Controlled release dosage forms

• US 7,780,987 B2
• Filed: 02/21/2003
• Issued: 08/24/2010
• Est. Priority Date: 02/21/2002
• Status: Active Grant

• Current Assignee: Bausch Health Ireland Limited (Bausch Health Cos., Inc.)
• Original Assignee: Biovail Laboratories International Srl (Bausch Health Cos., Inc.)
• Inventors: Zhou, Fang, Maes, Paul
• Primary Examiner(s): TRAN, SUSAN T
• Application Number:
  US10/370,109
• Publication Number:
  US 20040037883A1
• Time in Patent Office: 2,741 Days
• Field of Search: 424/451, 424/464
• US Class Current: 424/475
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/155 Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2846 Poly(meth)acrylates
• CPC Class Codes: A61K 9/2853 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 29/02 without antiinflammatory effect
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The invention provides stable controlled release monolithic coating compositions for use in coating pharmaceutical oral dosage forms comprising a polyglycol having a melting point greater than 55° C. and an aqueous dispersion of a neutral ester copolymer lacking functional groups.

Claims

1. A pharmaceutical oral dosage form comprising an oral dosage form coated with a stable controlled release monolithic coating, wherein the stable controlled release monolithic coating is applied onto the oral dosage form by a process comprising

coating the oral dosage form with a coating composition to form a coated oral dosage form, and

curing the coated oral dosage form at a temperature of at least 55°

C. to form the stable controlled release monolithic coating,

wherein the coating composition consists essentially of

a neutral ester copolymer in an amount of from about 1% to about 35% by weight of the coating composition based on ethyl acrylate and methyl acrylate selected from the group consisting of a 30% aqueous dispersion of a neutral ester copolymer based on ethyl acrylate and methyl methacrylate, a 40% aqueous dispersion of a neutral ester copolymer based on ethyl acryl ate and methyl methacrylate, and combinations thereof;

a polyethylene glycol selected from the group consisting of polyethylene glycol 6000, polyethylene glycol 8000, polyethylene glycol 10000, polyethylene glycol 20000, and combinations thereof in an amount of from about 0.1% to about 3% by weight of the coating composition; and

one or more of a hydrophilic agent, and a pharmaceutically acceptable excipient.

2. The pharmaceutical dosage form of claim 1, wherein said pharmaceutical dosage form is selected from the group consisting of a tablet and a capsule.

3. The pharmaceutical oral dosage form of claim 1, wherein the oral dosage form comprises metformin, a pharmaceutically acceptable salt thereof, or a combination thereof.

4. A method of manufacturing a pharmaceutical oral dosage form coated with a stable controlled release monolithic coating, the method comprising

coating the oral dosage form with a coating composition to form a coated oral dosage form, and

curing the coated oral dosage form at a temperature of at least 55°

C. to form the stable controlled release monolithic coating,

wherein the coating composition consists essentially of

a neutral ester copolymer based on ethyl acrylate and methyl acrylate selected from the group consisting of a 30% aqueous dispersion of a neutral ester copolymer based on ethyl acrylate and methyl methacrylate, a 40% aqueous dispersion of a neutral ester copolymer based on ethyl acrylate and methyl methacrylate, and combinations thereof in an amount of from about 1% to about 35% by weight of the coating composition;

a polyethylene glycol selected from the group consisting of polyethylene glycol 6000, polyethylene glycol 8000, polyethylene glycol 10000, polyethylene glycol 20000, and combinations thereof in an amount of from about 0.1% to about 3% by weight of the coating composition; and

one or more of a hydrophilic agent, and a pharmaceutically acceptable excipient.

5. The method of claim 4, wherein said pharmaceutical dosage form is selected from the group consisting of a tablet and a capsule.

6. The method of claim 4, wherein the oral dosage form comprises metformin, a pharmaceutically acceptable salt thereof, or a combination thereof.