Compositions of lipoxygenase inhibitors

A technology of lipoxygenase and composition, applied in the directions of drug combination, active ingredient of heterocyclic compound, anti-inflammatory agent, etc., can solve the problems of unreachable, discouraged, and difficult to remove solvent, etc.

Inactive Publication Date: 2008-11-19
BAXTER INT INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the method of the '684 patent discourages the use of solvents to form precipitates in that such solvents may be too difficult to remove to achieve pharmaceutically acceptable levels

Method used

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  • Compositions of lipoxygenase inhibitors
  • Compositions of lipoxygenase inhibitors
  • Compositions of lipoxygenase inhibitors

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0177] A small particle suspension containing 3% (w / v) zileuton in an aqueous solution comprising mPEG-DSPE, Poloxamer 188, glycerol and phosphate buffered saline was prepared using the direct homogenization method as described below agent.

[0178] Glycerol and sodium phosphate buffer were dissolved in distilled water to produce an aqueous solution of 2.25% glycerol and 10 mM phosphate buffer. mPEG-DSPE and Poloxamer 188 were then added such that each of these surfactants was present at 0.3% (w / v). Adjust the pH to 7 with 1N sodium hydroxide and / or hydrochloric acid solution. Zileuton was added to provide 3% (w / v) zileuton to form a pre-suspension.

[0179] One aliquot of the pre-suspension was circulated through the piston gap homogenizer approximately 250 times and a second aliquot was circulated through the homogenizer approximately 800 times to produce small particle suspension formulations A1 and A2, respectively. The average particle size and the largest particle siz...

Embodiment 2

[0181] A small particle suspension containing 3% (w / v) zileuton in an aqueous solution comprising mPEG-DSPE, Poloxamer 188, glycerol and phosphate buffered saline was prepared using the direct homogenization method as described below agent.

[0182] Glycerol and sodium phosphate buffer were dissolved in distilled water to produce an aqueous solution of 2.25% glycerol and 10 mM phosphate buffer. mPEG-DSPE and Poloxamer 188 were then added such that 0.5% (w / v) of each of these surfactants was present. Adjust the pH to 7 with 1N sodium hydroxide and / or hydrochloric acid solution. Zileuton was added to provide 3% (w / v) zileuton to form a pre-suspension.

[0183] One aliquot of the pre-suspension was circulated through the piston gap homogenizer approximately 260 times and a second aliquot was circulated through the homogenizer approximately 600 times to produce small particle suspension formulations B1 and B2, respectively. The average particle size and the maximum particle siz...

Embodiment 3

[0188] A small particle suspension containing 3% (w / v) zileuton in an aqueous solution comprising lipid E80, mPEG-DSPE, glycerol and phosphate buffer was prepared using the direct homogenization method as described below.

[0189] Glycerol and sodium phosphate buffer were dissolved in distilled water to produce an aqueous solution of 2.25% glycerol and 10 mM phosphate buffer. Lipid E80 and mPEG-DSPE were then added such that lipid 80 was present at 1.5% (w / v) and mPEG-SPE was present at 0.4% (w / v). Adjust the pH to 7 with 1N sodium hydroxide and / or hydrochloric acid solution. Zileuton was added to provide 3% (w / v) zileuton to form a pre-suspension.

[0190] The pre-suspension was circulated through the piston gap homogenizer to produce small particle suspension formulation C. The average particle size and the maximum particle size of 99% of the samples were determined by laser diffraction (Horiba LA-920).

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Abstract

Pharmaceutical compositions comprising particles of lipoxygenase inhibitor compounds having an effective average size of from about 10 nm to about 50 microns are provided. More particularly, pharmaceutical compositions of particle of a 5 -lipoxygenase inhibitor compound having an effective average size of from about 50 nm to about 5 microns are provided. The pharmaceutical compositions are in the form of aqueous suspensions with the particle of the 5-lipoxygenase-inhibitor compound present in concentrations of from about 5 to about 200 mg / ml. In addition, methods for making such pharmaceutical compositions are provided. In particular, microprecipitation and direct homogenization in the presence of at least one surfactant are disclosed for making the pharmaceutical compositions.

Description

[0001] This application claims priority to US Provisional Application 60 / 737,005, filed November 15,2006. Background of the invention [0002] The present invention relates to compositions of lipoxygenase inhibitors, methods for their production and methods for use in the treatment of conditions mediated by lipoxygenase and / or leukotriene activity. In particular, the present invention relates to stable formulations comprising small particles of 5- and / or 12-lipoxygenase inhibitors in therapeutically effective concentrations, methods for their production and the use of said formulations in the treatment of Methods for Activity-Mediated Conditions. A preferred embodiment of the present invention relates to a stable suspension, a stable dry suspension, comprising small particles of zileuton at a therapeutically effective concentration, for parenteral, oral, pulmonary, ophthalmic, nasal, rectal , vaginal, aural, topical, buccal, transdermal, intravenous, intramuscular, subcutaneo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/10A61K9/19A61K31/38A61P1/00A61P9/10A61P11/06A61P17/06A61P17/10A61P29/00A61P35/00A61P37/08
CPCA61K9/0048A61K31/381A61K31/38A61K9/19A61K9/0043A61K9/5146A61K9/10A61P1/00A61P1/04A61P11/00A61P11/02A61P11/06A61P17/06A61P17/10A61P19/06A61P29/00A61P31/04A61P31/12A61P35/00A61P37/08A61P7/06A61P9/00A61P9/10
Inventor 詹姆斯·E·基普珍·韦林普拉莫德·古普塔里塔·布里什
Owner BAXTER INT INC
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