Process for the production of an abuse-proofed solid dosage form

Patent metadata

Field	Value
Publication number	US-2016367484-A1
Application number	US-201615252764-A
Country	US
Kind code	A1
Filing date	Aug 31, 2016
Priority date	Apr 22, 2004
Publication date	Dec 22, 2016
Grant date	—

Abstract

The present invention relates to a process for the production of an abuse-proofed solid dosage form containing at least one active ingredient with potential for abuse and a binder with a breaking strength of ≧500 N, by exposing a mixture comprising the active ingredient and the binder to ultrasound and force.

First claim

What is claimed:

1 . A process for the production of an abuse-proofed solid dosage form comprising at least one active ingredient with potential for abuse and at least one binder, the at least one active ingredient with potential for abuse being selected from the group consisting of oxymorphone and physiologically acceptable compounds and derivatives thereof, said dosage form having a breaking strength of at least 500 N, and said process comprising exposing a mixture comprising the at least one active ingredient and the at least one binder to ultrasound and force.

2 . A process according to claim 1 , wherein the dosage form is an oral dosage form.

3 . A process according to claim 1 , wherein the physiologically acceptable compounds and derivatives are selected from the group consisting of salts, solvates, esters, ethers and amides.

4 . A process according to claim 1 , wherein the active ingredient with potential for abuse is selected from the group consisting of morphine, hydromorphone, and the physiologically acceptable salts thereof.

5 . A process according to claim 1 , wherein the binder is present in a quantity of at least 20 wt. % relative to the total weight of the dosage form.

6 . A process according to claim 1 , wherein the binder is at least one synthetic or natural polymer and optionally a wax.

7 . A process according to claim 6 , wherein the polymer exhibits a viscosity at 25° C. of 4500 to 17600 cP, measured on a 5 wt. % aqueous solution with the assistance of a Brookfield viscosimeter.

8 . A process according to claim 7 , wherein the polymer is at least one polymer selected from among the group consisting of polyethylene oxides, polyethylenes, polypropylenes, polyvinyl chlorides, polycarbonates, polystyrenes, polyacrylates and the copolymers thereof.

9 . A process according to claim 8 , wherein the polymer is a polyethylene oxide and the polyethylene oxide has a molecular weight of at least 1 million g/mol.

10 . A process according to claim 1 , wherein, apart from the active ingredient with potential for abuse and the binder, the dosage form also comprises at least one further auxiliary substance.

11 . A process according to claim 10 , wherein the at least one further auxiliary substance is a plasticiser.

12 . A process according to claim 1 , wherein the ultrasound has a frequency of 1 kHz to 2 MHz.

13 . A process according to claim 1 , wherein the mixture directly contacts the ultrasound source during ultrasonication.

14 . A process according to claim 1 , wherein ultrasonication proceeds until the binder has softened.

15 . A process according to claim 1 , which further comprises shaping the mixture by compaction during or after ultrasonication or by extrusion with rollers and/or by calendering during or after ultrasonication.

16 . A process according to claim 15 , which further comprises applying a force for the purpose of compaction.

17 . A process according to claim 15 , which further comprises compaction, wherein the mixture is in the form of powder, pellets, microparticles or granules.

18 . A process according to claim 1 , which further comprises shaping the mixture into tablets.

19 . A process according to claim 1 , which further comprises shaping the mixture into a multiparticulate final shape.

Assignees

• Gruenenthal Gmbh

Inventors

• Arkenau-Maric Elisabeth
• Bartholomäus Johanness
• Kugelmann Heinrich

Classifications

• A61P25/04

  Centrally acting analgesics, e.g. opioids · CPC title

• B29L2031/00

  Other particular articles · CPC title

• A61K31/135 Primary

  having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)} · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title

• A61J3/10

  into the form of compressed tablets (tablet presses B30B11/00) · CPC title