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
• • 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
  • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
  • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat

Definitions

• PCT publication WO2007078895 (Biovail Laboratories) relates to a specific type of controlled and modified release dosage form containing tramadol or at least one pharmaceutically acceptable salt, enantiomer, or metabolite-thereof, that passes the specific pharmacokinetic properties and which desirably are not subject to the dose dumping, e.g, induced by food or alcohol.
• '3991 discloses a controlled release oral solid dosage form comprising: a matrix comprising a therapeutically effective amount of Venlafaxine, an active metabolite of Venlafaxine or a pharmaceutically acceptable salt thereof, dispersed in a cross linked agent, said matrix providing a controlled release of Venlafaxine, active metabolite of Venlafaxine, or salt thereof to provide 24 hour therapeutic plasma levels after oral administration to human patients.
• the '3991 application relates to controlled release dosage forms containing therapeutically effective amount of Venlafaxine, an active metabolite of venlafaxine which are resistant to alcohol induced dose dumping.
• United States Patent application US20070264346 discloses an oral pharmaceutical or dietetic form comprising microparticles of the reservoir type for the modified release of at least one active principle (AP), characterized in that it is resistant to immediate dumping of the dose of the AP in the presence of alcohol.
• AP active principle
• the present invention also provides use of a therapeutically active ingredient in the manufacture of an oral controlled release tablet; said tablet comprising:
• upper compressed layer comprising a swelling agent
• a coating surrounding the said core comprising a polymer insoluble in an aqueous medium comprising from 0 % v/v to 40% v/v of alcohol content, whereby upon contact with aqueous gastrointestinal fluids, the upper compressed layer and the bottom compressed layer swell to cause removal of the coating from the upper surface of the upper compressed layer and the lower surface bottom compressed layer of the tablet and then said upper layer and the said bottom layer disintegrate, allowing the release of the active ingredient from the defined surface area of the upper and lower surface of said middle compressed layer with the coating covering its side surfaces.
• the amount of excipients that are soluble in alcohol does not exceed 40 % by weight of the compressed layer that comprising active ingredient and release rate controlling excipients. More particularly, the said amount of alcohol soluble excipients does not exceed 35 % by weight of the said compressed layer.
• the compressed layer comprising swelling agent additionally may comprise other excipients such as surfactants, lubricants, and other excipients commonly used in the pharmaceutical art.
• the upper compressed layer may optionally, include same or a different therapeutically active ingredient to cause a rapid release followed by a controlled release from the lower compressed layer comprising release rate controlling excipients. It may be noted that the upper compressed layer comprising swelling agent or the bottom compressed layer comprising swelling agents may have same of different composition.
• the coating may comprises one or more plasticizers.
• the plasticizers may be those that are conventionally used in the pharmaceutical art. These may be hydrophilic or hydrophobic in nature. Examples of hydrophilic plasticizer that may be used in the coating, include, but are not limited to, triethyl citrate, triethyl acetyl citrate, triacetin, tributyl citrate, polyethylene glycol 6000, polysorbate 80, glycerol and the like and mixtures thereof.
• Figure 1 Specific embodiments where the coating has a preformed passageway, for example, laser drilled passageway, are illustrated in Figure 1.
• the term "without a substantial delay” as used herein means that the active ingredient release is initiated from the oral controlled release tablet of the present invention within 0 to 60 minutes from the time the tablet contacts an aqueous environment, preferably within 0 to 20 minutes, and most preferably within 0 to 5 minutes.
• Such embodiments are described in our co-pending PCT application, WO2005039481 which is incorporated herein as reference.
• the coating comprises one or more polymers that are insoluble in an aqueous medium having 0 % v/v to 40 % v/v alcohol, leachable components and other conventional coating additives such as plasticizers, colour and mixtures thereof and the like.
• leachable components include water soluble inorganic compounds and water soluble organic compounds. More specifically inorganic leachable compounds include, for example, sodium chloride, sodium bromide, sodium carbonate, potassium chloride, potassium sulfate, potassium phosphate, potassium nitrate, calcium phosphate, calcium nitrate, calcium chloride, and the like.
• Oral controlled release tablets were prepared using the ingredients listed in the Table 1 below.

Landscapes

• Health & Medical Sciences (AREA)
• Epidemiology (AREA)
• Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Life Sciences & Earth Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Engineering & Computer Science (AREA)
• Medicinal Preparation (AREA)

Priority Applications (7)

Applications Claiming Priority (2)

Publications (2)

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ID=40955347

Family Applications (1)

Country Status (10)

Cited By (4)

Families Citing this family (15)

Family Cites Families (32)

• 2009
  • 2009-02-16 CA CA2715584A patent/CA2715584A1/en not_active Abandoned
  • 2009-02-16 JP JP2010546446A patent/JP2011512349A/ja active Pending
  • 2009-02-16 KR KR1020107019012A patent/KR20100136967A/ko not_active Withdrawn
  • 2009-02-16 BR BRPI0908114A patent/BRPI0908114A2/pt not_active IP Right Cessation
  • 2009-02-16 WO PCT/IN2009/000106 patent/WO2009122431A2/en not_active Ceased
  • 2009-02-16 MX MX2010008861A patent/MX2010008861A/es not_active Application Discontinuation
  • 2009-02-16 CN CN2009801103021A patent/CN102026628A/zh active Pending
  • 2009-02-16 EP EP09727912.9A patent/EP2242485A4/en not_active Withdrawn
  • 2009-02-17 US US12/372,161 patent/US20090208572A1/en not_active Abandoned
• 2010
  • 2010-09-22 ZA ZA2010/06793A patent/ZA201006793B/en unknown

Non-Patent Citations (1)

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