Process for the production of an abuse-proofed dosage form

Patent metadata

Field	Value
Publication number	US-2016367487-A1
Application number	US-201615257079-A
Country	US
Kind code	A1
Filing date	Sep 6, 2016
Priority date	Dec 24, 2003
Publication date	Dec 22, 2016
Grant date	—

Abstract

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

First claim

1 . A process for the production of a solid pharmaceutic dosage forms with at least reduced potential for abuse, comprising:
a) a formulation mixture containing at least one active ingredient with potential for abuse, at least one synthetic or natural polymer (C), which exhibits a breaking strength of at least 500 N, and optionally auxiliary substances (B) is shaped into formed articles by application of force, b) the formed articles are optionally singulated and optionally in each case graded by size and, c) after or during heating at least to the softening point of the polymer (C), the formed articles are exposed to force until they have a breaking hardness of at least 500 N, and optionally provided with a cover and all the formed articles are optionally mixed back together again.

2 . A process according to claim 1 , which is performed continuously or discontinuously.

3 . A process according to claim 1 , wherein the formulation mixture consists to an extent of at least 30 wt. % of component (C).

4 . A process according to claim 1 , wherein the formulation mixture consists to an extent of at least 50 wt. % of component (C).

5 . A process according to claim 1 , wherein a) shaping of the formulation mixture proceeds with application of a force of at least 0.5 kN and optionally with heating to less than 60° C.

6 . A process according to claim 1 , wherein, according to c), the formed articles are heated to at least 60° C before or during application of force of at least 0.1 kN.

7 . A process according to claim 1 , wherein the application of force according to a) or c) is performed with the assistance of a press, shaping rollers or with shaping belts equipped with rollers.

8 . A process according to claim wherein shaping according to a) gives rise to tablets.

9 . A process according to claim 1 , wherein shaping according to a) gives rise to a multiparticulate dosage form with a minimum size of 0.5 mm.

10 . A process according to claim 1 , wherein opioid active ingredients are used as active ingredients.

Assignees

• Gruenenthal Gmbh

Inventors

• Arkenau-Maric Elisabeth
• Bartholomäus Johannes

Classifications

• A61P25/04

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

• A61P25/36

  Opioid-abuse · CPC title

• A61P25/30

  for treating abuse or dependence · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61K9/2054

  Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose · CPC title