Analgesic compositions

• US 4,582,835 A
• Filed: 12/05/1984
• Issued: 04/15/1986
• Est. Priority Date: 12/06/1983
• Status: Expired due to Term

• Current Assignee: Reckitt Benckiser Healthcare Limited (Reckitt Benckiser Group PLC)
• Original Assignee: Reckitt & Colman Products Limited (Reckitt Benckiser Group PLC)
• Inventors: Lewis, John W., Lloyd-Jones, John G.
• Primary Examiner(s): Friedman, Stanley J.
• Application Number:
  US06/678,478
• Time in Patent Office: 496 Days
• Field of Search: 424/10, 424/260, 514/282, 514/812
• US Class Current: 514/282
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61K 9/0056 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
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

A method of treating pain which comprises the administration to a patient of a parenterally or sublingually effective dose of buprenorphine together with an amount of naloxone sufficient to prevent substitution in an opiate dependent subject. Preferably when the administration is parenteral the weights of naloxone and buprenorphine are within the ratio of 1:3 to 1:1 and when administered sublingually the weights are within the ratio of 1:2 to 2:1.

Claims

1. A method of treating pain which comprises the administration to a patient of a parenterally effective unit dosage of buprenorphine wherein the weight of buprenorphine is between about 0.3 to about 0.6 mg and simultaneously an amount of naloxone sufficient to prevent substitution in an opiate dependent subject, the weights of naloxone and buprenorphine administered parenterally being within the ratio of 1:

3 to 1;

1.

2. A method of treating pain which comprises the administration to a patient of a sublingually effective unit dosage of buprenorphine wherein the weight of buprenorphine is between about 0.1 to about 0.6 mg and simultaneously an amount of naloxone sufficient to prevent substitution in an opiate dependent subject, the weights of naloxone and buprenorphine administered sublingually being within the ratio of 1:

2 to 2;

1.

3. An analgesic composition in parenteral unit dosage form comprising an active dose of buprenorphine of from about 0.3 to about 0.6 mg and an amount of naloxone sufficient to prove aversive to a narcotic addict by parenteral administration but insufficient to compromise the analgesic action of the buprenorphine, the weights of naloxone and buprenorphine being within the ratio of 1:

3 to 1;

1.

4. An analgesic composition in sublingual unit dosage form comprising an active dose of buprenorphine of from about 0.1 to about 0.6 mg and an amount of naloxone sufficient to prove aversive to a narcotic addict by parenteral administration but insufficient to compromise the analgesic action of the buprenorphine, the weights of naloxone and buprenorphine being within the ratio of 1:

2 to 2;

1.