably the carrier matrix of a microsphere, has a water vapor permeability of 0.009 to 32,000 x 10 13 cm 3 cm cnr 2 Pa s -1 , and preferably from 100 to 1500 x 10 13 cm 3 cm cnr 2 Pa s -1 has.
13. Use according to one of claims 2 to 12, characterized in that the shell or the carrier matrix, which is preferably the carrier matrix of a microsphere, has a mass fraction of 10 to 95 wt.%, preferably of 40 to 60 wt.% and particularly preferably of 55 to 65 wt.%, based on the weight of the coated active ingredient formulation.
14. Use according to one of claims 2 to 13, characterized in that the shell or the carrier matrix has an average layer thickness of 10 to 500 pm, preferably of 50 to 250 pm and particularly preferably of 100 to 200 pm.
15. Use according to one of claims 2 to 14, characterized in that the wall material of the shell is selected from the group consisting of poly(organo)siloxane; polyolefin; polyester; polybutylene succinate; polybutylene adipate terephthalate (PBAT); thermoplastic polyurethane (TPU), polyethylene such as high-density polyethylene (HDPE) or low-density polyethylene (LDPE); polylactide (PLA), polyhydroxyacetic acid (PGA) and poly(lactide-co-glycolide) (PLGA); lipids such as fatty acids or phospholipids, and is preferably a polyester.
16. Use according to one of claims 2 to 15, characterized in that the C0 2-Absorber selected from the group consisting of inorganic hydroxide compound, lithium peroxide and mixtures thereof, wherein lithium hydroxide, sodium hydroxide, potassium hydroxide, calcium hydroxide and magnesium hydroxide and mixtures thereof.
17. Use according to claim 16, characterized in that the CO 2 - absorbent material comprises calcium hydroxide and optionally an effective amount of a hygroscopic or deliquescent humectant capable of absorbing carbon dioxide, wherein the calcium hydroxide is substantially free of sodium and potassium hydroxide.
18. Use according to one of claims 2 to 17, characterized in that the C0 2 -Absorber a CO 2 -Absorption capacity of more than 10 mg CO 2 / g active ingredient formulation, preferably more than 40 mg CO 2 / g active ingredient formulation, particularly preferably more than 50 mg CO 2 / g active ingredient formulation, and in particular more than 100 mg CO 2 / g active ingredient formulation.
19. Use according to one of the preceding claims, characterized in that the ergogenic food supplement is selected from the group consisting of bar, gummy candy, dragee, tablet, granulate, powder, capsule, gel, syrup or drink.
20. Use according to claim 19, characterized in that the food supplement in the form of a beverage is an energy drink or a sports drink.
21. Use according to claim 20, characterized in that the energy drink or sports drink comprises one or more of the following substances: caffeine, creatine, beta-hydroxy-beta-methylbutyrate (HMB), carnitine, coenzyme Q10, inositol, glucuronolactone, taurine, branched-chain amino acids (BCAA), glucose, sweeteners.
22. Use according to claim 21, characterized in that the energy drink contains 0.05 to 50 g taurine / I, 0.1 to 10 g glucuronolactone / I, 0.1 to 1 g caffeine / I, 1 to 50 g glucose / I, 10 to 150 g sucrose / I and 20 to 500 mg inositol / I.
23. Use according to claims 20 to 22, characterized in that the drink, especially energy drink or sports drink, contains 20 to 70% calcium hydroxide and / or 20 to 70% magnesium hydroxide.
24. Ergogenic food supplement, in particular drink, especially energy drink or sports drink, having a CO 2 absorbent formulation, especially a C0 2 -Absorber used according to one of claims 1 to 23.
25. Use of the dietary supplement according to claim 24 for optimizing acid-base balance by acid elimination after oral administration.
26. Use of the dietary supplement according to claim 24 for reducing the work of breathing after oral administration.
27. Use of the dietary supplement according to claim 24 for increasing alertness or attention after oral administration.
28. Use of the dietary supplement according to claim 24 for detoxifying the body after oral administration.
Citation Information
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