WO2004095942A2 - Caffeinated tablet - Google Patents
Caffeinated tablet Download PDFInfo
- Publication number
- WO2004095942A2 WO2004095942A2 PCT/DE2004/000843 DE2004000843W WO2004095942A2 WO 2004095942 A2 WO2004095942 A2 WO 2004095942A2 DE 2004000843 W DE2004000843 W DE 2004000843W WO 2004095942 A2 WO2004095942 A2 WO 2004095942A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- mass
- tablet according
- caffeine
- tablet
- isomalt
- Prior art date
Links
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 claims abstract description 82
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 claims abstract description 41
- 229960001948 caffeine Drugs 0.000 claims abstract description 41
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 claims abstract description 41
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims abstract description 15
- 239000000905 isomalt Substances 0.000 claims abstract description 15
- 235000010439 isomalt Nutrition 0.000 claims abstract description 15
- HPIGCVXMBGOWTF-UHFFFAOYSA-N isomaltol Natural products CC(=O)C=1OC=CC=1O HPIGCVXMBGOWTF-UHFFFAOYSA-N 0.000 claims abstract description 15
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims abstract description 15
- 239000000811 xylitol Substances 0.000 claims abstract description 15
- 235000010447 xylitol Nutrition 0.000 claims abstract description 15
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims abstract description 15
- 229960002675 xylitol Drugs 0.000 claims abstract description 15
- SERLAGPUMNYUCK-DCUALPFSSA-N 1-O-alpha-D-glucopyranosyl-D-mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O SERLAGPUMNYUCK-DCUALPFSSA-N 0.000 claims abstract description 11
- 239000000203 mixture Substances 0.000 claims abstract description 11
- 239000011230 binding agent Substances 0.000 claims abstract description 9
- 239000000796 flavoring agent Substances 0.000 claims abstract description 8
- 235000019634 flavors Nutrition 0.000 claims abstract 4
- 230000001681 protective effect Effects 0.000 claims description 23
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 18
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 12
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 8
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims description 6
- 235000017557 sodium bicarbonate Nutrition 0.000 claims description 6
- 239000000126 substance Substances 0.000 claims description 6
- 239000000843 powder Substances 0.000 claims description 5
- 235000013355 food flavoring agent Nutrition 0.000 claims description 4
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 4
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 4
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 4
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 4
- 235000019359 magnesium stearate Nutrition 0.000 claims description 4
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 3
- 235000021355 Stearic acid Nutrition 0.000 claims description 3
- 239000004203 carnauba wax Substances 0.000 claims description 3
- 235000013869 carnauba wax Nutrition 0.000 claims description 3
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 3
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 3
- 239000002245 particle Substances 0.000 claims description 3
- 239000008117 stearic acid Substances 0.000 claims description 3
- 239000001993 wax Substances 0.000 claims description 3
- 239000001913 cellulose Substances 0.000 claims description 2
- 229920002678 cellulose Polymers 0.000 claims description 2
- 230000000979 retarding effect Effects 0.000 claims 3
- 230000009931 harmful effect Effects 0.000 abstract 1
- 239000003826 tablet Substances 0.000 description 17
- 230000000694 effects Effects 0.000 description 6
- 239000007938 effervescent tablet Substances 0.000 description 5
- SERLAGPUMNYUCK-YJOKQAJESA-N 6-O-alpha-D-glucopyranosyl-D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O SERLAGPUMNYUCK-YJOKQAJESA-N 0.000 description 4
- 210000001035 gastrointestinal tract Anatomy 0.000 description 3
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
- 238000007792 addition Methods 0.000 description 2
- 235000013361 beverage Nutrition 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 230000007774 longterm Effects 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 229920001800 Shellac Polymers 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000001569 carbon dioxide Substances 0.000 description 1
- 229910002092 carbon dioxide Inorganic materials 0.000 description 1
- 230000001055 chewing effect Effects 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 235000020965 cold beverage Nutrition 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 230000006735 deficit Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 239000007789 gas Substances 0.000 description 1
- 230000008821 health effect Effects 0.000 description 1
- 235000012171 hot beverage Nutrition 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- 239000004208 shellac Substances 0.000 description 1
- 235000013874 shellac Nutrition 0.000 description 1
- ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 description 1
- 229940113147 shellac Drugs 0.000 description 1
- 230000004936 stimulating effect Effects 0.000 description 1
- 235000019605 sweet taste sensations Nutrition 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L2/00—Non-alcoholic beverages; Dry compositions or concentrates therefor; Their preparation
- A23L2/385—Concentrates of non-alcoholic beverages
- A23L2/39—Dry compositions
- A23L2/395—Dry compositions in a particular shape or form
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L2/00—Non-alcoholic beverages; Dry compositions or concentrates therefor; Their preparation
- A23L2/40—Effervescence-generating compositions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0007—Effervescent
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
- A23V2002/00—Food compositions, function of food ingredients or processes for food or foodstuffs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
- A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
Definitions
- the invention relates to a caffeine-containing tablet with which caffeine is made available for oral ingestion.
- caffeine is usually taken in the form of cold and hot drinks, possibly with the addition of other substances that influence the taste of the drinks.
- the caffeine-containing tablets according to the invention are composed in such a way that, in addition to the powdered caffeine, isomalt and xylitol, which form the largest proportion of the composition (a minimum mass fraction of 50%), additionally an aroma substance or an aroma substance mixture and with a low one Share a binder are included.
- Such a tablet should not contain more than a total of 150 mg, preferably not more than 100 mg, particularly preferably 50 mg of caffeine.
- At least 20% by mass, preferably approximately 50% by mass, of the powdered caffeine should be enclosed with such a protective cover.
- This effect can be spread out over time if individual powder particles are coated with caffeine with protective casings of different thicknesses or if different substances are used to form protective casings, which can preferably be solved differently in the digestive tract.
- Caffeine can also be influenced in such a way that it only occurs in the digestive tract. This can also be achieved with different protective covers, stretched in time and differentiated in time in the digestive tract, so that an extended total active time can be achieved. Stearic acid has proven to be preferred for the formation of such protective shells on caffeine powder particles.
- a cellulose derivative or shellac can also be used to form the protective cover.
- the protective covers can also be formed from a natural wax, preferably carnauba wax.
- the substances already mentioned as constituents of tablets according to the invention namely isomalt and xylitol, not only essentially form the carrier matrix of such tablets, but also ensure a pleasant, sweet taste, even though no sugar is used.
- Xylitol also has a beneficial plaque removal effect.
- Tablets consisting of at least 60% by mass up to 90% by mass of isomalt and xylotol can simply be swallowed, sucked in the mouth or chewed.
- Tablets containing sodium bicarbonate should also contain citric acid in addition to the flavorings already mentioned to improve the taste and release of gases in order to achieve a refreshing taste improvement.
- citric acid should shot to achieve a sufficient release of carbon dioxide.
- the soluble effervescent tablets containing sodium bicarbonate show a comparison to beverages
- Such effervescent tablets should preferably be enclosed individually, if appropriate several, together after manufacture for the transport and storage period by a gas-tight film. The inclusion is intended to ensure the smallest possible volume of air inside and prevent the ingress of moisture.
- the tablets according to the invention can be produced in such a way that caffeine powder, isomalt and xylitol are mixed with one another and a suitable binder is added.
- the binder comes, for example, as an inert binder, e.g. Hydroxypropylmethylcellulose in question, where the binder content can be about 1 to 10% by mass.
- An encapsulated flavoring or a flavoring mixture can already be contained, but can also be added later.
- This mixture is then granulated, which can be done in a fluidized bed system, but also in other suitable mixing devices.
- the granules thus obtained are then dried until a residual moisture content of 1 to 5%, preferably up to 2%, % has been obtained.
- the granulate prepared in this way can be screened off in order to ensure a relatively uniform grain size distribution.
- a solid tablet for sucking or chewing can contain 20 to 35 mass% caffeine, in which a ratio of approx. 2 to 3 is advantageous for pure caffeine powder provided with a protective cover, 60 to 80 mass% isomalt and xylitol , 1.5 to 5% by mass of aroma or aroma mixture as well as hydroxypropylmethyl cellulose (approx. 3-5% by mass) and magnesium stearate (approx. 0.3 to 1% by mass) and possibly small proportions of a colorant.
- the protective covers for caffeine should consist of carnauba wax.
- Such a tablet can then contain 119 mg of isomalt, 116 mg of xylitol, 9 mg of flavoring, 39.7 mg of pure caffeine, 59.5 mg of caffeine coated with canauba wax, 4.4 mg of hydroxypropylmethyl cellulose, 2 mg of magnesium stearate and contain less than 1 mg of a dye.
- a 2 g tablet can contain 1000 mg isomalt, 900 mg xylitol, 50 mg caffeine, 25 mg of which in pure form and 25 mg with a stearic acid coating, and 20 mg of flavoring.
- a "effervescent tablet” that dissolves easily in water can have the same total mass of 2g, 700 mg isomalt, 700 mg xylitol, 250 mg sodium bicarbonate, 250 mg citric acid, 50 mg caffeine, which in turn can be partially surrounded by a protective cover and 20 mg of a flavoring.
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Nutrition Science (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Zoology (AREA)
- Physiology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention relates to caffeinated tablets that can be administered orally, that are characterized by an improved taste and that are at least substantially devoid of undesired harmful effects. The caffeinated tablets according to the invention contain, in addition to pulverized caffeine, isomalt and xylitol in approximately equal percentages and constituting the major portion, a flavor or a flavor mixture and a binder.
Description
Coffein enthaltende TabletteTablet containing caffeine
Die Erfindung betrifft eine Coffein enthaltende Tablette, mit der Coffein für die orale Aufnahme zur Verfügung gestellt wird. Dabei soll die anregendeThe invention relates to a caffeine-containing tablet with which caffeine is made available for oral ingestion. The stimulating
Wirkung von Coffein neben weiteren positiven mit der Erfindung erreichbaren Effekten gesichert werden.Effect of caffeine in addition to other positive effects that can be achieved with the invention.
So wird Coffein üblicherweise in Form von Kalt- und Heißgetränken, gegebenenfalls unter Zugabe weiterer den Geschmack der Getränke beeinflussenden Stoffen aufgenommen.For example, caffeine is usually taken in the form of cold and hot drinks, possibly with the addition of other substances that influence the taste of the drinks.
Es sind auch ansatzweise Coffein enthaltende Tablet- ten bekannt, die in fester, aber auch gelöster Form oral appliziert werden können.There are also some known tablets containing caffeine, which can be administered orally in solid but also in dissolved form.
Bei den bekannten Lösungen treten häufig aber auch geschmackliche Defizite auf, die dann nur über stark
erhöhte Zugaben von Zucker mit den bekannten unerwünschten Nebenwirkungen, teilweise kompensiert werden können.In the known solutions, however, there are also taste deficits, which are then only severe Increased additions of sugar with the known undesirable side effects, can be partially compensated.
Außerdem ist ein häufig gewünschter Langzeiteffekt nicht erreichbar und es wird außerdem Coffein in Ü- berdosen appliziert, die dann gegebenenfalls keine oder eine unerwünschte Wirkung auf einen menschlichen Organismus erreichen.In addition, a frequently desired long-term effect cannot be achieved and, in addition, caffeine is applied in overdoses, which may then have no or an undesirable effect on a human organism.
Es ist daher Aufgabe der Erfindung eine Möglichkeit zur oralen Applikation von Coffein vorzuschlagen, die einen verbesserten Geschmack erreicht und mindestens nahezu frei von unerwünschten gesundheitsschädlichen Wirkungen ist.It is therefore the object of the invention to propose a possibility for the oral application of caffeine which achieves an improved taste and is at least almost free of undesirable health effects.
Erfindungsgemäß wird diese Aufgabe mit einer Tablette, deren Konsistenz mit dem Patentanspruch 1 definiert ist, gelöst. Vorteilhafte Ausgestaltungsformen und Weiterbildungen der Erfindung können mit den in den untergeordneten Ansprüchen bezeichneten Merkmalen erreicht werden.According to the invention, this object is achieved with a tablet, the consistency of which is defined in claim 1. Advantageous refinements and developments of the invention can be achieved with the features specified in the subordinate claims.
Die erfindungsgemäßen Coffein enthaltenden Tabletten sind dabei so zusammengesetzt, dass neben dem pulver- förmigen Coffein auch Isomalt und Xylitol, die den größten Anteil an der Zusammensetzung bilden (einen Mindestmasseanteil von 50%) , zusätzlich ein Aromastoff oder ein Aromastoffgemisch und mit einem gerin- gen Anteil ein Binder enthalten sind.The caffeine-containing tablets according to the invention are composed in such a way that, in addition to the powdered caffeine, isomalt and xylitol, which form the largest proportion of the composition (a minimum mass fraction of 50%), additionally an aroma substance or an aroma substance mixture and with a low one Share a binder are included.
In einer solchen Tablette sollten nicht mehr als insgesamt 150 mg, bevorzugt nicht mehr als 100 mg, besonders bevorzugt 50 mg Coffein enthalten sein.Such a tablet should not contain more than a total of 150 mg, preferably not more than 100 mg, particularly preferably 50 mg of caffeine.
Vorteilhaft ist es, zumindest einen Teil des in einer
Tablette enthaltenden Coffeins mit einer retardierend wirkenden Schutzhülle zu umschließen. Mit einer solchen Schutzhülle kann erreicht werden, dass Coffein mit einem bestimmten Zeitverzug freigesetzt und vom jeweiligen Organismus aufgenommen wird. So kann ein Langzeitwirkeffekt erzielt werden.It is advantageous to have at least part of the in one Enclose tablet-containing caffeine with a retardant protective cover. With such a protective cover it can be achieved that caffeine is released with a certain time delay and is absorbed by the respective organism. In this way a long-term effect can be achieved.
Es sollten möglichst mindestens 20 Masse- %, bevorzugt ca. 50 Masse-% des pulverförmigen Coffeins mit einer solchen Schutzhülle umschlossen sein.If possible, at least 20% by mass, preferably approximately 50% by mass, of the powdered caffeine should be enclosed with such a protective cover.
So kann das nicht umhüllte Coffein nahezu unmittelbar nach der oralen Aufnahme freigesetzt werden und seine belebende Wirkung hervorrufen. Wohingegen der Anteil, der eine Umhüllung aufweist, nachfolgend zeitversetzt freigegeben und beim Stoffwechsel umgesetzt werden kann.This means that the uncoated caffeine can be released almost immediately after oral intake and have an invigorating effect. In contrast, the portion that has a covering can subsequently be released with a time lag and implemented in the metabolism.
Dieser Effekt kann zeitlich noch gespreizt werden, wenn einzelne Pulverpartikel mit Coffein mit unterschiedlich dicken Schutzhüllen überzogen oder verschiedene Stoffe für die Ausbildung von Schutzhüllen, die bevorzugt im Verdauungstrakt unterschiedlich lösbar sind, eingesetzt werden.This effect can be spread out over time if individual powder particles are coated with caffeine with protective casings of different thicknesses or if different substances are used to form protective casings, which can preferably be solved differently in the digestive tract.
Es besteht aber auch die Möglichkeit das gesamte pul- verförmige Coffein mit Schutzhüllen zu umschließen. So kann eine geschmackliche Beeinflussung durch das Coffein bei der oralen Applikation vermieden zumin- dest jedoch reduziert werden. Die Freisetzung desHowever, there is also the option of enclosing the entire powdered caffeine with protective covers. In this way, taste influence by the caffeine during oral administration can be avoided or at least reduced. The release of the
Coffeins kann so auch beeinflusst werden, dass diese erst im Verdauungstrakt erfolgt . Dies kann auch mit unterschiedlichen Schutzhüllen zeitlich gestreckt und zeitlich differenziert im Verdauungstrakt erreicht werden, so dass eine verlängerte Gesamtwirkzeit erzielbar ist.
Als bevorzugt hat sich Stearinsäure für die Ausbildung solcher Schutzhüllen auf Coffeinpulverpartikeln herausgestellt .Caffeine can also be influenced in such a way that it only occurs in the digestive tract. This can also be achieved with different protective covers, stretched in time and differentiated in time in the digestive tract, so that an extended total active time can be achieved. Stearic acid has proven to be preferred for the formation of such protective shells on caffeine powder particles.
Es können aber auch ein Zellulosederivat oder Schellack für die Schutzhüllenbildung eingesetzt werden.However, a cellulose derivative or shellac can also be used to form the protective cover.
Die Schutzhüllen können aber auch aus einem natürli- chen Wachs, bevorzugt Carnaubawachs gebildet sein.The protective covers can also be formed from a natural wax, preferably carnauba wax.
Die bereits als Bestandteile von erfindungsgemäßen Tabletten erwähnten Stoffe, nämlich Isomalt und Xylitol bilden nicht nur im Wesentlichen die Trägermatrix von solchen Tabletten, sondern sichern auch eine angenehme süßliche Geschmacksnote, obwohl keinerlei Zucker eingesetzt wird. Xylitol hat außerdem eine vorteilhafte Zahnbelag entfernende Wirkung.The substances already mentioned as constituents of tablets according to the invention, namely isomalt and xylitol, not only essentially form the carrier matrix of such tablets, but also ensure a pleasant, sweet taste, even though no sugar is used. Xylitol also has a beneficial plaque removal effect.
Tabletten, die aus mindestens 60 Masse-% bis hin zu 90 Masse-% Isomalt und Xylotol bestehen, können einfach verschluckt, im Mund gelutscht oder zerkaut zu sich genommen werden.Tablets consisting of at least 60% by mass up to 90% by mass of isomalt and xylotol can simply be swallowed, sucked in the mouth or chewed.
Es besteht aber auch die Möglichkeit, mittels in einer Tablette enthaltenem Natriumbikarbonat eine so genannte Brausetablette zur Verfügung zu stellen, die in Wasser einfach gelöst und dann die Lösung als Getränk appliziert werden kann.However, there is also the possibility of providing a so-called effervescent tablet by means of sodium bicarbonate contained in a tablet, which is simply dissolved in water and the solution can then be applied as a drink.
Natriumbikarbonat enthaltende Tabletten sollten zur Geschmacksverbesserung und Freisetzung von Gasen außerdem neben den bereits erwähnten Aromastoffen, zusätzlich Zitronensäure enthalten, um eine erfrischen- de Geschmacksverbesserung zu realisieren. Zitronensäure sollte in Bezug Zum Natriumbikarbonat im Über-
schuss enthalten sein, um eine ausreichende Freisetzung von Kohlendioxid zu erreichen.Tablets containing sodium bicarbonate should also contain citric acid in addition to the flavorings already mentioned to improve the taste and release of gases in order to achieve a refreshing taste improvement. In relation to sodium bicarbonate, citric acid should shot to achieve a sufficient release of carbon dioxide.
Insbesondere die löslichen Natriumbikarbonat enthal- tenden Brausetabletten weisen gegenüber GetränkenIn particular, the soluble effervescent tablets containing sodium bicarbonate show a comparison to beverages
Vorteile bezüglich der Handhabbarkeit, bei Transport und Lagerung auf. So die erforderlichen Verpackungen nicht nur kostengünstiger, sondern bereiten auch deutlich weniger Aufwand, als dies bei Behältnissen, in denen Coffein enthaltende Getränke für den Genuss zur Verfügung gestellt werden.Advantages in terms of manageability, transportation and storage. This means that the required packaging is not only less expensive, but also involves significantly less effort than in containers in which caffeine-containing beverages are made available for enjoyment.
Solche Brausetabletten sollten bevorzugt einzeln gegebenenfalls auch mehrere gemeinsam nach der Herstel- lung für den Transport- und Lagerungszeitraum von einer gasdichten Folie eingeschlossen sein. Der Ein- schluss soll ein möglichst geringes Luftvolumen im Inneren sichern und ein Eindringen von Feuchtigkeit verhindern.Such effervescent tablets should preferably be enclosed individually, if appropriate several, together after manufacture for the transport and storage period by a gas-tight film. The inclusion is intended to ensure the smallest possible volume of air inside and prevent the ingress of moisture.
Die erfindungsgemäßen Tabletten können so hergestellt werden, dass Coffeinpulver, Isomalt und Xylitol miteinander vermischt und ein geeigneter Binder zugegeben wird. Als Binder kommt beispielsweise als inertes Bindemittel z.B. Hydroxypropylmethylcellulose in Frage, wobei der Binderanteil ca. 1 bis hin zu 10 Masse- % betragen kann. Ein verkapselter Aromastoff oder ein Aromastoffgemisch kann bereits enthalten sein, aber auch erst später zugegeben werden.The tablets according to the invention can be produced in such a way that caffeine powder, isomalt and xylitol are mixed with one another and a suitable binder is added. The binder comes, for example, as an inert binder, e.g. Hydroxypropylmethylcellulose in question, where the binder content can be about 1 to 10% by mass. An encapsulated flavoring or a flavoring mixture can already be contained, but can also be added later.
Dieses Gemisch wird dann granuliert, was in einer Wirbelschichtanlage, aber auch in anderen geeigneten Mischvorrichtungen erfolgen kann.This mixture is then granulated, which can be done in a fluidized bed system, but also in other suitable mixing devices.
Das so erhaltene Granulat wird dann getrocknet, bis eine Restfeuchte von 1 bis 5 %, bevorzugt bis 2 Mas-
se-% erhalten worden ist.The granules thus obtained are then dried until a residual moisture content of 1 to 5%, preferably up to 2%, % has been obtained.
Gegebenenfalls können das so vorbereitete Granulat abgesiebt werden, um eine relativ gleichmäßige Korn- größenverteilung zu sichern.If necessary, the granulate prepared in this way can be screened off in order to ensure a relatively uniform grain size distribution.
Durch Zugabe von ca. 0,5 Masse-% Magnesiumstearat und ca. 1 Masse-% eines Aromastoffes oder Aromastoffgemi- sches wird die zu der Tablette verpressbare Endkon- sistenz eingestellt und die jeweils gewünschte Geschmacksnote beeinflusst .By adding approx. 0.5% by mass of magnesium stearate and approx. 1% by mass of a flavoring agent or flavoring agent mixture, the final consistency that can be compressed into the tablet is adjusted and the desired taste note is influenced.
Sollen Natriumbikarbonat enthaltende Brausetabletten hergestellt werden, reduzieren sich der Anteil an Isomalt und Xylitol und werden durch ca. 12,5 Masse-% Natriumbikarbonat und ca. 12,5 Masse-% Zitronensäure ersetzt .If effervescent tablets containing sodium bicarbonate are to be produced, the proportion of isomalt and xylitol is reduced and are replaced by approximately 12.5% by weight sodium bicarbonate and approximately 12.5% by weight citric acid.
Im Übrigen erfolgt die Herstellung wie bereits vorab beschrieben.Otherwise, the production takes place as already described in advance.
Eine feste Tablette zum Lutschen oder Kauen kann 20 bis 35 Masse-% Coffein, bei dem ein Verhältnis von ca. 2 zu 3 für reines und mit einer Schutzhülle ver- sehenes Coffeinpulver vorteilhaft ist, 60 bis 80 Mas- se-% Isomalt und Xylitol, 1,5 bis 5 Masse-% Aromaoder Aromastoffgemiseh sowie Hydroxypropylmethylcel- luse (ca. 3-5 Masse-%) und Magnesiumstearat (ca. 0,3 bis 1 Masse-%) und ggf. geringe Anteile eines Farb- Stoffes enthalten. Die Schutzhüllen für Coffein sollten aus Carnaubawachs bestehen.A solid tablet for sucking or chewing can contain 20 to 35 mass% caffeine, in which a ratio of approx. 2 to 3 is advantageous for pure caffeine powder provided with a protective cover, 60 to 80 mass% isomalt and xylitol , 1.5 to 5% by mass of aroma or aroma mixture as well as hydroxypropylmethyl cellulose (approx. 3-5% by mass) and magnesium stearate (approx. 0.3 to 1% by mass) and possibly small proportions of a colorant. The protective covers for caffeine should consist of carnauba wax.
Eine solche Tablette kann dann 119 mg Isomalt, 116 mg Xylitol, 9 mg Aromastoff, 39,7 mg reines Coffein, 59,5 mg mit Canaubawachs umhülltes Coffein, 4,4 mg Hydroxypropylmethylcellulose, 2 mg Magnesiumstearat
und weniger als 1 mg eines Farbstoffes enthalten.Such a tablet can then contain 119 mg of isomalt, 116 mg of xylitol, 9 mg of flavoring, 39.7 mg of pure caffeine, 59.5 mg of caffeine coated with canauba wax, 4.4 mg of hydroxypropylmethyl cellulose, 2 mg of magnesium stearate and contain less than 1 mg of a dye.
So kann eine 2g Tablette 1000 mg Isomalt, 900 mg Xylitol, 50 mg Coffein, von dem 25 mg in reiner Form und 25 mg mit einer Stearinsäureumhüllung versehen sind, sowie 20 mg Aromastoff enthalten.A 2 g tablet can contain 1000 mg isomalt, 900 mg xylitol, 50 mg caffeine, 25 mg of which in pure form and 25 mg with a stearic acid coating, and 20 mg of flavoring.
Eine sich leicht in Wasser lösende "Brausetablette" kann bei der gleichen Gesamtmasse von 2g, 700 mg Iso- malt, 700 mg Xylitol, 250 mg Natriumbikarbonat, 250 mg Zitronensäure, 50 mg Coffein, das wiederum teilweise mit einer Schutzhülle umgeben sein kann und 20 mg eines Aromastoffes enthalten.
A "effervescent tablet" that dissolves easily in water can have the same total mass of 2g, 700 mg isomalt, 700 mg xylitol, 250 mg sodium bicarbonate, 250 mg citric acid, 50 mg caffeine, which in turn can be partially surrounded by a protective cover and 20 mg of a flavoring.
Claims
1. Coffein enthaltende Tablette, die neben pulver- förmigem Coffein,1. tablet containing caffeine which, in addition to powdered caffeine,
zu annähernd gleichen Anteilen Isomalt und Xylitol, die den größten Anteil bilden,in approximately equal proportions, the largest proportion of isomalt and xylitol,
einen Aromastoff oder ein Aromastoffgemisch und einen Binder enthält.contains a flavoring or a flavoring mixture and a binder.
2. Tablette nach Anspruch 1, dadurch gekennzeichnet, dass maximal 100 mg Coffein enthalten sind.2. Tablet according to claim 1, characterized in that a maximum of 100 mg of caffeine are contained.
3. Tablette nach Anspruch 1 oder 2, dadurch gekennzeichnet, dass ein Teil des pul- verfδrmigen Coffeins mit einer retardierend wirkenden Schutzhülle umschlossen ist.3. Tablet according to claim 1 or 2, characterized in that a part of the powdered caffeine is enclosed with a retarding protective cover.
4. Tablette nach Anspruch 1 oder 2, dadurch gekennzeichnet, dass das gesamte pulver- förmige Coffein mit retardierend wirkenden4. Tablet according to claim 1 or 2, characterized in that the entire powdered caffeine with a retarding effect
Schutzhüllen umschlossen ist.Protective covers is enclosed.
5. Tablette nach Anspruch 3, dadurch gekennzeichnet, dass mindestens 20 Mas- se-% des pulverförmigen Coffeins von einer Schutzhülle umschlossen sind.5. Tablet according to claim 3, characterized in that at least 20 mass% of the powdered caffeine are enclosed by a protective cover.
6. Tablette nach Anspruch 3 oder 4, dadurch gekennzeichnet, dass 50 Masse-% des pul- verförmigen Coffeins von einer Schutzhülle umschlossen sind.6. Tablet according to claim 3 or 4, characterized in that 50% by mass of the powdered caffeine are enclosed by a protective cover.
7. Tablette nach einem der Ansprüche 3 bis 6, dadurch gekennzeichnet, dass die Schützhüllen aus Stearinsäure gebildet sind. 7. Tablet according to one of claims 3 to 6, characterized in that the protective sleeves are formed from stearic acid.
8. Tablette nach einem der Ansprüche 3 bis 6, dadurch gekennzeichnet, dass die Schutzhüllen aus einem Zellulosederivat gebildet sind.8. Tablet according to one of claims 3 to 6, characterized in that the protective covers are formed from a cellulose derivative.
9. Tablette nach einem der Ansprüche 3 bis 6, da- durch gekennzeichnet, dass die Schutzhüllen aus einem natürlichen Wachs gebildet sind.9. Tablet according to one of claims 3 to 6, characterized in that the protective covers are formed from a natural wax.
10. Tablette nach Anspruch 9, dadurch gekennzeichnet, dass die Schutzhüllen aus Carnaubawachs gebildet sind.10. Tablet according to claim 9, characterized in that the protective covers are formed from carnauba wax.
11. Tablette nach einem der vorhergehenden Ansprüche, dadurch gekennzeichnet, dass die Schutzhüllen von Coffeinpulverpartikeln unterschiedliche Dicken aufweisen oder die Schutzhüllen aus zeitlich unterschiedlich retardierenden Stoffen ge- bildet sind.11. Tablet according to one of the preceding claims, characterized in that the protective sleeves of caffeine powder particles have different thicknesses or the protective sleeves are formed from differently retarding substances.
12. Tablette nach einem der vorhergehenden Ansprüche, dadurch gekennzeichnet, dass der Anteil von Isomalt und Xylitol oberhalb 50 Masse-% gehalten ist.12. Tablet according to one of the preceding claims, characterized in that the proportion of isomalt and xylitol is kept above 50% by mass.
13. Tablette nach einem der vorhergehenden Ansprüche, dadurch gekennzeichnet, dass zusätzlich Natriumbikarbonat enthalten ist.13. Tablet according to one of the preceding claims, characterized in that sodium bicarbonate is additionally contained.
14. Tablette nach Anspruch 9, dadurch gekennzeichnet, dass die Tablette (n) temporär von einer gasdichten Folie eingeschlossen ist/sind.14. Tablet according to claim 9, characterized in that the tablet (s) is / are temporarily enclosed by a gas-tight film.
15. Tablette nach einem der vorhergehenden Ansprüche, dadurch gekennzeichnet, dass zusätzlich Zitronensäure enthalten ist .15. Tablet according to one of the preceding claims, characterized in that citric acid is additionally contained.
16. Tablette nach einem der vorhergehenden Ansprüche, dadurch gekennzeichnet, dass 50 mg Coffein, mindestens 90 Masse-% Isomalt und Xylitol,16. Tablet according to one of the preceding claims, characterized in that 50 mg of caffeine, at least 90% by mass of isomalt and xylitol,
1 Masse-% Aromastoff oder Aromastoffgemisch und 0,5 Masse-% Binder enthalten sind.1 mass% flavoring or flavoring mixture and 0.5 mass% binder are included.
17. Tablette nach einem der Ansprüche 1 bis 15, dadurch gekennzeichnet, dass 20 bis 35 Masse-% Coffein,17. Tablet according to one of claims 1 to 15, characterized in that 20 to 35% by mass of caffeine,
60 bis 80 Masse-% Isomalt und Xylitol,60 to 80% by mass of isomalt and xylitol,
1,5 bis 5 Masse- Aroma- oder Aromastoffgemisch1.5 to 5 mass, flavor or flavor mixture
sowiesuch as
3 bis 5 Masse-% Hydroxypropylmethylcellulose und3 to 5% by mass of hydroxypropylmethyl cellulose and
0,3 bis 1 Masse-% Magnesiumstearat enthaltenContain 0.3 to 1% by mass of magnesium stearate
sind.are.
18. Tablette nach einem der Ansprüche 1 bis 15, dadurch gekennzeichnet, dass 50 mg Coffein,18. Tablet according to one of claims 1 to 15, characterized in that 50 mg of caffeine,
70 Masse-% Isomalt und Xylitol,70% by mass isomalt and xylitol,
12,5 Masse-% Natriumbikarbonat,12.5 mass% sodium bicarbonate,
12,5 Masse-% Zitronensäure,12.5 mass% citric acid,
1 Masse-% Aromastoff oder Aromastoffgemisch und1% by mass of flavoring agent or flavoring agent mixture and
0,5 Masse-% Binder enthalten sind. 0.5% by mass of binder are included.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
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DE10320049.5 | 2003-04-30 | ||
DE10320049 | 2003-04-30 | ||
DE10339864.3 | 2003-08-26 | ||
DE10339864A DE10339864A1 (en) | 2003-04-30 | 2003-08-26 | Caffeine-containing tablet |
Publications (2)
Publication Number | Publication Date |
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WO2004095942A2 true WO2004095942A2 (en) | 2004-11-11 |
WO2004095942A3 WO2004095942A3 (en) | 2005-01-06 |
Family
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Application Number | Title | Priority Date | Filing Date |
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PCT/DE2004/000843 WO2004095942A2 (en) | 2003-04-30 | 2004-04-16 | Caffeinated tablet |
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Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2006065140A1 (en) * | 2004-12-17 | 2006-06-22 | 4Sight Innovation B.V. | Method for manufacturing products for enriching a drink with additives |
CN103564593A (en) * | 2012-08-02 | 2014-02-12 | 佳格食品股份有限公司 | Effervescent tablets with enhanced refreshing effect |
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US6165511A (en) * | 1996-04-22 | 2000-12-26 | Merck Patent Gesellschaft Mit Beschrankter Haftung | Polyol composition |
DE19943491A1 (en) * | 1999-09-10 | 2001-03-15 | Suedzucker Ag | Improved compressions |
US6426090B1 (en) * | 1999-04-06 | 2002-07-30 | Wm. Wrigley Jr. Company | Over-coated product including tableted center and medicament |
US6444241B1 (en) * | 2000-08-30 | 2002-09-03 | Wm. Wrigley Jr. Company | Caffeine coated chewing gum product and process of making |
WO2002078459A1 (en) * | 2001-03-29 | 2002-10-10 | Societe Des Produits Nestles S.A. | Chewing gum-containing tablet |
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2004
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Publication number | Priority date | Publication date | Assignee | Title |
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US6165511A (en) * | 1996-04-22 | 2000-12-26 | Merck Patent Gesellschaft Mit Beschrankter Haftung | Polyol composition |
US6426090B1 (en) * | 1999-04-06 | 2002-07-30 | Wm. Wrigley Jr. Company | Over-coated product including tableted center and medicament |
DE19943491A1 (en) * | 1999-09-10 | 2001-03-15 | Suedzucker Ag | Improved compressions |
US6444241B1 (en) * | 2000-08-30 | 2002-09-03 | Wm. Wrigley Jr. Company | Caffeine coated chewing gum product and process of making |
WO2002078459A1 (en) * | 2001-03-29 | 2002-10-10 | Societe Des Produits Nestles S.A. | Chewing gum-containing tablet |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2006065140A1 (en) * | 2004-12-17 | 2006-06-22 | 4Sight Innovation B.V. | Method for manufacturing products for enriching a drink with additives |
CN103564593A (en) * | 2012-08-02 | 2014-02-12 | 佳格食品股份有限公司 | Effervescent tablets with enhanced refreshing effect |
CN105412041A (en) * | 2012-08-02 | 2016-03-23 | 佳格食品股份有限公司 | Effervescent tablet with energizing enhancing effect |
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