Analgesic tablet compositions

• US 6,284,274 B1
• Filed: 03/03/2000
• Issued: 09/04/2001
• Est. Priority Date: 02/28/1997
• Status: Expired due to Fees

• Current Assignee: Encinal Pharmaceutical Investments, LLC
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Hwang, Paul M., Merrill, Sonya, Johnson, Deborah J., Ahlgren, Nils W., Ayer, Atul D., Kuczynski, Anthony L.
• Primary Examiner(s): Jarvis, William R. A.
• Application Number:
  US09/518,584
• Time in Patent Office: 550 Days
• Field of Search: 424/464, 424/472, 424/468
• US Class Current: 424/472
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• 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 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Abstract

An opiate analgesic composition and a non-opiate analgesic composition are disclosed for delivering an analgesic in either embodiment to a patient in need of relief from pain. The analgesics are present optionally with a nonionic surfactant and with an osmotic composition comprising a carbonate or bicarbonate for delivering the opiate analgesic and non-opiate analgesic from a dosage form.

Claims

1. An osmotic composition comprising 30 to 225 mg of a member selected from the group consisting of sodium carboxymethylcellulose, potassium carboxymethylcellulose and calcium carboxymethylcellulose of 75,000 to 2,500,000 molecular weight, 25 to 150 mg of a member selected from the group consisting of a alkali metal carbonate, alkali metal bicarbonate, alkaline earth carbonate and alkaline earth bicarbonate, 1 to 30 mg of hydroxypropylmethylcellulose of 9,200 to 125,000 molecular weight, 1 to 30 mg of hydroxypropylcellulose of 7,500 to 125,000 molecular weight and 0.1 to 3 mg of a lubricant.

2. A bilayer tablet comprising a first layer comprising 50 ng to 1000 mg of an opiate analgesic, 35 to 275 mg of a poly(alkylene oxide) of 100,000 to 650,000 molecular weight, 0.5 to 50 mg of a poly(vinyl pyrrolidone) of 7,500 to 225,000 molecular weight, 0.1 to 10 mg of a lubricant selected from the group consisting of magnesium stearate, calcium stearate, potassium oleate, and sodium stearate;

and a second layer comprising 30 to 225 mg of a carboxymethylcellulose of 75,000 to 2,500,000 molecular weight, 25 to 150 mg of a member selected from the group consisting of lithium carbonate, sodium carbonate, potassium carbonate, lithium bicarbonate, sodium bicarbonate, potassium bicarbonate, and magnesium bicarbonate, 1 to 30 mg of a hydroxypropylmethylcellulose of 9,200 to 125,000 molecular weight and 1 to 30 mg of a hydroxypropylcellulose of 7,500 to 125,000 molecular weight.

3. A bilayer tablet comprising a first layer comprising 50 ng to 1,000 mg of a opiate analgesic, 35 to 275 mg of a poly(alkylene oxide) of 100,000 to 650,000 molecular weight, 0.5 to 50 mg of a poly(vinyl pyrrolidone) of 7,500 to 225,000 molecular weight, and 0.01 to 0.5 mg of an antioxidant;

and a second layer comprising 30 to 375 mg of a poly(alkylene oxide) of 3,000,000 to 10,000,000 molecular weight, 25 to 150 of a member selected from the group consisting of a carbonate and bicarbonate, 1 to 60 mg of a hydroxypropylmethylcellulose of 9,200 to 125,000 molecular weight and 0.01 to 3 mg of an antioxidant.

4. A bilayer tablet comprising a first layer comprising 50 ng to 1,000 mg of a non-opiate analgesic selected from the group consisting of alfentanil, ketoprofen, buprenorphine, butorphanol, fentanyl, meperidine, methadone, nalbuphine, propoxyphene, natrexone, pentazocine, sufentanil, acetaminophen, aspirin, ibuprofen, and naproxen, 35 to 275 mg of a poly(ethylene oxide) of 100,000 to 650,000 molecular weight, 0.5 to 50 mg of a poly(vinyl pyrrolidone) of 7,500 to 225,000 molecular weight, and 0 to 10 mg of a nonionic surfactant;

and second layer possessing aqueous-fluid imbibing property comprising 30 to 225 mg of a carboxymethylcellulose of 75,000 to 2,500,000 molecular weight, 25 to 150 mg of a member selected from the group consisting of lithium carbonate, sodium carbonate, potassium carbonate, lithium bicarbonate, sodium bicarbonate, potassium bicarbonate, and magnesium bicarbonate, 1 to 30 mg of a hydroxypropylalkylcellulose of 9,200 to 125,000 molecular weight, and 1 to 30 mg of a hydroxypropylcellulose of 7,500 to 125,000 molecular weight, and 0 to 5 mg of an antioxidant.

5. A bilayer tablet comprising a first layer comprising 50 ng to 1,000 mg of a non-opiate analgesic selected from the group consisting of alfentanil, ketoprofen, buprenorphine, butorphanol, fentanyl, meperidine, methadone, nalbuphine, propoxyphene, natrexone, pentazocine, sufentanil, acetaminophen, aspirin, ibuprofen, and naproxen, 35 to 275 mg of a poly(ethylene oxide) of 100,000 to 650,000 molecular weight, 0.5 to 50 mg of a poly(vinyl pyrrolidone) of 7,500 to 225,000 molecular weight, and 0 to 10 mg of a nonionic surfactant;

and second layer possessing aqueous-fluid imbibing properties consisting of 30 to 375 mg of a poly(alkylene oxide) possessing a 3,000,000 to 10,000,000 molecular weight, 25 to 150 mg of a member selected from the group consisting of lithium carbonate, sodium carbonate, potassium carbonate, lithium bicarbonate, sodium bicarbonate, potassium bicarbonate, and magnesium bicarbonate, 1 to 60 mg of a hydroxypropylalkylcellulose of 9,200 to 125,000 molecular weight, 0 to 60 mg of a hydroxypropylcellulose of 7,500 to 125,000 molecular weight, and 0.01 to 3 mg of an antioxidant.