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
  • A61K9/2004—Excipients; Inactive ingredients
  • A61K9/2022—Organic macromolecular compounds
  • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
  • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
• • 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
  • A61K31/13—Amines
• • 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
• • 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
  • 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
  • A61K9/2022—Organic macromolecular compounds
  • A61K9/2027—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
  • A61K9/20—Pills, tablets, discs, rods
  • A61K9/2004—Excipients; Inactive ingredients
  • A61K9/2022—Organic macromolecular compounds
  • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
  • A61K9/2054—Cellulose; Cellulose derivatives, 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
  • A61K9/20—Pills, tablets, discs, rods
  • A61K9/2095—Tabletting processes
• • 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
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
  • A61P25/04—Centrally acting analgesics, e.g. opioids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P25/00—Drugs for disorders of the nervous system
  • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

Definitions

• Patent Document 2 describes an orally disintegrating tablet containing drug-granulated particles wet-granulated by adding an aqueous solution containing a monosaccharide to a drug-containing powder. Describes that crystalline cellulose and corn starch, which are poorly soluble components, are preferably blended, and in particular, crystalline cellulose can be suitably used because it has the property of improving the friability of tablets with a small blend. In this document, it is essential to wet granulate a drug-containing powder with an aqueous solution containing a water-soluble monosaccharide, thereby obtaining excellent moldability and disintegration as an orally disintegrating tablet. It is described that it can.
• the other subject of this invention provides the method excellent in industrial productivity which manufactures the orally disintegrating tablet which has the above outstanding characteristics by normal compression molding, without requiring special equipment. There is.
• An orally disintegrating tablet obtained by compression molding a drug-free granule containing crystalline cellulose having a bulk density of 0.23 g / cm 3 or less, sugar alcohol and pregelatinized starch, and the drug or drug-containing granule.
• a drug-free granule is obtained by granulating a mixed powder containing crystalline cellulose having a bulk density of 0.23 g / cm 3 or less and sugar alcohol with a solution in which pregelatinized starch is dissolved or dispersed.
• loxoprofen sodium hydrate used as an antipyretic analgesic anti-inflammatory agent carvedilol used as an anti-cardiac insufficiency drug or antihypertensive drug, bisoprolol fumarate, olmesartan medoxomil, azilsartan used as an antihypertensive drug, antihyperlipidemic drug Pravastatin sodium used as an antibacterial agent, levofloxacin hydrate used as an antibacterial agent, sitafloxacin hydrate, edoxabantosilate hydrate used as an anticoagulant, memantine used as a treatment for Alzheimer's dementia or its pharmacology It is suitable for a topically acceptable salt (particularly memantine hydrochloride), donepezil or a pharmacologically acceptable salt thereof (particularly donepezil hydrochloride), and hydromorphone used as a therapeutic agent for cancer pain.
• a topically acceptable salt particularly memantine hydrochloride
• One or more selected from acid copolymer LD, methacrylic acid copolymer S, aminoalkyl methacrylate copolymer RS, aminoalkyl methacrylate copolymer RS, ethyl acrylate / methyl methacrylate copolymer, polyvinyl acetal / diethylamino acetate, and polyvinyl acetate resin Can be mentioned.
• soot foaming agents examples include tartaric acid and / or anhydrous citric acid.
• A-3 Step of mixing and compression-molding drug-free granules, drug or drug-containing granules and other additives
• Drug-free granules, drug or drug-containing granules and optionally disintegrants, lubricants, other Additives are mixed and compression molded to make an orally disintegrating tablet.
• Mixing is performed by using, for example, a tumble mixer or a convection mixer.
• the blending ratio of the drug-free granules to the total weight of the tablet components may be 30 to less than 100%.
• the blending ratio of the drug-free granules is 60 to less than 100%, and when the drug is granulated and used, it is 30 to 85%, preferably 35 to 80%.
• the blending weight ratio between the drug-free granule and the drug-containing granule is preferably 0.5 to 5.0 with respect to the drug-containing granule 1.
• the drug-containing granule provides desirable disintegration and moldability as an orally disintegrating tablet. You may mix
• Example 4 2880g of D-mannitol (Merck) and 2000g of crystalline cellulose (Asahi Kasei Chemicals, Theolas KG-1000, bulk density 0.10-0.15g / cm 3 ) were put into a fluidized bed granulator (Freund, FLO-5). A granulated product was obtained by spraying a solution obtained by dispersing 200 g of pregelatinized starch (manufactured by Asahi Kasei Chemicals Co., Ltd., swelstar PD-1) in 2300 g of purified water and then drying.
• pregelatinized starch manufactured by Asahi Kasei Chemicals Co., Ltd., swelstar PD-1
• Example 11 455 g of the granulated product obtained in the same manner as in the previous stage of Example 3 and 40 g of carmellose calcium (manufactured by Gotoku Pharmaceutical, ECG-505) were mixed to obtain a mixture. After mixing 5 g of magnesium stearate (manufactured by Marinck Rod) with 495 g of the obtained mixture, tableting was performed with a tableting pressure of 8 kN using a rotary tableting machine, and an orally disintegrating tablet (tablet diameter 9 mm ⁇ , mass 280 mg) was obtained. Obtained.
• Example 17 4.89 g of the drug-containing coating obtained by the same method as in the previous stage of Example 16, 2.91 g of the granulated product obtained by the same method as in the previous stage of Example 3, 0.52 g of crospovidone (BASF, Kollidon CL-F) Were mixed to obtain a mixture. After mixing 8.84 g of the obtained mixture with 0.084 g of magnesium stearate (manufactured by Marinck Rod), tableting was performed with a single tableting machine at a tableting pressure of 10 kN to obtain an orally disintegrating tablet (9 mm ⁇ , 280 mg). It was.
• the wrinkle hardness was measured with a tablet continuous measuring device (WHT: manufactured by Pharm Test) (the average value of 10 tablets is described).

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Chemical & Material Sciences (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Animal Behavior & Ethology (AREA)
• Pharmacology & Pharmacy (AREA)
• Medicinal Chemistry (AREA)
• Epidemiology (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Molecular Biology (AREA)
• Biophysics (AREA)
• Zoology (AREA)
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• Nutrition Science (AREA)
• Neurosurgery (AREA)
• Biomedical Technology (AREA)
• Neurology (AREA)
• General Chemical & Material Sciences (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Psychiatry (AREA)
• Hospice & Palliative Care (AREA)
• Pain & Pain Management (AREA)
• Medicinal Preparation (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

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Cited By (15)

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• 2013
  • 2013-04-23 BR BR112014026292-6A patent/BR112014026292B1/pt active IP Right Grant
  • 2013-04-23 CN CN201380021692.1A patent/CN104244930A/zh active Pending
  • 2013-04-23 KR KR1020147028967A patent/KR101943686B1/ko active Active
  • 2013-04-23 IN IN2029MUN2014 patent/IN2014MN02029A/en unknown
  • 2013-04-23 EP EP13781585.8A patent/EP2842549B1/en active Active
  • 2013-04-23 US US14/395,428 patent/US9827200B2/en active Active
  • 2013-04-23 ES ES13781585.8T patent/ES2694224T3/es active Active
  • 2013-04-23 WO PCT/JP2013/061936 patent/WO2013161823A1/ja not_active Ceased
  • 2013-04-23 JP JP2014512615A patent/JP6066351B2/ja active Active
  • 2013-04-23 CA CA2870868A patent/CA2870868C/en active Active
  • 2013-04-23 CN CN201710256576.8A patent/CN106913553A/zh active Pending
  • 2013-04-24 TW TW102114513A patent/TWI572371B/zh active
• 2016
  • 2016-10-17 JP JP2016203530A patent/JP6325627B2/ja active Active
• 2018
  • 2018-01-22 JP JP2018008108A patent/JP6545839B2/ja active Active
• 2019
  • 2019-06-19 JP JP2019113467A patent/JP7028829B2/ja active Active

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