Classifications

• • 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
  • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
  • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K33/00—Medicinal preparations containing inorganic active ingredients
  • A61K33/44—Elemental carbon, e.g. charcoal, carbon black
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
  • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P13/00—Drugs for disorders of the urinary system
  • A61P13/12—Drugs for disorders of the urinary system of the kidneys
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P39/00—General protective or antinoxious agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P39/00—General protective or antinoxious agents
  • A61P39/02—Antidotes
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P7/00—Drugs for disorders of the blood or the extracellular fluid

Definitions

• the invention relates to a hydrous suspension formulation comprising a coarse-grained carbon adsorbent which is suitable for binding and removal of harmful substances from the gastrointestinal tract, and to a water-soluble or water-dispersible structuring agent and a humectant.
• these activated carbons are used as dry granules.
• this dry application form is only conditionally suitable because it does not mix homogeneously with dry foods.
• the application to dry food is an essential prerequisite for the commercial success of such a product in animals.
• a liquid or pasty formulation containing the adsorbent can be combined with any type of feed.
• the most important requirements for such a formulation are that the adsorption properties are not unduly reduced and the palatability of the food or feedstuff is not restricted by the composition and consistency nor by the dose volume, even in the case of accidental overdosage or top dressing.
• Formulation based on a water-soluble carrier which mixes with oral administration without problems with the aqueous media of the gastrointestinal tract and the adsorbent is rapidly distributed freely for the adsorption of toxins dissolved in the aqueous medium. good compatibility even with permanent administration
• the invention relates to:
• a hydrous suspension formulation comprising a coarse-grained carbon adsorbent, a humectant, and a water-soluble or water-dispersible structuring agent.
• coarse-grained carbon adsorbents are meant here those having a diameter of at least 0.1 mm, preferably 0.1 to 1 mm, particularly preferably 0.1 to 0.8 mm, in particular 0.1 to 0.6 mm.
• these adsorbents have a spherical shape, an ideal spherical shape is not necessarily feasible in practice, therefore, “spherical” particles should also be understood as meaning approximately spherical particles.
• the carbon adsorbents used according to the invention preferably have a specific surface, determined by the BET method, of 700 m 2 / g or more, more preferably 800 m 2 / g or more.
• the carbon adsorbents may have functional groups.
• they may have acidic groups which are preferably present in a total amount of 0.30 to 1.20 meq / g, in particular 0.30 to 1.00 meq / g.
• the adsorbents may have basic groups, which are preferably present in a total amount of 0.20 to 0.70 meq / g, in particular 0.30 to 0.60 meq / g.
• the adsorbents may have phenolic hydroxyl groups, which are preferably present in a total amount of 0.20 to 0.70 meq / g.
• the adsorbents may also have carboxyl groups.
• the adsorbents contain functional groups, they preferably have acidic and basic functional groups, preferably 0.30 to 1.20 meq / g, in particular 0.30 to 1.00 meq / g of acidic groups and 0.20 to 0 , 70 meq / g, especially 0.30 to 0.60 meq / g of basic groups.
• these have a total amount of 0.30 to 1.20 meq / g, in particular 0.30 to 1.00 meq / g of acidic groups and a total of 0.20 to 0.70 meq / g, especially 0.30 to 0.60 meq / g of basic groups, with 0.20 to 0.70 meq / g of phenolic hydroxyl groups and 0.15 meq / g or less of carboxyl groups.
• the ratio (a: b) of the total amount of acidic groups (a) to the total amount of basic groups (b) is 0.40 to 2.5.
• the value of [(b + c) -d] for the total amount of basic groups (b), the amount of phenolic hydroxyl groups (c) and the amount of carboxyl groups (d) is preferably 0.60 or more (amounts in meq / g).
• the carbon adsorbents preferably have a pore volume of the pores with a diameter of 20 to 15 000 nm of 0.04 mL / g to 0.1 mL / g, preferably 0.05 mL / g to 0.1 mL / g.
• the formulations according to the invention usually contain 10 to 80% m / V, preferably 20 to 60% m / V, particularly preferably 30 to 50% m / V carbon adsorbent.
• % m / V mass of the respective ingredient in grams per 100 mL of the final formulation.
• the formulations usually contain 1 to 95% m / V, preferably 5 to 60% m / V, more preferably 10 to 40% m / V water.
• the humectant is usually liquid to viscous and water soluble.
• Humectants are preferably used di- or trihydric alcohols having 2 to 10, preferably 3 to 6 carbon atoms, for example, glycerol, ethylene glycol, Diethylene glycol or propylene glycol. Preference is given to propylene glycol and in particular glycerol.
• the humectant is usually contained in the formulations in an amount of 10 to 95% m / V, preferably 50 to 80% m / V.
• the formulations according to the invention also contain a water-soluble or water-dispersible structuring agent, which generally forms a yield-limit gel structure in the suspension formulations. It was found that the addition of a structuring agent improves the stability, in particular the long-term stability of the formulations, which is not easy with the relatively coarse-grained adsorbent.
• suitable structuring agents may be mentioned in particular: cellulose derivatives, such as. Methylcellulose, carboxymethylcellulose, sodium carboxymethylcellulose, hydroxyethylcellulose, polymeric carbohydrates, such as. Xanthan gum, alginate, gum arabic, pectins; Polypeptides, such as. As gelatin, casein, and polyvinylpyrrolidone (PVP), ethyl acrylate and methyl methacrylate copolymers or polyacrylic acid and mixtures of such components.
• PVP polyvinylpyrrolidone
• the structuring agent is usually present in amounts of 0.2 to 15% m / V, preferably 0.5 to 10% m / V, particularly preferably 1 to 5% m / V. If a mixture of structuring agents is used, the above information refers to the total amount.
• the formulation of the invention may contain other conventional pharmaceutical ingredients, such as.
• food dyes and / or pigments such as titanium dioxide or iron oxide.
• pigments are usually contained in amounts of 0.1 to 10% m / V, preferably 0.2 to 8% m / V.
• the formulation may also contain conventional preservatives, such as. B. sorbic acid optionally in combination with ascorbic acid. Standard concentrations are used which are familiar to the expert, such as. From 0.01 to 1% m / V.
• the formulations do not contain any preservatives, and are particularly preferred if they contain more than 30% m / V, preferably more than 40% m / V, in particular more than 50% m / V of humectant.
• the formulations of the invention are liquid, preferably viscous, to a pasty consistency.
• the formulations according to the invention preferably have viscosities of from 1 to 100 Pas, particularly preferably from 1 to 30 Pas, very particularly preferably from 5 to 20 Pas (measured at a shear rate of 25 s -1 .)
• the formulations according to the invention are preferably characterized by pseudoplastic flow behavior Preferably, they also show thixotropy.
• the formulations according to the invention preferably have yield points of from 10 to 500 Pa, in particular from 30 to 200 Pa.
• formulations according to the invention can be prepared, for example, by adding the
• Structurant and optionally pigments and other auxiliaries mixed in a mixture of humectant and water, dissolves or dispersed and then incorporated the carbonaceous adsorbent in the formulation base and distributed homogeneously.
• the formulations according to the invention are generally suitable for use in humans and animals. Preferably, they are used in livestock and animal breeding in livestock, breeding, zoo, laboratory, experimental and hobby animals, especially in mammals.
• the livestock and breeding animals include mammals such as e.g. Cattle, horses, sheep, pigs, goats, camels, water buffalo, donkeys, rabbits, fallow deer, reindeer, fur animals such as e.g. Mink, chinchilla, raccoon, as well as birds such as e.g. Chickens, geese, turkeys, ducks, pigeons and ostriches.
• mammals such as e.g. Cattle, horses, sheep, pigs, goats, camels, water buffalo, donkeys, rabbits, fallow deer, reindeer, fur animals such as e.g. Mink, chinchilla, raccoon, as well as birds such as e.g. Chickens, geese, turkeys, ducks, pigeons and ostriches.
• preferred farm animals are beef, sheep, pork and chicken.
• Laboratory and experimental animals include dogs, cats, rabbits and rodents such as mice, rats, guinea pigs and golden hamsters.
• the hobby animals include dogs, cats, horses, rabbits, rodents such as golden hamsters, guinea pigs, mice, reptiles, amphibians and birds for home and zoo keeping.
• the formulations of the invention are used in pets, and most preferably in dogs and especially cats.
• the application can be both prophylactic and therapeutic.
• the formulations of the invention are usually and preferably administered orally. Furthermore, a rectal administration is possible.
• the formulations according to the invention are administered orally with the feed; they can be applied to both wet and dry food, mixed in or even on top.
• Examples include: hepatotoxic encephalitis, chronic aflatoxin intoxication, acute intoxication.
• the formulations of the invention are usually dosed so that 0.05 to 4.0, preferably 0.1 to 0.4 grams of carbon adsorbent per kilogram of body weight and day are administered.
• these are typically dosing volumes of 0.5 to 10 mL.
• these are typically dosing volumes of 0.5 to 10 mL.
• the invention also relates to aqueous formulations of the preferred and particularly preferred spherical carbon adsorbents mentioned above and in EP-A-1249241.
• the formulations of the invention have a good palatability, for example, the palatability of dry cat food in the dose range 5 - 2O g AST-120 / kg feed is not adversely affected.
• AST-120 is used in the prior art only as a dry granule. Suspension formulations or pastes, in particular with a high proportion of adsorbent, have not been described so far.
• the following table contains the measured values for the adsorption capacity of AST-120 in various paste formulations in comparison with pure, dry granules:
• the adsorption values of the target toxins are generally only about 2-3% and not more than 5% below the dry granule data for all the formulations investigated.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Chemical & Material Sciences (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Medicinal Chemistry (AREA)
• Animal Behavior & Ethology (AREA)
• Pharmacology & Pharmacy (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Epidemiology (AREA)
• Toxicology (AREA)
• Inorganic Chemistry (AREA)
• Urology & Nephrology (AREA)
• Gastroenterology & Hepatology (AREA)
• Hematology (AREA)
• Diabetes (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicinal Preparation (AREA)
• Carbon And Carbon Compounds (AREA)
• Solid-Sorbent Or Filter-Aiding Compositions (AREA)

Applications Claiming Priority (2)

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• 2008
  • 2008-03-13 DE DE102008014109A patent/DE102008014109A1/de not_active Withdrawn
• 2009
  • 2009-02-28 CN CN2009801087705A patent/CN101969925A/zh active Pending
  • 2009-02-28 US US12/922,137 patent/US20110021641A1/en not_active Abandoned
  • 2009-02-28 BR BRPI0908576A patent/BRPI0908576A2/pt not_active IP Right Cessation
  • 2009-02-28 AU AU2009225055A patent/AU2009225055A1/en not_active Abandoned
  • 2009-02-28 KR KR1020107021446A patent/KR20100135760A/ko not_active Withdrawn
  • 2009-02-28 MX MX2010008982A patent/MX2010008982A/es not_active Application Discontinuation
  • 2009-02-28 CA CA2718142A patent/CA2718142A1/en not_active Abandoned
  • 2009-02-28 JP JP2010550063A patent/JP2011513448A/ja not_active Withdrawn
  • 2009-02-28 WO PCT/EP2009/001450 patent/WO2009112169A2/de not_active Ceased
  • 2009-02-28 EP EP09720023A patent/EP2265254A2/de not_active Withdrawn
  • 2009-03-03 PE PE2009000323A patent/PE20091578A1/es not_active Application Discontinuation
  • 2009-03-05 UY UY0001031692A patent/UY31692A/es not_active Application Discontinuation
  • 2009-03-06 CL CL2009000538A patent/CL2009000538A1/es unknown
  • 2009-03-09 AR ARP090100834A patent/AR070974A1/es not_active Application Discontinuation
  • 2009-03-12 TW TW098107953A patent/TW200950791A/zh unknown
• 2010
  • 2010-08-26 ZA ZA2010/06082A patent/ZA201006082B/en unknown

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