DE19733094A1 - Formulation based on ascorbic acid with improved color stability - Google Patents
Formulation based on ascorbic acid with improved color stabilityInfo
- Publication number
- DE19733094A1 DE19733094A1 DE19733094A DE19733094A DE19733094A1 DE 19733094 A1 DE19733094 A1 DE 19733094A1 DE 19733094 A DE19733094 A DE 19733094A DE 19733094 A DE19733094 A DE 19733094A DE 19733094 A1 DE19733094 A1 DE 19733094A1
- Authority
- DE
- Germany
- Prior art keywords
- preparation according
- weight
- ascorbic acid
- several
- cellulose
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
Links
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 title claims abstract description 46
- 229960005070 ascorbic acid Drugs 0.000 title claims abstract description 23
- 235000010323 ascorbic acid Nutrition 0.000 title claims abstract description 23
- 239000011668 ascorbic acid Substances 0.000 title claims abstract description 23
- 239000000203 mixture Substances 0.000 title claims abstract description 18
- 238000009472 formulation Methods 0.000 title abstract description 10
- 238000002360 preparation method Methods 0.000 claims description 27
- 150000005846 sugar alcohols Chemical class 0.000 claims description 14
- 239000007787 solid Substances 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 9
- 235000019640 taste Nutrition 0.000 claims description 9
- 239000011230 binding agent Substances 0.000 claims description 6
- 239000002245 particle Substances 0.000 claims description 6
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 5
- 229930195725 Mannitol Natural products 0.000 claims description 5
- 238000005469 granulation Methods 0.000 claims description 5
- 230000003179 granulation Effects 0.000 claims description 5
- 239000000594 mannitol Substances 0.000 claims description 5
- 235000010355 mannitol Nutrition 0.000 claims description 5
- 239000001913 cellulose Substances 0.000 claims description 4
- 229920002678 cellulose Polymers 0.000 claims description 4
- 235000010980 cellulose Nutrition 0.000 claims description 4
- 239000000832 lactitol Substances 0.000 claims description 4
- 235000010448 lactitol Nutrition 0.000 claims description 4
- VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 claims description 4
- 229960003451 lactitol Drugs 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 235000009508 confectionery Nutrition 0.000 claims description 3
- 235000015872 dietary supplement Nutrition 0.000 claims description 3
- 239000000126 substance Substances 0.000 claims description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 3
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 2
- 239000004386 Erythritol Substances 0.000 claims description 2
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 claims description 2
- 239000005913 Maltodextrin Substances 0.000 claims description 2
- 229920002774 Maltodextrin Polymers 0.000 claims description 2
- 229920002472 Starch Polymers 0.000 claims description 2
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 2
- 239000007864 aqueous solution Substances 0.000 claims description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 2
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 2
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 2
- 229940112822 chewing gum Drugs 0.000 claims description 2
- 235000015218 chewing gum Nutrition 0.000 claims description 2
- 235000019414 erythritol Nutrition 0.000 claims description 2
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims description 2
- 229940009714 erythritol Drugs 0.000 claims description 2
- -1 hydroxymethyl propyl Chemical group 0.000 claims description 2
- 229940035034 maltodextrin Drugs 0.000 claims description 2
- 229960001855 mannitol Drugs 0.000 claims description 2
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 2
- 229920000609 methyl cellulose Polymers 0.000 claims description 2
- 239000001923 methylcellulose Substances 0.000 claims description 2
- 235000010981 methylcellulose Nutrition 0.000 claims description 2
- 239000000243 solution Substances 0.000 claims description 2
- 239000000600 sorbitol Substances 0.000 claims description 2
- 239000008107 starch Substances 0.000 claims description 2
- 235000019698 starch Nutrition 0.000 claims description 2
- 239000000811 xylitol Substances 0.000 claims description 2
- 235000010447 xylitol Nutrition 0.000 claims description 2
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 2
- 229960002675 xylitol Drugs 0.000 claims description 2
- 229920001971 elastomer Polymers 0.000 claims 1
- 238000004064 recycling Methods 0.000 claims 1
- 239000005060 rubber Substances 0.000 claims 1
- 239000000796 flavoring agent Substances 0.000 abstract description 3
- 235000019634 flavors Nutrition 0.000 abstract description 3
- 239000003826 tablet Substances 0.000 description 9
- 239000004480 active ingredient Substances 0.000 description 7
- 239000000047 product Substances 0.000 description 6
- 239000007921 spray Substances 0.000 description 6
- 238000009477 fluid bed granulation Methods 0.000 description 3
- 239000007937 lozenge Substances 0.000 description 3
- 239000007910 chewable tablet Substances 0.000 description 2
- 230000001055 chewing effect Effects 0.000 description 2
- 239000006187 pill Substances 0.000 description 2
- 238000003860 storage Methods 0.000 description 2
- 239000007916 tablet composition Substances 0.000 description 2
- 229940088594 vitamin Drugs 0.000 description 2
- 229930003231 vitamin Natural products 0.000 description 2
- 235000013343 vitamin Nutrition 0.000 description 2
- 239000011782 vitamin Substances 0.000 description 2
- 150000003722 vitamin derivatives Chemical class 0.000 description 2
- 229920000084 Gum arabic Polymers 0.000 description 1
- 241000978776 Senegalia senegal Species 0.000 description 1
- 238000005299 abrasion Methods 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 235000019658 bitter taste Nutrition 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 238000002845 discoloration Methods 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- 210000002200 mouth mucosa Anatomy 0.000 description 1
- 238000003825 pressing Methods 0.000 description 1
- 238000007391 self-medication Methods 0.000 description 1
- 230000001953 sensory effect Effects 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 235000019614 sour taste Nutrition 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 230000009469 supplementation Effects 0.000 description 1
- 238000004383 yellowing Methods 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G3/00—Sweetmeats; Confectionery; Marzipan; Coated or filled products
- A23G3/34—Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
- A23G3/346—Finished or semi-finished products in the form of powders, paste or liquids
-
- 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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/02—Nutrients, e.g. vitamins, minerals
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23G—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
- A23G2200/00—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF containing organic compounds, e.g. synthetic flavouring agents
- A23G2200/04—COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF containing organic compounds, e.g. synthetic flavouring agents containing vitamins, antibiotics, other medicaments
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Nutrition Science (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Physiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Zoology (AREA)
- Diabetes (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Food Science & Technology (AREA)
- Polymers & Plastics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Confectionery (AREA)
Abstract
Description
Die Erfindung betrifft eine neue Formulierung auf der Basis von Ascorbinsäure mit einem verbesserten Geschmacksbild, welche direkt komprimierbar ist und eine verbesserte Farbstabilität aufweist.The invention relates to a new formulation based on Ascorbic acid with an improved taste, which is directly compressible and has improved color stability.
Bei der Formulierung oral zu verabreichender pharmazeutischer Zusammensetzungen bereitet in vielen Fällen nicht nur bei flüssigen Applikationsformen das vom Verwender empfundene Geschmacksbild Probleme.When formulated orally administered pharmaceutical In many cases, compositions do not only prepare liquids Application forms that perceived by the user Taste problems.
Als problematisch hat sich auch bei verschiedensten Wirkstoffen ein als äußerst bitter oder auch sauer empfundener Geschmack erwiesen. Eine Maskierung besonders saurer, bitterer oder kreidiger Wirkstoffe ist bisher durch den Zusatz von Geschmacks- oder Aromastoffen nicht gelungen. Es besteht zwar die Möglichkeit, entsprechende Wirkstoffe enthaltende Tabletten mit einem Überzug zu versehen, diese Methode ist jedoch ungeeignet, wenn eine schnelle Aufnahme des Wirkstoffs, die bereits beim Kauen der Tabletten über die Mundschleimhaut erfolgt, angestrebt wird.A problem has also arisen with a wide variety of active ingredients as an extremely bitter or sour taste proven. A mask that is particularly acidic, bitter or chalky Active ingredients has so far been added by adding flavor or Flavors failed. It is possible to corresponding active ingredient-containing tablets with a coating this method is unsuitable if a rapid absorption of the active ingredient, already when chewing the Tablets are taken over the oral mucosa, the aim is.
Besondere Anforderungen werden auch an die Oberfläche von Tabletten gestellt, die gelutscht werden sollen, wie beispielsweise Halstabletten. Erwünscht ist hierbei eine glatte Oberfläche der eigentlichen Tablette, die während des Lutschens erhalten bleibt und sich nicht nach und nach aufrauht.Special requirements are also placed on the surface of Pills to be sucked, such as Throat tablets. What is desired here is a smooth surface of the actual tablet that is preserved during sucking and does not gradually roughen up.
Weiterhin werden heute im Bereich der Nahrungsergänzung (Vitamin- und Mineralstoffsupplementierung) vermehrt Lutsch- und vor allem Kautabletten angeboten.Furthermore, in the area of nutritional supplements (vitamin and mineral supplementation) increased sucking and especially Chewable tablets offered.
Des weiteren versucht man, bei der Herstellung von festen Formulierungen zunehmend direkt verpreßbare Wirkstoffe (DC-Wirkstoffe) einzusetzen, um Produktionskosten zu senken.Furthermore, one tries to produce solid ones Formulations increasingly directly compressible active ingredients (DC active ingredients) to reduce production costs.
Hier hat es sich nun insbesondere bei der Herstellung von Vitamin haltigen Formulierungen als problematisch erwiesen, daß Ascorbinsäure im Handel nicht in direkt verpreßbarer Form erhältlich ist. Here it is now particularly in the production of vitamin containing formulations proved problematic that Ascorbic acid is not commercially available in a directly compressible form is.
Aufgabe der vorliegenden Erfindung ist es daher, ein Verfahren zur Verfügung zu stellen, wodurch einerseits Ascorbinsäure in einer direkt verpreßbaren Form zugänglich gemacht wird, andererseits das Geschmacksbild von Ascorbinsäure haltigen festen Formulierungen verbessert wird und gleichzeitig das sensorische Mundgefühl der hergestellten Produkte vorteilhaft beeinflußt wird.The object of the present invention is therefore to provide a method for To provide, on the one hand, ascorbic acid in a direct compressible form is made accessible, on the other hand, the Taste of solid formulations containing ascorbic acid is improved and at the same time the sensory mouthfeel of the manufactured products is advantageously influenced.
Es wurde nun gefunden, daß das Geschmacksbild von Ascorbinsäure enthaltenden festen Zubereitungen, welche 85 bis 98 Gew.-% Ascorbinsäure enthalten, verbessert werden kann, indem eine einen oder mehrere Zuckeralkohole in einer Menge von 1,5 bis 15 Gew.-%, bezogen auf die eingewogene Feststoffmenge, enthaltende wäßrige Zusammensetzung, durch Sprühgranulation bzw. Wirbelschichtgranulation oder Sprüh- Wirbelschichtgranulation in eine fester Form überführt wird.It has now been found that the taste profile of ascorbic acid solid preparations containing 85 to 98% by weight Containing ascorbic acid can be improved by a one or several sugar alcohols in an amount of 1.5 to 15% by weight, based on the weighed amount of solids, containing aqueous Composition, by spray granulation or Fluid bed granulation or spray fluid bed granulation in a solid form is transferred.
Gegenstand der Erfindung sind somit Ascorbinsäure enthaltende Zubereitungen in direkt verpreßbarer Form mit verbessertem Geschmacksbild.The invention thus relates to ascorbic acid Preparations in a directly compressible form with improved Taste.
Gegenstand der Erfindung ist daher auch ein Verfahren zur
Herstellung von Ascorbinsäure enthaltenden festen Zubereitungen in
direkt verpreßbarer Form mit verbessertem Geschmacksbild, dadurch
gekennzeichnet, daß man
The invention therefore also relates to a process for the preparation of ascorbic acid-containing solid preparations in directly compressible form with an improved taste, characterized in that
-
a) eine wäßrige Lösung hergestellt, enthaltend
- - 85 bis 98 Gew.-% an Ascorbinsäure,
- - 1,5 bis 15 Gew.-% eines oder mehrerer Zuckeralkohole,
- - bis zu 1,2 Gew.-% eines Bindemittels,
- 85 to 98% by weight of ascorbic acid,
- 1.5 to 15% by weight of one or more sugar alcohols,
- up to 1.2% by weight of a binder,
- b) die erhaltene Lösung in Luftströmungen, welche verschiedene Temperaturen zwischen Raumtemperatur bis 180°C, bevorzugt 60 bis 140°C, aufweisen versprüht,b) the solution obtained in air currents, which different Temperatures between room temperature up to 180 ° C, preferably 60 to 140 ° C, have sprayed,
- c) wasserdampfhaltiger Luftströmungen, abzieht, undc) steam-containing air currents, deducts, and
- d) die sich in einem Wirbelbett niedriger Höhe, welches zudem eine variable Höhe aufweist, bildenden homogenen Partikel als feste Form abführt und d) which is in a fluidized bed of low height, which is also a variable height, forming homogeneous particles as solid Form dissipates and
- e) bis zu 1 Gew.-% der gebildeten Partikel wieder in den Prozeß zurückführt.e) up to 1% by weight of the particles formed back into the process leads back.
Gegenstand der Erfindung sind weiterhin direkt verpreßbare Ascorbinsäure enthaltende Zubereitungen, welche außer mindestens einem Zuckeralkohol bis zu 1,5 Gew.-% eines oder mehrerer Bindemittel aus der Gruppe Cellulose, Methylcellulose, Hydroxymethylpropylcellulose, Carboxymethylcellulose, Stärke, Maltodextrin und Gummi arabicum enthalten.The invention further relates to directly compressible Preparations containing ascorbic acid which, apart from at least a sugar alcohol up to 1.5% by weight of one or more Binders from the group cellulose, methyl cellulose, Hydroxymethyl propyl cellulose, carboxymethyl cellulose, starch, Contain maltodextrin and gum arabic.
Die eingesetzte Gesamtmenge Zuckeralkohol ist dabei so zu wählen, daß in dem nach dem erfindungsgemäßen Verfahren hergestellten pulverförmige Substanzgemisch 1,5 bis 15 Gew.-%, insbesondere 2 bis 10 Gew.-% enthalten sind.The total amount of sugar alcohol used should be selected so that in the manufactured by the method according to the invention powdery mixture of substances 1.5 to 15% by weight, in particular 2 up to 10 wt .-% are included.
Erfindungsgemäß sind zur Herstellung der Ascorbinsäure enthaltenden Zubereitungen Zuckeralkohole aus der Gruppe C4-C12 Zuckeralkohole geeignet. Besonders geeignete Zuckeralkohole sind insbesondere solche aus der Gruppe Erythrit, Xylit, Mannit und Lactit.According to the invention, sugar alcohols from the group C 4 -C 12 sugar alcohols are suitable for the preparation of the preparations containing ascorbic acid. Particularly suitable sugar alcohols are in particular those from the group of erythritol, xylitol, mannitol and lactitol.
Erfindungsgemäß können in den Zubereitungen 1 Teil Mannit oder Lactit bezogen auf 0,5 bis 2,0 Teilen Sorbit enthalten sein.According to the invention, 1 part of mannitol or Lactitol based on 0.5 to 2.0 parts of sorbitol may be included.
Die erfindungsgemäße Zusammensetzung ist daher erhältlich durch Lösen von mindestens einem Zuckeralkohol in Wasser und Lösen oder Suspendieren der Ascorbinsäure und Versprühen des erhaltenen wäßrigen Gemischs in einem Luftstrom mit einer Temperatur von Raumtemperatur bis 180°C, vorzugsweise 60 bis 140°C, Abziehen wasserdampfhaltiger Luftströmungen, und Wirbelbett-Behandlung, wobei das Wirbelbett eine niedrige und zugleich variable Höhe aufweist. Die sich bildenden homogenen Partikel werden in fester Form abgeführt. Bis zu 1 Gew.-% der gebildeten Partikel werden wieder in den Prozeß zurückführt.The composition according to the invention is therefore obtainable from Dissolve at least one sugar alcohol in water and dissolve or suspending the ascorbic acid and spraying the obtained aqueous mixture in an air stream with a Temperature from room temperature to 180 ° C, preferably 60 to 140 ° C, extraction of water vapor-containing air currents, and Fluidized bed treatment, the fluidized bed being a low and at the same time has variable height. The forming homogeneous Particles are discharged in solid form. Up to 1% by weight of the Particles formed are returned to the process.
Es ist aber auch möglich das hergestellte wäßrige Gemisch in einem Luftstrom mit einer Temperatur von 40 bis 120°C zu verwirbeln und einer einfachen Sprühgranulation zu unterziehen. Es hat sich aber gezeigt, daß die vorab beschriebene kombinierte Sprüh- Wirbelschichtgranulation Produkte mit besonders vorteilhaften Eigenschaften liefert. But it is also possible to produce the aqueous mixture in one Swirl air flow with a temperature of 40 to 120 ° C and undergo a simple spray granulation. But it did demonstrated that the previously described combined spray Fluid bed granulation products with particularly advantageous Delivers properties.
An sich lassen sich aus den oben beschriebenen erfindungsgemäßen Zubereitungen ohne weitere Aufbereitung direkt durch Verpressen feste Darreichungsformen herstellen, wie z. B. Komprimate. Die durch Sprühgranulation bzw. Sprüh-Wirbelschichtgranulation erhältlichen festen Ascorbinsäurezubereitungen lassen sich auch in einfacher Weise mit einem oder mehreren Wirkstoffen vermischen und zu Tablettenformulierungen verarbeiten. Insbesondere lassen sich diese Formulierungen zu Produkten verarbeiten, die dem Kunden zur Selbstmedikation verkauft werden können. Hierzu zählen unter anderem auch Schmerzmittel in Tablettenform, Mittel gegen Erkältungen, wie z B. Halstabletten u. a. Lutschtabletten. In solchen Lutschtabletten machen sich die verbesserten Eigenschaften durch eine glattere Oberfläche nicht nur direkt nach der Herstellung sondern auch während des Lutschens bemerkbar.As such, the invention described above can be used Preparations without further processing directly by pressing produce solid dosage forms such. B. Compresses. The by spray granulation or spray fluidized bed granulation available solid ascorbic acid preparations can also be found in simply mix with one or more active ingredients and process into tablet formulations. In particular let these formulations process into products that Customers can be sold for self medication. Which includes among other things also painkillers in tablet form, agents against Colds, such as throat pills u. a. Lozenges. In such Lozenges are experiencing the improved properties a smoother surface not only immediately after production but also also noticeable while sucking.
Besonders vorteilhaft lassen sich die erfindungsgemäßen Formulierungen hier in entsprechende Kautabletten einarbeiten, da sie sich einerseits ohne großen Energieaufwand verpressen lassen, andererseits durch das verbesserte Geschmacksbild zu einem verbesserten Kauverhalten führen.The inventive can be particularly advantageous Incorporate the formulations here into the corresponding chewable tablets, because on the one hand, they can be pressed in without a lot of energy, on the other hand through the improved taste to one lead to improved chewing behavior.
Es sind mit den erfindungsgemäßen Zubereitungen in einfacher Weise auch Nahrungsergänzungspräparate herstellbar, sowohl in Tablettenform als auch in jeglicher anderen, dem Fachmann bekannten Weise. Die pulverförmigen direkt verpreßbaren Ascorbinsäurezubereitungen lassen sich aber auch in die verschiedensten Süßwaren, wie Lutschbonbons, Kaugummis oder anders geartete Süßwaren einarbeiten.It is simpler with the preparations according to the invention In this way, dietary supplements can also be produced, both in Tablet form as well as in any other, the expert known way. The powdery, directly compressible Ascorbic acid preparations can also be used in the various sweets, such as lozenges, chewing gum or incorporate different types of confectionery.
Es wurde gefunden, daß die erfindungsgemäßen Ascorbinsäureformulierungen neben einem verbesserten Geschmacksbild und der direkten Verpreßbarkeit auch zu einer besseren Lagerstabilität der hergestellten Produkte führen. Üblicherweise neigen Tablettenformulierungen in denen Ascorbinsäure enthalten ist und denen Bindemittel zugesetzt ist, um eine ausreichende Tablettenhärte zu erzielen, zum Vergilben. Im Gegensatz hierzu weisen entsprechenden Produkte, welche unter Verwendung der erfindungsgemäßen Zubereitungen hergestellt worden sind, auch nach einer Lagerung von mehreren Monaten keine Verfärbung auf. Dieses ist insbesondere der Fall, wenn zur Herstellung der Zubereitungen nicht hygroskopische Zuckeralkohole, wie Mannit, verwendet werden. Auch werden zufriedenstellende Tablettenhärten ohne Zusatz von Bindemitteln erzielt. Im Vergleich zu üblicherweise hergestellten Tabletten mit einem hohen Ascorbinsäureanteil werden durch Verwendung der erfindungsgemäßen Zubereitungen Produkte erhalten welche in Versuchen einen verminderten Abrieb aufweisen.It has been found that the inventive Ascorbic acid formulations in addition to an improved Taste and direct compressibility also into one lead to better storage stability of the manufactured products. Usually tablet formulations tend to be in those Ascorbic acid is included and to which binder is added to to achieve sufficient tablet hardness for yellowing. in the In contrast, corresponding products, which are listed under Use of the preparations according to the invention produced none, even after storage for several months Discoloration on. This is particularly the case when Preparation of the preparations of non-hygroscopic sugar alcohols like mannitol. Also be satisfactory Tablet hardness achieved without the addition of binders. Compared to Usually manufactured tablets with a high Ascorbic acid content is obtained using the Preparations according to the invention receive products which in Try to show reduced abrasion.
Claims (12)
- a) 85 bis 98 Gew.-% an Ascorbinsäure,
- b) 1 ,5 bis 15 Gew.-% eines oder mehrerer Zuckeralkohole.
- a) 85 to 98% by weight of ascorbic acid,
- b) 1.5 to 15% by weight of one or more sugar alcohols.
- a) eine wäßrige Lösung hergestellt wird, enthaltend
- - 85 bis 98 Gew.-% an Ascorbinsäure,
- - 1,5 bis 15 Gew.-% eines oder mehrerer Zuckeralkohole,
- - bis zu 1,2 Gew.-% eines Bindemittels,
- b) die erhaltene Lösung in Luftströmungen, welche verschiedene Temperaturen zwischen Raumtemperatur bis 180°C, bevorzugt 60 bis 140°C, aufweisen versprüht wird,
- c) wasserdampfhaltiger Luftströmungen, abgezogen werden, und
- d) die sich in einem Wirbelbett mit niedriger und zugleich variabler Höhe, bildenden homogenen Partikel als feste Form abführt und
- e) bis zu 1 Gew.-% der gebildeten Partikel wieder in den Prozeß zurückführt.
- a) an aqueous solution is prepared containing
- 85 to 98% by weight of ascorbic acid,
- 1.5 to 15% by weight of one or more sugar alcohols,
- up to 1.2% by weight of a binder,
- b) the solution obtained is sprayed in air currents which have different temperatures between room temperature to 180 ° C., preferably 60 to 140 ° C.,
- c) water vapor-containing air currents are subtracted, and
- d) which forms in a fluidized bed with a low and at the same time variable height, homogeneous particles as a solid form and
- e) recycling up to 1% by weight of the particles formed back into the process.
Priority Applications (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19733094A DE19733094A1 (en) | 1997-07-31 | 1997-07-31 | Formulation based on ascorbic acid with improved color stability |
| PCT/EP1998/004556 WO1999006029A1 (en) | 1997-07-31 | 1998-07-21 | Ascorbic acid-based formulation with improved colour stability |
| EP98943755A EP1007007A1 (en) | 1997-07-31 | 1998-07-21 | Ascorbic acid-based formulation with improved colour stability |
| JP2000504844A JP2001511442A (en) | 1997-07-31 | 1998-07-21 | Formulations based on ascorbic acid with improved color stability |
| CA002298624A CA2298624A1 (en) | 1997-07-31 | 1998-07-21 | Ascorbic acid-based formulation having improved colour stability |
| CN98807777A CN1265584A (en) | 1997-07-31 | 1998-07-21 | Ascorbic acid-based formulation with improved colour stability |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19733094A DE19733094A1 (en) | 1997-07-31 | 1997-07-31 | Formulation based on ascorbic acid with improved color stability |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DE19733094A1 true DE19733094A1 (en) | 1999-02-04 |
Family
ID=7837556
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE19733094A Withdrawn DE19733094A1 (en) | 1997-07-31 | 1997-07-31 | Formulation based on ascorbic acid with improved color stability |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP1007007A1 (en) |
| JP (1) | JP2001511442A (en) |
| CN (1) | CN1265584A (en) |
| CA (1) | CA2298624A1 (en) |
| DE (1) | DE19733094A1 (en) |
| WO (1) | WO1999006029A1 (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002072071A1 (en) * | 2001-03-09 | 2002-09-19 | Astrazeneca Ab | Method to obtain microparticles containing a h+, k+ -atp-ase inhibitor |
| WO2002072074A1 (en) * | 2001-03-09 | 2002-09-19 | Astrazeneca Ab | Method to prepare microparticles metoprolol that contain |
| DE102008004893A1 (en) * | 2008-01-17 | 2009-07-23 | Add Technologies Ltd. | Carrier pellets, process for their preparation and their use |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1110550B2 (en) | 1999-12-22 | 2007-04-04 | DSM IP Assets B.V. | Composition comprising ascorbic acid as a principal component and pectin |
| CN1549710A (en) | 2001-09-03 | 2004-11-24 | DSM IP�ʲ�����˾ | Composition containing pectin and ascorbic acid |
| EP3770145A1 (en) | 2019-07-24 | 2021-01-27 | Basf Se | A process for the continuous production of either acrolein or acrylic acid as the target product from propene |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3293132A (en) * | 1963-03-25 | 1966-12-20 | Merck & Co Inc | Spray dried vitamin compositions and method of preparation |
| NL184308C (en) * | 1975-07-24 | 1989-06-16 | Takeda Chemical Industries Ltd | PROCESS FOR PREPARING L-ASCORBIC ACID GRANULES. |
| DE2706660A1 (en) * | 1977-02-17 | 1978-08-24 | Merck Patent Gmbh | GRANULATES CONTAINING ASCORBIC ACID AND THE PROCESS FOR THEIR MANUFACTURING |
| JPS5759803A (en) * | 1980-09-30 | 1982-04-10 | Takeda Chem Ind Ltd | Granule of l-sodium ascorbate, its preparation, and tablet comprising it |
| CA1279574C (en) * | 1985-04-17 | 1991-01-29 | Jeffrey L. Finnan | Process for lubricating water-soluble vitamin powders |
-
1997
- 1997-07-31 DE DE19733094A patent/DE19733094A1/en not_active Withdrawn
-
1998
- 1998-07-21 CN CN98807777A patent/CN1265584A/en active Pending
- 1998-07-21 CA CA002298624A patent/CA2298624A1/en not_active Abandoned
- 1998-07-21 JP JP2000504844A patent/JP2001511442A/en active Pending
- 1998-07-21 WO PCT/EP1998/004556 patent/WO1999006029A1/en not_active Ceased
- 1998-07-21 EP EP98943755A patent/EP1007007A1/en not_active Withdrawn
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002072071A1 (en) * | 2001-03-09 | 2002-09-19 | Astrazeneca Ab | Method to obtain microparticles containing a h+, k+ -atp-ase inhibitor |
| WO2002072074A1 (en) * | 2001-03-09 | 2002-09-19 | Astrazeneca Ab | Method to prepare microparticles metoprolol that contain |
| DE102008004893A1 (en) * | 2008-01-17 | 2009-07-23 | Add Technologies Ltd. | Carrier pellets, process for their preparation and their use |
| EP2244696B1 (en) * | 2008-01-17 | 2015-08-05 | ADD Advanced Drug Delivery Technologies, Ltd. | Carrier pellets, method for the production thereof and use thereof |
| US11191726B2 (en) | 2008-01-17 | 2021-12-07 | Ipc Process-Center Gmbh & Co. Kg | Carrier pellets, method for production thereof and use thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2001511442A (en) | 2001-08-14 |
| WO1999006029A1 (en) | 1999-02-11 |
| CN1265584A (en) | 2000-09-06 |
| EP1007007A1 (en) | 2000-06-14 |
| CA2298624A1 (en) | 1999-02-11 |
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