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
  • A61K9/20—Pills, tablets, discs, rods
  • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
  • A61K9/2806—Coating materials
  • A61K9/2833—Organic macromolecular compounds
  • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
  • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Definitions

• This invention relates to taste-masking of solid medicaments, particularly by enveloping them in a tasta- masking polymer film coating.
• Therapeutic formulations designed for oral adminis ⁇ tration often contain active ingredients which have an unpleasant taste. For instance, many drugs produce a bitter or acrid sensation when taken by mouth.
• the proportion of PVP in the film coating is from about 12% to 20% by weight. If used alone, however, the patentees found that the cellulose ester coating would not provide adequate bioavailability of the active ingredient at the specified coating levels of 5% to 20% by weight. This is clearly evident from Figure 1 of the patent depicting in graphic form the dissolution rate of APAP in simulated gastric fluid at a coating level of 17.5% by weight and which the percent o-f PVP in the coating blend varied from 0% to 25% 'by weight. As will be noted, at 0% PVP in the film coating drug release amounted to only 40% after 40 minutes.
• solid medicaments can be effectively taste-masked with a film envelope consisting essentially of a cellulose ester applied from a latex dispersion of the ester, while maintaining rapid release of active ingredients.
• a film envelope consisting essentially of a cellulose ester applied from a latex dispersion of the ester, while maintaining rapid release of active ingredients.
• Figure 1 is a graph of percent dissolution versus time for aspirin tablets (acetylsalicylic acid - ASA) coated with the ultra-thin cellulose ester films made in accordance with the invention and the uncoated core control.
• Figure 2 is a graph of percent dissolution versus time for ASA tablets coated with the ultra-thin cellu ⁇ lose ester films of the invention, for ASA tablets simi ⁇ larly coated with the cellulose ester/PVP blend of U. S. Patent No. 4,851,226 to Julian et al., and for the.un- coated core control.
• aqueous plasticized cellulose ester dispersion used in the practice of the invention is a known chemi- cal entity. Commonly referred to as a cellulose ester latex, it is prepared by dissolving the polymer in a suitable organic solvent, dispersing the resulting solu ⁇ tion in an aqueous phase, homogenizing, and evaporating the solvent. To the resulting latex is added an appro- priate plasticizer.
• cellulose ester latexes suita ⁇ ble for producing the ultra-thin coatings of the in ⁇ vention are latexes made from cellulose acetate, cellu- lose acetate butyrate and cellulose acetate phthalate.
• Cellulose ester polymers are manufactured and sold com ⁇ surgeally by a number of suppliers of industrial chemi ⁇ cals, for example, the Eastman Kodak Company, Kingsport, Tenn.
• suitable plasticizers for cellulose aqueous dispersions include triacetin, diacetin and triethylcitrate.
• medicament can be, for ex ⁇ ample, granules, tablets including tablets of the co - pressed coated granules of drugs such as aspirin (ASA) , acetaminophen, and ibuprofen.
• drugs such as aspirin (ASA) , acetaminophen, and ibuprofen.
• the ultra-thin, taste-masking films of the in ⁇ vention are conveniently produced by coating the solid medicament substrate with an aqueous cellulose acetate dispersion in which the preferred plasticizer is tri ⁇ acetin.
• the triacetin is added to the dispersion and the mixture thoroughly mixed.
• the amount of plasticizer ranges by weight from about 50% to about 150%, preferably from about '30% to 120%, optimally about 100% of the solids content of the dispersion.
• a cellu ⁇ lose acetate aqueous dispersion having a solids content of by weight of from about 28% to 32% is available from the FMC Corporation under the designation CA398-10 latex dispersion.
• the ultra-thin, taste-masking cellulose films of the invention are applied to the solid medicament in a known manner and with standard pharmaceutical coating equipment. Coating is normally carried out by spraying in a pan or in a fluidized bed. Solids content of the aqueous cellulose ester coat ⁇ ing formulation plus plasticizer is in the neighborhood of from about by weight 10% to about 30%, preferably 15% to 20%. In the final dried coating, the amount of plas ⁇ ticizer present in the film coating ranges by weight from about 30% to about 60%.
• ultra-thin cellulose ester film coatings of the invention can be realized with the ultra-thin cellulose ester film coatings of the invention at coating levels of about 0.4% by weight based on total solid dosage form weight.
• Other types of solid dosage forms such as granules may require somewhat higher coating levels. So far as has been determined, overall coating levels will vary from about 0.3% to about 1.0% by weight for effective taste- masking.
• the amount of coating applied to the substrate can be controlled in known manner such as solids content of the coating dispersion and contact times.
• ASA release was more rapid for aspirin tablets coated solely with CA latex than with the CA latex/PVP blend.

Landscapes

• Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Epidemiology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Engineering & Computer Science (AREA)
• Life Sciences & Earth Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Applications Claiming Priority (2)

Publications (2)

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ID=24785870

Family Applications (1)

Country Status (6)

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Citations (1)

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• 1992
  • 1992-04-03 JP JP4511820A patent/JP2538491B2/ja not_active Expired - Lifetime
  • 1992-04-03 AU AU21673/92A patent/AU651721B2/en not_active Ceased
  • 1992-04-03 CA CA002107229A patent/CA2107229C/en not_active Expired - Fee Related
  • 1992-04-03 WO PCT/US1992/002692 patent/WO1992019209A2/en not_active Application Discontinuation
  • 1992-04-03 EP EP92912798A patent/EP0583399A4/en not_active Withdrawn
• 1993
  • 1993-10-29 NO NO933920A patent/NO933920L/no unknown

Patent Citations (1)

Non-Patent Citations (1)

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