Abuse-proofed dosage form

• US 10,130,591 B2
• Filed: 09/14/2016
• Issued: 11/20/2018
• Est. Priority Date: 08/06/2003
• Status: Expired due to Term

• Current Assignee: Grunenthal GMBH (Grünenthal Pharma GmbH & Co. KG)
• Original Assignee: Grunenthal GMBH (Grünenthal Pharma GmbH & Co. KG)
• Inventors: Bartholomaus, Johannes, Kugelmann, Heinrich, Arkenau-Maric, Elisabeth
• Primary Examiner(s): Hartley, Michael G
• Assistant Examiner(s): Perreira, Melissa J
• Application Number:
  US15/265,263
• Publication Number:
  US 20170000739A1
• Time in Patent Office: 797 Days
• Field of Search: None
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/515 Barbituric acids; Derivatives thereof, e.g. sodium pentobarbital
• CPC Class Codes: A61K 31/5513 1,4-Benzodiazepines, e.g. diazepam or clozapine
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61K 9/20 Pills, tablets, discs, rods A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• 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 9/205 Polysaccharides, e.g. alginate, gums; Cyclodextrin
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2068 Compounds of unknown constitution, e.g. material from plants or animals oils, fats, waxes, shellac A61K9/2013
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/22 Anxiolytics
• CPC Class Codes: A61P 25/30 for treating abuse or dependence

Abstract

The present invention relates to an abuse-proofed, thermoformed dosage form containing, in addition to one or more active ingredients with abuse potential optionally together with physiologically acceptable auxiliary substances, at least one synthetic or natural polymer with a breaking strength of at least 500 N and to a process for the production thereof.

Claims

1. An abuse-proofed, thermoformed dosage form having a breaking strength of at least 500 N, said dosage form being in the form of a tablet obtained by a process comprising:

a) mixing;

i) an opioid or a physiologically acceptable salt thereof;

ii) optionally physiologically acceptable substances (B);

iii) at least one polyalkylene oxide (C) having a molecular weight of 1-15 million according to rheological measurements, wherein the content of component (C) is at least 60 wt. %, relative to the total weight of the tablet; and

iv) optionally at least one wax (D);

to form a resultant mixture;

b) press-forming the resultant mixture to form a press-formed product; and

c) exposing the press-formed product to heat to yield the dosage form.

2. A dosage form according to claim 1, wherein the opioid or physiologically acceptable salt thereof is oxycodone or a physiologically acceptable salt thereof.

3. A method of treating pain in a patient suffering therefrom, said method comprising administering to said patient a dosage form according to claim 1.

4. A dosage form according to claim 1, wherein the opioid or physiologically acceptable salt thereof is morphine or a physiologically acceptable salt thereof.

5. A method according to claim 3, wherein the opioid or physiologically acceptable salt thereof is oxycodone or a physiologically acceptable salt thereof.

6. A method according to claim 3, wherein the opioid or physiologically acceptable salt thereof is morphine or a physiologically acceptable salt thereof.