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
  • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
  • A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
  • A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
  • A61K31/546—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
  • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
  • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• • 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
  • A61K9/10—Dispersions; Emulsions
• • 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
  • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
  • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
  • A61K9/5005—Wall or coating material
  • A61K9/5015—Organic compounds, e.g. fats, sugars

Definitions

• the common oral dosage form include , liquid mixture like solution, suspension, solid dosage form like tablets , capsules and liquid filled capsules etc.
• patient at extremes of ages such as children and the elderly , often experience difficulty in swallowing solid oral dosage form, for these patients the drug are mostly in liquid dosage form such as solution , suspension and emulsion.
• This dosage form usually lead to perceptible exposure of active ingredients to taste buds and if the active ingredient is bitter this gives extremely unpleasant bitter taste.
• taste masking is major problem when the drug is extremely unpleasant and bitter in taste. This problem is not restricted to liquid oral composition like solution and syrups but is also encountered in oral dry suspension wherein the dosage form usually lead to perceptible exposure of active ingredients to taste buds.
• Cefuroxime axetil In the formulation of Cefuroxime axetil into granules it is important to avoid the release of the drug into any liquid medium in which it is suspended or indeed into the mouth when administering. Such problem may be minimized by formulating the Cefuroxime axetil as lipid coated particles.
• WO 2007/061803 Patent relates to functional sweeteners composition comprising non - caloric or low - caloric natural or synthetic, high potency sweeteners and method of masking and using them.
• This invention discloses in its specification the use of different functional sweetener comprising of atleast one non - caloric or low caloric natural or synthetic, high potency sweetener, at least one sweet taste improving sweetener, and atleast one functional ingredient, such as C - reactive protein reducing substance.
• This invention also includes the method to improve the taste of non - caloric or low caloric high potency sweetener by imparting a more sugar like taste or characteristic.
• the sweetener system used in the composition of present invention prove to be better to overcome the bitter taste, which has been evaluated and results discussed herein below in this application.
• the taste masked composition of present invention comprises a bitter tasting active drug, wherein the active drug used is cefuroxime axetil , a integral coating of lipid which is insoluble in aqueous media and serve to mask the bitter taste of cefuroxime axetil upon oral administration , a "sweetener system" as lipid coating goes up to some extend to provide bitterness inhibition.
• cefuroxime axetil used in the examples was highly pure spray dried amorphous material.
• the Sweetener system was blended together with the cefuroxime axetil granules as a dry mix ensuring that they are evenly in admixture.
• Sweetener system comprises of acesulfame, neotame & along with the third sweetener sucralose was blended together with the cefuroxime axetil lipid coated granules as a dry mix ensuring that they are evenly in admixture.
• Cefuroxime Axetil oral suspension 125mg/5ml
• Sweetener system comprises of neotame, sucralose along with sugar alcohol sorbitol as sweetener was blended together with the cefuroxime axetil lipid coated granules as a dry mix ensuring that they are evenly in admixture.

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Dispersion Chemistry (AREA)
• Biochemistry (AREA)
• Molecular Biology (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Oil, Petroleum & Natural Gas (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

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Publications (1)

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Cited By (4)

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• 2012
  • 2012-06-28 EP EP12750614.5A patent/EP2741750A1/de not_active Withdrawn
  • 2012-06-28 WO PCT/IB2012/053283 patent/WO2013024373A1/en active Search and Examination

Non-Patent Citations (1)

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