Semisolid aqueous pharmaceutical composition containing tapentadol

Patent metadata

Field	Value
Publication number	US-9446008-B2
Application number	US-201213410837-A
Country	US
Kind code	B2
Filing date	Mar 2, 2012
Priority date	Mar 4, 2011
Publication date	Sep 20, 2016
Grant date	Sep 20, 2016

Abstract

A semisolid aqueous pharmaceutical composition containing tapentadol or a physiologically acceptable salt thereof.

First claim

The invention claimed is:

1. A pharmaceutical composition comprising water and tapentadol or a physiologically acceptable salt thereof, wherein said composition is a semi-solid, and wherein the antimicrobial properties of tapentadol are sufficient such that the composition is either free of any preservative or, when the composition contains a preservative, the preservative is contained in an amount that in the absence of tapentadol would be insufficient to preserve the pharmaceutical composition according to Ph. Eur., and wherein said composition has an aqueous phase pH value of at least 5.5, and wherein said composition has a content of tapentadol within the range of from 0.1 to 40 wt.-%, based on the total weight of the composition.

2. The pharmaceutical composition according to claim 1 , wherein said composition is adapted for topical or local administration.

3. The pharmaceutical composition according to claim 1 , wherein said composition is selected from the group consisting of ointments, creams, magmas, gels, emulsions, suspensions, lotions, liniments, pastes, poultices, suspension gels and emulsion gels.

4. The pharmaceutical composition according to claim 1 , wherein said composition is a bi-phasic formulation or a multi-phase formulation.

5. The pharmaceutical composition according to claim 1 , wherein said composition has a tapentadol content amounting to at least 0.55 wt.-%, based on the total weight of the composition.

6. The pharmaceutical composition according to claim 1 , wherein preservative content is at most 5.0 wt.-%, based on the total weight of the composition.

7. The pharmaceutical composition according to claim 1 , wherein said composition further comprises at least one substance selected from the group consisting of lipids and surfactants.

8. The pharmaceutical composition according to claim 7 , wherein said composition comprises a lipid selected from the group consisting of monoglycerides, diglycerides, triglycerides, and mixtures of two or more thereof.

9. The pharmaceutical composition according to claim 7 , wherein said composition comprises a surfactant having an HLB value of at least 12.

10. The pharmaceutical composition according to claim 1 , wherein said composition exhibits fluid characteristics of a pseudoplastic fluid.

11. The pharmaceutical composition according to claim 1 , wherein said composition has a shelf-life under accelerated storage conditions of at least 3 months.

12. A method of treating pain in a subject in need thereof, said method comprising administering to said subject a pharamacologically effective amount of a semi-solid composition according to claim 1 .

13. A method according to claim 12 , wherein said pain is selected from the group consisting of chronic pain and acute pain.

14. A method according to claim 12 , wherein said pain is related to rheumatic disorders, arthritic disorders, painful joints, postoperative complaints, dental surgery, dermatitis, skin lesions, skin cancer, mouth sores or athletic injuries.

Assignees

• Reinhold Ulrich
• Schiller Marc
• Wulsten Eva
• Inghelbrecht Sabine Karine Katrien
• Embrechts Roger Carolus Augusta
• Feil Ulrich
• Gruenenthal Gmbh

Inventors

• Reinhold Ulrich
• Schiller Marc
• Wulsten Eva
• Inghelbrecht Sabine Karine Katrien
• Embrechts Roger Carolus Augusta
• Feil Ulrich

Classifications

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title

• A61K47/14

  Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters · CPC title

• A61K9/107

  Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)} · CPC title

• A61K9/0014

  Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00) · CPC title

• A61K47/06

  Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite · CPC title