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Nanoparticulate kinase inhibitor formulations

A kinase inhibitor, nanoparticle technology, applied in nanoparticle LS104 composition, treatment or prevention of disease or disorder composition, preparation and use of such nanoparticle composition, nanoparticle kinase inhibitor composition field, can solve Poor water-soluble inhibitor bioavailability and other issues

Inactive Publication Date: 2009-08-05
ELAN PHRMA INT LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0022] While the high therapeutic value of kinase inhibitors such as LS104 is recognized in the art, bioavailability of poorly water-soluble inhibitors is limited when administered orally or by injection and may be difficult or impossible for other types of administration Formulated as a safe and effective product

Method used

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  • Nanoparticulate kinase inhibitor formulations
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  • Nanoparticulate kinase inhibitor formulations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0148] The purpose of this example was to prepare a nanoparticle formulation of LS104 suitable for intravenous administration. As described below, an exemplary successful nanoparticle dispersion formulation ("NCD") comprised 10% LS104, 2.5% Povidone K-12PF, and 0.1% sodium deoxycholate.

[0149]Initial formulation sieving was performed using the low energy tumbler mill (Stoneware) method. The grinding media used was 0.8 mm yttrium treated zirconia (Tosoh). All formulations were milled at 170 rpm. Milling times are shown in Table 1 below. Light microscopy was performed with a Leica optical microscope utilizing a 100x objective. All particle sizes were measured using a Horiba LA 910 using deionized (DI) water as the diluent and sonicating for 30 seconds.

[0150] Four different formulations, identified in Table 1 below, were screened. The first formulation contained Poloxamer 338 (Pluronic F108) as a stabilizer. Large crystals were observed at the end of the process. This...

Embodiment 2

[0152] The second and fourth formulations were further evaluated. Previous experience with slightly smaller particle sizes of PVPK-12 and NaDOC suggests that the fourth formulation is slightly more favorable. Therefore, the PVP K12 / sodium deoxycholate combination was chosen as a desired stabilizer combination for LS104.

[0153] All processing after the initial drum mill sieving was performed using a high energy media mill using highly cross-linked polystyrene beads as the milling media. It has been shown that this method can be used to prepare lead formulations since high shear environments may sometimes induce aggregation. Formulations containing the same stabilizer components are suitable for high energy processes. The formulation contained 5% LS104 / 1.25% PVPK-12 / 0.05% NaDOC and was successfully evaluated in a high energy mill.

[0154] Product particle size was measured using standard R&D methods on a Horiba LA910 particle size analyzer with target sample concentration ...

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Abstract

The invention is directed to compositions comprising at least one nano particulate kinase inhibitor, such as LS 104 or a salt or derivative thereof, having improved dissolution rate providing a faster onset of drug availability. The nanoparticulate kinase inhibitor particles, such as LS 104, have an effective average particle size of less than about 2000 nm and are useful in the treatment of cancers, such as leukemia, myeloproliferative disorders and related diseases.

Description

[0001] Related Application Cross Reference [0001] This application claims priority to US Provisional Patent Application 60 / 812,960, filed June 13, 2006, the contents of which are hereby incorporated by reference in their entirety. field of invention [0002] The present invention relates to kinase inhibitor compounds and compositions useful in the treatment or prevention of diseases or disorders such as myeloproliferative diseases, leukemias and related diseases or conditions. More particularly, the present invention relates to nanoparticulate kinase inhibitor compositions, such as nanoparticulate LS104 compositions, having an effective average particle size of less than about 2000 nm. The invention also relates to methods of making and using such nanoparticle compositions. Background of the invention A. Background on LS104 [0003] Aberrant kinase activity is implicated in many diseases. Leukemia is a cancer of the bone marrow and blood. They are characterized by the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/20
CPCA61K9/2013A61K9/0019A61K9/145A61K9/146A61K9/2018A61K9/2009A61K47/32A61K9/2054A61P35/02A61P43/00A61K9/14A61K9/20B82Y5/00
Inventor E·利弗西奇G·凯里W·H·博世J·凯勒N·赖德
Owner ELAN PHRMA INT LTD
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