Tamper resistant immediate release capsule formulation comprising tapentadol

Patent metadata

Field	Value
Publication number	US-9913814-B2
Application number	US-201615257972-A
Country	US
Kind code	B2
Filing date	Sep 7, 2016
Priority date	May 12, 2014
Publication date	Mar 13, 2018
Grant date	Mar 13, 2018

Abstract

The invention is directed to an immediate release capsule which mitigates the abuse of Tapentadol or physiologically acceptable salt thereof by direct intravenous injection. The capsule comprises a tamper resistant formulation which when mixed with water and heated, results in a turbid, bubbling mixture that is not injectable with a standard insulin syringe.

First claim

The invention claimed is:

1. A tamper resistant pharmaceutical capsule comprising a capsule filling and a capsule shell, wherein said capsule filling is encapsulated by said capsule shell and comprises:
(a) Tapentadol or a physiologically acceptable salt thereof in an amount within the range of from 10 mg to 400 mg, as equivalent weight relative to Tapentadol free base; and
(b) a liquid excipient blend comprising a solvent, a surfactant, and a viscosity enhancer;
wherein the viscosity enhancer comprises colloidal anhydrous silica and a gum;
wherein a mixture of 250 milligrams of the liquid excipient blend with 5 milliliters of water at the mixture's boiling point forms a viscous phase which cannot pass through a 25 millimeter long needle having an inner diameter of 0.60 millimeters; and
wherein the capsule provides immediate release of Tapentadol or the physiologically acceptable salt thereof upon oral administration.

2. The capsule according to claim 1 , wherein the gum is selected from the group consisting of acacia, agar, tragacanth, guar gum, xanthan gum, locust bean gum, tara gum, karaya, gellan gum, welan gum, and rhamsan gum.

3. The capsule according to claim 1 , wherein the total content of viscosity enhancer is within the range of from 0.1 to 10 wt.-%, relative to the total weight of the capsule filling.

4. The capsule according to claim 1 , wherein the total content of solvent is within the range of from 10 to 90 wt.-%, relative to the total weight of the capsule filling.

5. The capsule according to claim 1 , wherein the liquid excipient blend comprises an ion exchange resin.

6. The capsule according to claim 5 , wherein the ion exchange resin is anionic.

7. The capsule according to claim 5 , wherein the total content of ion exchange resin is within the range of from 0.1 to 25 wt.-%, relative to the total weight of the capsule filling.

8. The capsule according to claim 1 , wherein the surfactant is nonionic.

9. The capsule according to claim 8 , wherein the nonionic surfactant is selected from the group consisting of glycerol monoesters with C 6-18 -fatty acids, glycerol diesters with identical or different C 6-18 -fatty acids, glycerol triesters with identical or different C 6 -18 -fatty acids, polyethylene glycol monoesters with C 6-18 -fatty acids, polyethylene glycol diesters with identical or different C 6-18 -fatty acids, and mixtures of any of the foregoing.

10. The capsule according to claim 1 , wherein the total content of surfactant is within the range of from 0.1 to 35 wt.-%, relative to the total weight of the capsule filling.

11. The capsule according to claim 1 , wherein the total content of Tapentadol or physiologically acceptable salt thereof, as equivalent weight relative to Tapentadol free base, is within the range of from 0.1 to 25 wt.-%, relative to the total weight of the capsule filling.

12. A method for treating pain in a patient in need of such treatment, said method comprising administering to said patient at least one capsule according to claim 1 .

13. A method for preventing parenteral abuse of Tapentadol or a physiologically acceptable salt thereof, said method comprising providing the Tapentadol or a physiologically acceptable salt thereof in the form of a capsule according to claim 1 .

Assignees

• Gruenenthal Gmbh

Inventors

• Friedrich Ingo
• Fuhrherr Richard
• Möschter Silke
• Wengner Simone

Classifications

• A61P29/00

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

• A61P25/36

  Opioid-abuse · CPC title

• A61P25/04

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

• A61K31/137 Primary

  Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone} · CPC title

• A61K9/4866

  Organic macromolecular compounds · CPC title