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Nanoparticulate meloxicam formulations

Inactive Publication Date: 2010-11-25
ALKERMES PHARMA IRELAND LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0018]The present invention is directed to a method of treating moderate to moderately severe acute pain with a composition comprising meloxicam. In an exemplary embodiment, method of treatment includes administering an injectable dosage form comprising meloxicam, polyvinylpyrrolidone, NaDOC, and sucrose to a patient in need thereof. In an embodiment of the invention, the composition provides meaningful pain relief for up to 24 hours when administered to a patient in need thereof.

Problems solved by technology

However, due to their typically long onset of action, conventional NSAIDs, including conventional meloxicam, are frequently inappropriate for management of acute pain.
Because meloxicam is practically insoluble in water, attaining sufficient bioavailability of this drug is problematic.
Because poorly water soluble active agents are difficult to solubilize in an aqueous based mammal environment, it can be difficult to formulate many poorly water soluble drugs for injectable formulations as conventional poorly water soluble drug formulations can contain particles of drug which do not meet the standards set forth in USP.
This is problematic, as an injectable formulation may be highly desirable over an alternative dosage form.

Method used

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  • Nanoparticulate meloxicam formulations
  • Nanoparticulate meloxicam formulations
  • Nanoparticulate meloxicam formulations

Examples

Experimental program
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Effect test

example 1

[0127]This example identifies and exemplary method to prepare a nanoparticulate meloxicam dispersion suitable for injection.

[0128]A slurry of 20% (w / w) meloxicam and 4% (w / w) polyvinyl pyrrolidone were milled in a NanoMill® milling system (Elan Drug Delivery, Inc., King of Prussia, Pa.; see e.g., U.S. Pat. No. 6,431,478 for “Small Scale Mill”).

example 2

[0129]Aqueous dispersions of 5 wt. % meloxicam and 1 wt. % stabilizer (see Table 1, below) were charged into a NanoMill® milling system (Elan Drug Delivery, Inc., King of Prussia, Pa.; see e.g., U.S. Pat. No. 6,431,478 for “Small Scale Mill”).

[0130]Particle size analysis of the resultant milled dispersions was performed using a Horiba LA-910 particle size analyzer (Horiba Instruments, Irvine, Calif.). The results are shown below in Table 1. In the table below, the value for D50 is the particle size below which 50% of the active agent particles fall. Similarly, D90 is the particle size below which 90% of the active agent particles fall.

TABLE 1MeanD50D90Stabilizer(nm)(nm)(nm)Optical Microscopy*poloxamer 188133110226Stablepoloxamer 388129108219Stablepolyvinylpyrrolidone k-129890125Stablepolyvinylpyrrolidone k-179895135StablePolysorbate 80227227322StableSodium Deoxycholate119101198StableLecithin190169271Mild aggregationat initialLysozyme9589117Moderate aggregationat initial;Stable at 24...

example 3

[0133]The purpose of this example was to test the stability of a nanoparticulate meloxicam formulation comprising mannitol.

[0134]A slurry of 10% (w / w) meloxicam, 2.5% (w / w) polyvinylpyrrolidone, 0.75% (w / w) NaDOC and 10% (w / w) mannitol was milled to obtain a nanoparticulate dispersion of meloxicam. The nanoparticulate meloxicam dispersion was diluted to 5% meloxicam, 1.25% polyvinylpyrrolidone, 0.375% NaDOC, 5% mannitol and 15% sucrose with a 30% sucrose solution. The formulation was stored at 5° C. for 3 months. The resulting nanoparticulate meloxicam formulation did not show any significant particle agglomeration or aggregation.

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Abstract

The present invention is directed to nanoparticulate compositions comprising meloxicam particles having an effective average particle size of less than about 2000 nm.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application is a continuation-in-part of U.S. patent application Ser. No. 10 / 784,900, filed Feb. 24, 2004, which claims priority to U.S. Provisional Patent Application No. 60 / 450,705, filed Mar. 3, 2003. The contents of these applications are incorporated herein by reference in their entirety.BACKGROUND OF THE INVENTION[0002]Nanoparticulate active agent compositions are described in U.S. Pat. No. 5,145,684 (“the '684 patent”) as particles comprising a poorly soluble therapeutic or diagnostic agent having adsorbed onto or associated with the surface thereof a non-crosslinked surface stabilizer.[0003]Methods of making nanoparticulate active agent compositions are described in, for example, U.S. Pat. Nos. 5,518,187 and 5,862,999, both for “Method of Grinding Pharmaceutical Substances;” U.S. Pat. No. 5,718,388, for “Continuous Method of Grinding Pharmaceutical Substances;” and U.S. Pat. No. 5,510,118 for “Process of Preparing Therapeutic...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/5415A61P29/00C07D417/12
CPCA61K9/0019A61K9/145A61K9/146A61K9/0053A61K31/5415A61K9/5138A61K9/5169A61K9/5192A61K9/5123A61P29/00A61K9/10A61K9/14
Inventor COOPER, EUGENE R.RYDE, TUULAPRUITT, JOHNKLINE, LAURA
Owner ALKERMES PHARMA IRELAND LTD
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