Nanoparticulate imatinib mesylate formulations

An imatinib mesylate, nanoparticle technology, applied in nanotechnology, nanotechnology, nanomedicine, etc., can solve the problems of limited treatment results, limited bioavailability, etc., and achieve small doses, increased bioavailability, The effect of increasing the dissolution rate

Inactive Publication Date: 2008-07-30
ELAN PHRMA INT LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Thus, the bioavailability of imatinib mesylate is limited in the fasted state compared to ...

Method used

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  • Nanoparticulate imatinib mesylate formulations
  • Nanoparticulate imatinib mesylate formulations
  • Nanoparticulate imatinib mesylate formulations

Examples

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Embodiment 1

[0164] The purpose of this example is to prepare a composition comprising nanoparticulate imatinib mesylate or a salt or derivative thereof.

[0165] 5% (w / w) imatinib mesylate mixed with one or more surface stabilizers such as hydroxypropyl cellulose (HPC-SL) and dioctyl sulfosuccinate (DOSS) can be Aqueous dispersion, and 500 micron PolyMill  Grinding media (Dow Chemical Co.) (e.g. at 89% media loading) in NanoMill  Mill in a 10 ml chamber of 0.01 (NanoMill Systems, King of Prussia, PA; see eg US Pat. No. 6,431,478). In an exemplary method, the mixture may be milled at 2500 rpm for 60 minutes.

[0166] After grinding, the particle size of the ground imatinib mesylate particles can be measured with a Horiba LA 910 particle size analyzer in deionized distilled water. For a successful composition, the initial mean and / or D50 ground imatinib mesylate particle size is expected to be less than 2000 nm.

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Abstract

The present invention is directed to a nanoparticulate compositions of imatinib mesylate, or a salt or derivative thereof, having improved pharmacokinetic profiles and reduced fed/fasted variability. The nanoparticulate imatinib mesylate particles of the composition have an effective average particle size of less than about 2000 nm and are useful in the treatment of chronic myeloid leukemia, gastrointestinal stromal tumors and related diseases.

Description

[0001] Cross References to Related Patent Applications [0002] This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Patent Application No. 60 / 687,146, filed June 3, 2005, which is hereby incorporated by reference in its entirety. field of invention [0003] The present invention generally relates to compounds and compositions useful in the treatment of chronic myelogenous leukemia, gastrointestinal stromal tumors, and related diseases. More specifically, the present invention relates to nanoparticulate imatinib mesylate compositions. The effective average particle size of the nanoparticulate imatinib mesylate composition is less than about 2000 nm. Background of the invention [0004] A. Background on imatinib mesylate [0005] Imatinib mesylate, chemically known as 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridyl) )-2-pyrimidinyl]amino]-phenyl]benzamide methanesulfonate, the molecular formula is C 29 h 31 N 7 O·CH 4 SO 3 , ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/506
CPCA61K9/145A61K9/146A61K31/506A61P1/04A61P35/00A61P35/02A61P35/04A61K9/16A61K9/14B82Y5/00
Inventor S·詹金斯G·G·利弗西奇
Owner ELAN PHRMA INT LTD
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