Process for the production of an abuse-proofed dosage form

Patent metadata

Field	Value
Publication number	US-11224576-B2
Application number	US-201615257079-A
Country	US
Kind code	B2
Filing date	Sep 6, 2016
Priority date	Dec 24, 2003
Publication date	Jan 18, 2022
Grant date	Jan 18, 2022

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

The invention claimed is:

1. A process of forming a tablet with a reduced potential for abuse, said process comprising:
a) producing a formed tablet by shaping a formulation mixture by application of force on a tablet press, wherein the formulation mixture comprises:
i) at least one active ingredient with potential for abuse;
ii) at least one polymer (C), which polymer (C) is a polyalkylene oxide having a molecular weight of at least 0.5 million g/mol, and exhibiting a breaking strength of at least 500 N; and
iii) optionally, one or more auxiliary substances (B); and

b) exposing the formed tablet to force i) during heating at least to the softening point of the polymer (C) or ii) after said heating while the formed tablet is still at a temperature at least at the softening point of the polymer (C), said exposing the formed tablet to force continuing until the formed tablet has a breaking hardness of at least 500N, and optionally providing the formed tablet with a cover, and optionally mixing the formed tablet with other formed tablets.

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 polymer (C).

4. A process according to claim 1 , wherein the formulation mixture consists to an extent of at least 50 wt. % of polymer (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 b), 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 b) is performed with the assistance of a press, shaping rollers or with shaping belts equipped with rollers.

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

Assignees

• Gruenenthal Gmbh

Inventors

• Arkenau-Marić Elisabeth
• Bartholomäus Johannes

Classifications

• A61K31/485 Primary

  Morphinan derivatives, e.g. morphine, codeine · CPC title

• A61K9/2095 Primary

  Tabletting processes · CPC title

• A61K31/5513

  1,4-Benzodiazepines, e.g. diazepam {or clozapine} · CPC title

• A61K9/2072

  characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms (A61K9/0004, A61K9/0056, A61K9/0065 take precedence) · CPC title

• A61K31/515

  Barbituric acids; Derivatives thereof, e.g. sodium pentobarbital · CPC title