Highly concentrated stable meloxicam solutions

Abstract

Aqueous cyclodextrin-free solution of meloxicam for administration by oral or parenteral route, 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 more than 10 mg / mL. The formulation according to the invention has a shelf-life of up to 24 months or more.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application claims priority to pending U.S. Nonprovisional application Ser. No. 11 / 290,933, filed 30 Nov. 2005 and entitled “Highly Concentrated Stable Meloxicam Solutions,” which claims priority to abandoned U.S. Nonprovisional application Ser. No. 09 / 860,737, filed 18 May 2001 and entitled “Highly Concentrated Stable Meloxicam Solutions,” which claims priority to U.S. Provisional Application No. 60 / 216,004, filed 3 Jul. 2000 and entitled “Highly Concentrated Stable Meloxicam Solutions,” and which claims priority to German Application No. 100 30 345.5, filed 20 Jun. 2000. The disclosure of each aforementioned application is incorporated herein by reference in its entirety.FIELD OF THE INVENTION[0002]The present invention relates to highly concentrated stable meloxicam solutions for oral and parenteral administration, particularly for treating respiratory diseases in large farm animals.BACKGROUND OF THE INVENTION[0003]Meloxicam (4-hy...

AI Technical Summary

Benefits of technology

The present invention provides a solution to the problem of producing a stable, high-concentration meloxicam solution for oral and parenteral administration, particularly for treating respiratory diseases in large farm animals. The solution is achieved by adding a meloxicam salt and certain excipients, such as citric acid, lecithin, gluconic acid, tartaric acid, phosphoric acid, and EDTA or the salts thereof, in a small amount of organic solubilizers. The solution is stable, free from particles, and suitable for injection into animals weighing up to 750 kg. The invention provides a new formulation for meloxicam solutions that can be used for both oral and parenteral administration.

Problems solved by technology

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

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

Thus, it has not hitherto been possible to treat large farm animals with an injectable meloxicam solution as the low concentration of active substance in the injectable solution did not allow an acceptable, well-tolerated injection volume due to the great weight of the animals.

Furthermore, parenteral administration requires that the solution be free from particles; if there are particles in a parenteral drug, there is a risk of vascular damage or embolism.

Moreover, organic solvents, solubilizers, and water-soluble substances can only be used in certain concentrations to achieve acceptable drug tolerance.