Analgetic compositions

• US 3,966,940 A
• Filed: 09/02/1975
• Issued: 06/29/1976
• Est. Priority Date: 11/09/1973
• Status: Expired due to Term

• Current Assignee: Bristol Myers Co (Bristol-Myers Squibb Company)
• Original Assignee: Bristol Myers Co (Bristol-Myers Squibb Company)
• Inventors: Gordon, Maxwell, Pachter, Irwin J.
• Primary Examiner(s): Drezin, Norman A.
• Application Number:
  US05/609,847
• Time in Patent Office: 301 Days
• Field of Search: 424/260, 424/10, 424/330
• US Class Current: 514/282
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• 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 31/22 of acyclic acids, e.g. pravastatin
• CPC Class Codes: A61K 31/435 having six-membered rings with one nitrogen as the only ring hetero atom
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine

Abstract

Orally effective, analgetic compositions have been developed which are useful in the prevention of drug abuse because upon parenteral administration, they do not produce analgesia, euphoria, or physical dependence. Such compositions comprise an orally active, strong analgetic in oral dosage form and containing, for each analgetic dose of the analgetic agent, an amount of naloxone sufficient, upon parenteral administration of said oral dosage form, to negate the analgetic, euphoretic and dependence producing action of the composition, but insufficient to block the therapeutic effect of the analgetic when the admixture is taken orally.

Claims

1. A method for the treatment of a narcotic-addicted subject which comprises orally administering to said subject an effective amount of a composition consisting essentially of (a) a narcotic selected from the group consisting of α

-dl-methadol, β

-dl-methadol, α

-1-methadol, β

-dl-acetylmethadol, α

-1-acetylmethadol and β

-1-acetylmethadol in an amount sufficient to substantially prevent narcotic craving and (b) naloxone in an amount sufficient to induce withdrawal symptoms when said composition is administered parenterally but insufficient to negate the action of said methadone when the composition is administered orally.

2. The method of claim 1 wherein said narcotic is α

-1-acetylmethadol.

3. The method of claim 2 wherein the weight ratio of α

-1-acetylmethadol to naloxone is from about 2.5;

1 to about 25;

1.

4. The method of claim 2 wherein said composition comprises from about 0.1 to about 10 milligrams of naloxone per analgetic oral dose of α

-1-acetylmethadol.