TAMPER-RESISTANT DOSAGE FORM COMPRISING PHARMACOLOGICALLY ACTIVE COMPOUND AND ANIONIC POLYMER

• US 20130225697A1
• Filed: 02/27/2013
• Published: 08/29/2013
• Est. Priority Date: 02/28/2012
• Status: Abandoned Application

• Current Assignee: Grunenthal GMBH (Grünenthal Pharma GmbH & Co. KG)
• Original Assignee: Grunenthal GMBH (Grünenthal Pharma GmbH & Co. KG)
• Inventors: BARNSCHEID, Lutz, SCHWIER, Sebastian, REDMER, Jessica
• Application Number:
  US13/778,186
• Publication Number:
  US 20130225697A1
• Time in Patent Office: Days
• US Class Current: 514/772.1
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• 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 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• 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
• CPC Class Codes: A61P 25/36 Opioid-abuse

Abstract

The invention relates to a pharmaceutical dosage form having a breaking strength of at least 300 N and comprising a pharmacologically active compound, an anionic polymer bearing carboxylic groups, wherein the content of the anionic polymer is 20 wt.-%, based on the total weight of the pharmaceutical dosage form, and a nonionic surfactant.

Claims

1. A pharmaceutical dosage form having a breaking strength of at least 300 N and comprising

a pharmacologically active compound,

an anionic polymer bearing carboxylic groups, wherein the content of the anionic polymer is ≧

20 wt.-%, based on the total weight of the pharmaceutical dosage form, and

a nonionic surfactant.

2. The pharmaceutical dosage form according to claim 1, wherein the anionic polymer is obtainable by polymerization of a monomer composition comprising an ethylenically unsaturated monomer selected from ethylenically unsaturated carboxylic acids, ethylenically unsaturated carboxylic acid anhydrides, ethylenically unsaturated sulfonic acids, and mixtures thereof.

3. The pharmaceutical dosage form according to claim 1, wherein the anionic polymer is derived from an ethylenically unsaturated monomer selected from (alk)acrylic acids, (alk)acrylic anhydrides, alkyl (alk)acrylates, or a combination thereof.

4. The pharmaceutical dosage form according to claim 2, wherein the monomer composition further comprises at least one cross-linking agent selected from the group consisting of allyl sucrose, allyl pentaerythritol, divinyl glycol, divinyl polyethylene glycol and (meth)acrylic acid esters of diols.

5. The pharmaceutical dosage form according to claim 1, which either does not contain any polyalkylene oxide having an average molecular weight of at least 200,000 g/mol, or wherein the total content of polyalkylene oxide(s) having an average molecular weight of at least 200,000 g/mol is ≦

35 wt.-%, based on the total weight of the pharmaceutical dosage form.

6. The pharmaceutical dosage form according to claim 1, wherein the pharmacologically active compound is an opioid.

7. The pharmaceutical dosage form according to claim 1, wherein the nonionic surfactant

(i) in pure water at a concentration of 25 wt.-% forms an aqueous dispersion having a viscosity η

₁ at a temperature of 20°

C. and a viscosity η

₂ at a temperature of more than 20°

C., where η

₂>

η

₁; and

/or

(ii) has an HLB value of at least 20, and/or

(iii) has a surface tension in 0.1% aqueous solution at 30°

C. of at least 35 dynes/cm; and

/or

(iv) has a viscosity of at most 4000 mPa·

s, measured at 70°

C. using a model LVF or LVT Brookfield viscosimeter.

8. The pharmaceutical dosage form according to claim 1, wherein the nonionic surfactant is a synthetic copolymer of ethylene oxide and propylene oxide.

9. The pharmaceutical dosage form according to claim 1, wherein the nonionic surfactant is selected from block copolymers according to general formula (I-a)

10. The pharmaceutical dosage form according to claim 1, wherein the content of the nonionic surfactant is at least 10 wt.-%, based on the total weight of the pharmaceutical dosage form.

11. The pharmaceutical dosage form according to claim 1, wherein the pharmacologically active compound is embedded in a prolonged release matrix comprising the anionic polymer and the optionally present nonionic surfactant.

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

13. The pharmaceutical dosage form according to claim 1, which is thermoformed.

14. The pharmaceutical dosage form according to claim 1, which is tamper-resistant.

15. A method of treating pain in a patient in need thereof, said method comprising administering to said patient a dosage form according to claim 6.