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
  • A61K9/48—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
  • A61K9/5021—Organic macromolecular compounds
  • A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• • 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
  • A61K9/5021—Organic macromolecular compounds
  • A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
  • A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
  • A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
• • 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
  • A61K9/501—Inorganic compounds
• • 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
  • A61K9/5073—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 having two or more different coatings optionally including drug-containing subcoatings
  • A61K9/5078—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 having two or more different coatings optionally including drug-containing subcoatings with drug-free core

Definitions

• drugs are administered orally as tablets or capsules.
• drugs can be provided either as chewable or dispersible tablets or, as liquid dosage forms such as solutions, emulsions and suspensions. These dosage forms permit perceptible exposure of the active drug to the taste buds.
• Some drugs are extremely bitter and therefore unpalatable when given in these dosage forms. As a consequence, measures need to be taken to mask the taste of these drugs in order to enhance patient compliance.
• US 4,865,851 describes a taste masked formulation of cefuroxime axetil where the drug particles are provided with integral coatings of a lipid or mixtures of lipids which are insoluble in water and which serve to mask the bitter taste of cefuroxime axetil upon oral administration.
• This coating however, results in a significant reduction in the dissolution and consequently the bioavailability of cefuroxime axetil suspension is significantly low as compared to tablet dosage form.
• the coating composition also contains lubricants which function as anti- sticking agents (e.g. talc, colloidal silica and magnesium stearate) and pharmaceutically acceptable plasticisers (e.g. triethyl citrate, polyethylene glycol, glyceryl monostearate, giyceryl triacetate, acetyl triethylcitrate, triethylcitrate, dibutyl phthalate and dibutyl sebacate).
• the lubricant quantity may be upto 200% of the dry weight of film-forming polymer, and more preferably, upto 100% of the dry weight of the film-forming polymer.
• the plasticiser quantity may be upto 40% the dry weight of the film forming polymer.
• the coated formulations may optionally be cured at elevated temperatures.
• a total polymer content in the coating of upto 30% by weight of pharmaceutical cores or, more preferably, 10% by weight of pharmaceutical cores is sufficient to mask the taste of bitter tasting, highly water soluble drugs.
• the total polymer content of the applied coat was 12.0% by weight of the core while the total solids applied was 26% by weight of the core.
• a total polymer coating of only 12% was sufficient to mask the bitter taste of Norfloxacin while giving optimum dissolution required for immediate release formulations. (Table 1.3).
• the total polymer content of the applied coat was 11.90% by weight of the core while the total solids application was 27% by weight of the core.
• the bitter taste of ciprofloxacin was masked with the applied coat without affecting dissolution, as shown in Table 5.3
• aqueous talc dispersion (30% w/w) was added to a 1% carbopol dispersion in water under stirring for 30 minutes.
• the carbopol - talc dispersion was finally added into plasticized (with triethyl citrate) ethyl cellulose dispersion with stirring for 30-40 minutes.

Landscapes

• Health & Medical Sciences (AREA)
• Epidemiology (AREA)
• Animal Behavior & Ethology (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Engineering & Computer Science (AREA)
• Life Sciences & Earth Sciences (AREA)
• Bioinformatics & Cheminformatics (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Priority Applications (3)

Applications Claiming Priority (2)

Publications (2)

Family

ID=11089863

Family Applications (1)

Country Status (7)

Cited By (7)

Family Cites Families (10)

• 1999
  • 1999-03-19 IN IN454DE1999 patent/IN191482B/en unknown
  • 1999-10-26 WO PCT/IB1999/001735 patent/WO2000056266A2/en not_active Ceased
  • 1999-10-26 BR BR9917219-4A patent/BR9917219A/pt not_active Application Discontinuation
  • 1999-10-26 CN CNA998165883A patent/CN1615121A/zh active Pending
  • 1999-10-26 AU AU62246/99A patent/AU6224699A/en not_active Abandoned
  • 1999-10-26 EP EP99949283A patent/EP1235556A4/en not_active Withdrawn
• 2001
  • 2001-09-19 ZA ZA200007724A patent/ZA200007724B/xx unknown

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