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

Patent metadata

Field	Value
Publication number	US-2016367501-A1
Application number	US-201615249574-A
Country	US
Kind code	A1
Filing date	Aug 29, 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

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 with a breaking strength of ≧500 N, wherein a mixture comprising the active ingredient and the binder is exposed 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 at least one active ingredient is at least one active ingredient selected from the group consisting of opioids, opiates, stimulants and further narcotics and the physiologically acceptable derivatives thereof.

4 . A process according to claim 3 , wherein the physiologically acceptable derivatives are salts, solvates, esters, ethers or amides.

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

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

7 . A process according to claim 1 , wherein the at least one binder is at least one synthetic or natural polymer and optionally a wax, in each case with a breaking strength of at least 500 N.

8 . A process according to claim 7 , 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.

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

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

11 . A process according to claim 1 , wherein, apart from the active ingredient with potential for abuse and the binder, the dosage form further comprises conventional auxiliary substances.

12 . A process according to claim 11 , wherein the dosage form comprises a plasticiser as the auxiliary substance.

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

14 . A process according to claim 1 , wherein there is direct contact between the mixture and the ultrasound source during ultrasonication.

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

16 . A process according to claim 1 , wherein shaping of the mixture proceeds by compaction during or after ultrasonication or by extrusion with rollers and/or by calendering during or after ultrasonication.

17 . A process according to claim 16 , wherein a force is applied for the purpose of compaction.

18 . A process according to claim 16 , wherein, for compaction, the mixture is already in the form of powder, pellets, microparticles or granules, which have been produced by conventional processes.

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

20 . A process according to claim 1 , wherein the mixture is shaped into a multiparticulate final shape.

Assignees

• Gruenenthal Gmbh

Inventors

• Arkenau-Maric Elisabeth
• Bartholomäus Johannes
• Kugelmann Heinrich

Classifications

• A61P25/04

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

• A61K31/135 Primary

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

• B29L2031/00

  Other particular articles · CPC title

• A61K9/2095

  Tabletting processes · CPC title

• A61K47/34

  Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence) · CPC title