Tamper-resistant tablet providing immediate drug release

• US 20130028970A1
• Filed: 07/27/2012
• Published: 01/31/2013
• Est. Priority Date: 07/29/2011
• Status: Active Grant

• Current Assignee: Grunenthal GMBH (Grünenthal Pharma GmbH & Co. KG)
• Original Assignee: Grunenthal GMBH (Grünenthal Pharma GmbH & Co. KG)
• Inventors: Schwier, Sebastian, Haupts, Marcel, Barnscheid, Lutz, Ptz, Jana
• Granted Patent: US 10,201,502 B2
• Time in Patent Office: Days
• US Class Current: 424/464
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/138 Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377
• CPC Class Codes: A61K 9/2081 with microcapsules or coated microparticles according to A61K9/50
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids

Abstract

The invention relates to a tamper-resistant tablet comprising

• (i) a matrix material in an amount of more than one third of the total weight of the tablet; and
• (ii) a plurality of coated particulates in an amount of less than two thirds of the total weight of the tablet; wherein said particulates comprise a pharmacologically active compound and a physiologically acceptable polymer, preferably a polyalkylene oxide; and form a discontinuous phase within the matrix material;
  which preferably provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur.;
  and method of using said tablet to treat pain and other conditions.

Claims

1. A tamper-resistant tablet comprising

(i) a matrix material in an amount of more than one third of the total weight of the tablet;

and

(ii) a plurality of coated particulates in an amount of less than two thirds of the total weight of the tablet;

wherein said particulates comprise a pharmacologically active compound and a physiologically acceptable polymer; and

form a discontinuous phase within the matrix material;

which provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur.

2. The tablet according to claim 1, which has under in vitro conditions a disintegration time measured in accordance with Ph. Eur. of at most 3 minutes.

3. The tablet according to claim 1, wherein the content of the matrix material is at least 40 wt.-%, based on the total weight of the tablet.

4. The tablet according to claim 1, wherein the pharmacologically active compound is an opioid.

5. The tablet according to claim 1, wherein the particulates have an average diameter of about 1000±

250 μ

m and/or an average length of about 750±

250 μ

m.

6. The tablet according to claim 1, wherein the content of the polymer is at least 25 wt.-%, based on the total weight of a particulate.

7. The tablet according to claim 1, wherein the content of the pharmacologically active compound is at least 25 wt.-%, based on the total weight of a particulate.

8. The tablet according to claim 1, which has a total weight of 500±

300 mg and contains

(i) 50±

15 wt.-% coated particulates having an average particle size of 800±

400 μ

m, wherein the coated particulates comprise

23±

20 wt.-% pharmacologically active compound,

22±

12 wt.-% physiologically acceptable polymer,

optionally, 4.0±

3.5 wt.-% plasticizer, and

optionally, 0.05±

0.05 wt.-% further excipients; and

(ii) 49±

15 wt.-% matrix material, wherein the matrix material comprises

43±

10 wt.-% filler and/or binder,

optionally, 5±

4 wt.-% disintegrant and

optionally, 0.15±

0.15 wt.-% lubricant;

all wt.-% being expressed relative to the total weight of the tablet.

9. The tablet according to claim 1, wherein the particulates are hot melt-extruded.

10. The tablet according to claim 1, wherein the polymer is a polyalkylene oxide.

11. The tablet according to claim 1, wherein the matrix material is also present in particulate form.

12. The tablet according to claim 1, wherein the particulates are coated with a coating material comprising a water-soluble polymer.

13. The tablet according to claim 12, wherein the water-soluble polymer is selected from the group consisting of cellulose esters, cellulose ethers, poly(meth)acrylates, vinyl polymers, and natural film formers.

14. The tablet according to claim 1, wherein the matrix material comprises binder, filler, disintegrant and/or lubricant.

15. A method of treating a condition in a patient in need thereof by administering to a patient in need of such treating a tablet comprising an effective amount therefor of a pharmacologically active compound, wherein the tablet is a tablet according to claim 1.

16. The method according to claim 15, wherein the condition is pain.

17. The method according to claim 16, wherein the pharmacologically active compound is an opioid.