Tamper Resistant Dosage Form Comprising An Anionic Polymer

• US 20120065220A1
• Filed: 09/01/2011
• Published: 03/15/2012
• Est. Priority Date: 09/02/2010
• Status: Active Grant

• Current Assignee: Grunenthal GMBH (Grünenthal Pharma GmbH & Co. KG)
• Original Assignee: Grunenthal GMBH (Grünenthal Pharma GmbH & Co. KG)
• Inventors: BARNSCHEID, Lutz, BARTHOLOMÄUS, Johannes, SCHWIER, Sebastian
• Granted Patent: US 9,636,303 B2
• Time in Patent Office: Days
• US Class Current: 514/282
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids

Abstract

A pharmaceutical dosage form and method of using same, the pharmaceutical dosage form exhibiting a breaking strength of at least 500 N, said dosage form containing

• • a pharmacologically active ingredient (A);
  • a physiologically acceptable polymer (B) obtainable by polymerization of a monomer composition comprising an ethylenically unsaturated monomer bearing an anionic functional group, in protonated form or a physiologically acceptable salt thereof;
  • a polyalkylene oxide (C) having a weight average molecular weight of at least 200,000 g/mol, wherein the content of the polyalkylene oxide (C) is at least 20 wt.-%, based on the total weight of the dosage form;
    wherein the pharmacologically active ingredient (A) is present in a controlled-release matrix comprising the polymer (B) and the polyalkylene oxide (C).

Claims

1. A pharmaceutical dosage form exhibiting a breaking strength of at least 500 N, said dosage form comprising:

a pharmacologically active ingredient (A);

a physiologically acceptable polymer (B) obtainable by polymerization of a monomer composition comprising an ethylenically unsaturated monomer bearing an anionic functional group, in protonated form or a physiologically acceptable salt thereof;

a polyalkylene oxide (C) having a weight average molecular weight of at least 200,000 g/mol, wherein the content of the polyalkylene oxide (C) is at least 20 wt.-%, based on the total weight of the dosage form;

wherein the pharmacologically active ingredient (A) is present in a controlled-release matrix comprising the polymer (B) and the polyalkylene oxide (C).

2. The pharmaceutical dosage form according to claim 1, wherein the pharmacologically active ingredient (A) is an opioid.

3. The pharmaceutical dosage form according to claim 1, wherein the anionic functional group is selected from carboxyl groups, sulfonyl groups, sulfate groups, and phosphoryl groups.

4. The pharmaceutical dosage form according to claim 1, wherein the monomer composition comprises a monomer selected from acrylic acid, alkyl acrylates, alkyl alkacrylates, and mixtures thereof.

5. The pharmaceutical dosage form according to claim 1, wherein the monomer composition further comprises a cross-linking agent.

6. The pharmaceutical dosage form according to claim 5, wherein the cross-linking agent is selected from the group consisting of allyl sucrose, allyl pentaerythritol, divinyl glycol, divinyl polyethylene glycol and (meth)acrylic acid esters of diols.

7. The pharmaceutical dosage form according to claim 1, wherein the relative weight ratio of the polyalkylene oxide (C) to the physiologically acceptable polymer (B) is within the range of from 8:

1 to 1.5;

1

8. The pharmaceutical dosage form according to claim 1, wherein the polyalkylene oxide (C) is a polyethylene oxide.

9. Pharmaceutical dosage form according to claim 8, wherein the polyethylene oxide (C) has a molecular weight of about 500,000 g/mol to about 15,000,000 g/mol.

10. Pharmaceutical dosage form according to claim 1, which has been prepared by melt-extrusion.

11. Pharmaceutical dosage form according to claim 1, which further comprises polyethylene glycol.

12. The pharmaceutical dosage form according to claim 1, which is adapted for administration once-daily, twice daily or thrice-daily.

13. Pharmaceutical dosage form according to claim 1, which is a tablet.

14. A method of treating a disease or disorder in a patient in need of such treatment, the disease or disorder being treatable with a pharmacologically active ingredient (A), the method comprising administering to said patient an effective amount therefor of a pharmaceutical dosage form according to claim 1 for a period of time sufficient to treat said disease or disorder.