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Nanoparticulate leukotriene receptor antagonist/corticosteroid formulations

A technology of corticosteroids and receptor antagonists, applied in nanotechnology, nanotechnology, nanomedicine, etc., can solve side effects and other problems, achieve the effects of relieving symptoms, enhancing pharmacological properties, and increasing water solubility

Inactive Publication Date: 2008-05-07
ELAN PHRMA INT LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Current Leukotriene Inhibitor Compositions and Corticosteroid Compositions Have Significant Side Effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0245] The purpose of this example is to prepare a nanoparticle formulation of the leukotriene receptor antagonist Zarukast.

[0246] 5% (w / w) Zarukast (provided by Camida (Tower House, New Quay, Clonmel, County Tipperary, Ireland) and manufactured by Morepen Laboratories Limited (Morepen Village, Nalagarh Road, Near Baddi, Distt, Solan) ) Water dispersion and 2.0% (w / w) Plasdone  S-630 (copovidone K25-34) merged. Combine this mixture with 500 micron PolyMill  Grinding media (Dow Chemical) (89% media load) together in NanoMill  Grinding in a 10ml chamber of 0.01 (NanoMill Systems, King of Prussia, PA). The mixture was milled at a speed of 2500 rpms for 60 minutes.

[0247] After grinding, the particle size of the ground Zallukast particles in deionized distilled water was measured with a Horiba LA 910 particle size analyzer. In addition, under various temperature conditions, fourteen (14) days have elapsed to measure the stability of the milled Zallukast. The results of the sta...

Embodiment 2

[0251] The purpose of this example is to prepare a nanoparticle formulation of the leukotriene receptor antagonist Zarukast.

[0252] 5% (w / w) Zarukast (provided by Camida (Tower House, New Quay, Clonmel, County Tipperary, Ireland) and manufactured by Morepen Laboratories Limited (Morepen Village, Nalagarh Road, Near Baddi, Distt, Solan) ) Water dispersion and 2.0% (w / w) Pharmacoat  603 (Hydroxypropyl Methyl Cellulose (HPMC)) combined. Combine this mixture with 500 micron PolyMill  Grinding media (Dow Chemical) (89% media load) together in NanoMill  0.01 (NanoMill Systems, King of Prussia, PA; see, for example, US Patent No. 6,431,478) 10ml chamber grinding. The mixture was milled at a speed of 2500 rpms for 60 minutes.

[0253] After grinding, the particle size of the ground Zallukast particles in deionized distilled water was measured with a Horiba LA 910 particle size analyzer. The average particle size of the milled Zallukast is 189 nm, D50 is 179 nm, D90 is 253 nm, and D95...

Embodiment 3

[0258] The purpose of this example is to prepare a nanoparticle formulation of the leukotriene receptor antagonist Zarukast.

[0259] 5% (w / w) Zarukast (provided by Camida (Tower House, New Quay, Clonmel, County Tipperary, Ireland) and manufactured by Morepen Laboratories Limited (Morepen Village, Nalagarh Road, Near Baddi, Distt, Solan) ) Water dispersion and 1.5% (w / w) Tween  80 (polyoxyethylene sorbitan fatty acid ester) combined. Combine this mixture with 500 micron PolyMill  Grinding media (Dow Chemical) (89% media load) together in NanoMill  Grinding in a 10ml chamber of 0.01 (NanoMill Systems, King of Prussia, PA). The mixture was milled at a speed of 2500 rpms for 60 minutes.

[0260]After grinding, the particle size of the ground Zallukast particles in deionized distilled water was measured with a Horiba LA 910 particle size analyzer. In addition, under various temperature conditions, fourteen (14) days have elapsed to measure the stability of the milled Zallukast. The...

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PUM

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Abstract

Nanoparticulate compositions containing corticosteroids and leukotriene receptor antagonists are described. The composition is used for prevention and long-term treatment of asthma in adults and children, and for relieving symptoms of allergic conjunctivitis and seasonal allergic rhinitis in adults and children. Combining a leukotriene receptor antagonist in the particle size range of less than 2000nm with a corticosteroid in one formulation resulted in increased potency. Additionally, patient compliance is enhanced since only one dosage form is required. Furthermore, topical administration of leukotriene receptor antagonists results in lower hepatotoxicity, since the liver will be exposed to a smaller amount of drug than would be the case after oral administration. The pharmaceutical compositions of the present invention may be formulated for inhalation, nasal or ophthalmic use.

Description

Field of invention [0001] The present invention relates to a composition comprising at least one nanoparticulate leukotriene receptor antagonist and at least one corticosteroid. The corticosteroid can be a nanoparticulate corticosteroid or a conventional non-nanoparticulate corticosteroid. The composition can be used, for example, to prevent and long-term treatment of asthma in adults and pediatric patients and to relieve symptoms of allergic conjunctivitis and seasonal allergic rhinitis in adults and pediatric patients. Background of the invention [0002] A. Background on leukotriene receptor antagonists [0003] Leukotriene receptor antagonists have been shown to be effective in the prevention and long-term treatment of asthma in adults and pediatric patients and in reducing the symptoms of seasonal allergic rhinitis in adults and pediatric patients. [0004] Leukotrienes are biologically active fatty acids derived from the oxidative metabolism of arachidonic acid. Leukotriene...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/404A61K31/573A61K45/06
CPCA61K9/145A61K31/47A61K47/44A61K9/146A61K31/573A61K47/10A61K31/4188A61K9/008A61K31/404A61K9/0075A61K45/06A61P11/02A61P11/06A61P27/02A61P43/00A61K2300/00A61K9/14B82Y5/00
Inventor G·利弗西奇S·詹金斯C·维尔茨H·博施
Owner ELAN PHRMA INT LTD
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