Highly concentrated stable meloxicam solutions for needleless injection

Abstract

Aqueous cyclodextrin-free solution of meloxicam suitable for administration by needleless injection, containing a pharmacologically acceptable meloxicam salt of an organic or inorganic base and one or more suitable excipients, the content of dissolved meloxicam salt being from 35 to 100 mg / ml. The formulation according to the invention has a shelf-life of up to 24 months or more.

Description

[0001]The present invention relates to highly concentrated stable meloxicam solutions for intracutaneous or subcutaneous needleless injection for treating respiratory diseases and inflammation in mammals.BACKGROUND OF THE INVENTION[0002]Meloxicam (4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide) is an active substance which belongs to the group of NSAIDs (non-steroidal-anti-inflammatory drugs). Meloxicam and the sodium and meglumine salt thereof (N-methyl-D-glucamine salt) are described in EP-A-0 002 482. EP-A-0 002 482 shows, inter alia, the example of a 0.2% injectable solution of meloxicam consisting of the meglumine salt of the active substance, sodium chloride and water.[0003]EP-A-0 945 134 discloses the pH-dependent solubility characteristics of meloxicam and its salts, i.e. the sodium salt, the ammonium salt and the meglumine salt, in aqueous solution. According to this, meloxicam is an active substance which does not dissolve readil...

AI Technical Summary

Benefits of technology

"The invention is a meloxicam solution that can be injected directly into the skin without the need for a needle. The solution contains a high concentration of meloxicam and other excipients, such as citric acid, lecithin, gluconic acid, and polyoxyethylene-polyoxypropylene copolymers. The solution is stable and can be sterilized. The invention solves the problem of previous formulations that contained high levels of solubilizers and had to be injected into the skin using a needle. The solution is suitable for needle-free injection and has a pH range of 8 to 10. The invention also provides a method for producing the meloxicam solution and a pharmacologically acceptable meloxicam salt."

Problems solved by technology

However, up till now it has only been possible to produce stable, clear, aqueous solutions with a low concentration of meloxicam.

Attempts to produce formulations with the same or a similar recipe led to cloudiness of the solution, e.g. if the meloxicam concentrations were higher, e.g. 2%.

It has not hitherto been possible to treat large farm animals with a meloxicam solution that could be injected without a needle.

The low concentration of active substance in the injectable solution did not allow an acceptable, well tolerated injection volume.