Nanoparticulate imatinib mesylate formulations
First Claim
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1. A stable nanoparticulate composition of imatinib mesylate, or a salt or derivative thereof, comprising:
- (a) particles of imatinib mesylate, or a salt or derivative thereof, having an effective average particle size of less than about 2000 nm; and
(b) at least one surface stabilizer.
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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.
127 Citations
22 Claims
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1. A stable nanoparticulate composition of imatinib mesylate, or a salt or derivative thereof, comprising:
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(a) particles of imatinib mesylate, or a salt or derivative thereof, having an effective average particle size of less than about 2000 nm; and
(b) at least one surface stabilizer. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 17, 18)
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- 13. A composition comprising imitanib mesylate, or a salt or a derivative thereof, wherein upon administration to a human the composition does not produce significantly different absorption levels when administered under fed as compared to fasting conditions.
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15. A stable nanoparticulate composition of imatinib mesylate, or a salt or derivative thereof, comprising:
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(a) particles of imatinib mesylate, or a salt or derivative thereof, having an effective average particle size of less than about 2000 nm; and
(b) at least one surface stabilizer, wherein upon administration to a mammal the composition produces therapeutic results at a dosage which is less than that of a non-nanoparticulate dosage form of the same imatinib mesylate, or salt or derivative thereof.
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16. A composition of imatinib mesylate, or a salt or derivative thereof, comprising imatinib mesylate or a salt or derivative thereof wherein the composition has:
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(a) a Cmax for imatinib mesylate, or a salt or derivative thereof, when assayed in the plasma of a mammalian subject following administration that is greater than the Cmax for a non-nanoparticulate formulation of the same imatinib mesylate, or a salt or derivative thereof, administered at the same dosage;
(b) an AUC for imatinib mesylate, or a salt or derivative thereof, when assayed in the plasma of a mammalian subject following administration that is greater than the AUC for a non-nanoparticulate formulation of the same imatinib mesylate, or a salt or derivative thereof, administered at the same dosage;
(c) a Tmax for imatinib mesylate, or a salt or derivative thereof, when assayed in the plasma of a mammalian subject following administration that is less than the Tmax for a non-nanoparticulate formulation of the same imatinib mesylate, or a salt or derivative thereof, administered at the same dosage;
or(d) any combination of (a), (b), and (c).
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- 19. A method for preparing imatinib mesylate, or a salt or derivative thereof, comprising contacting particles of imatinib mesylate, or a salt or derivative thereof with at least one surface stabilizer for a time and under conditions sufficient to provide a nanoparticulate imatinib mesylate composition having an effective average particle size of less than about 2000 nm.
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21. A method for treating of chronic myeloid leukemia, gastrointestinal stromal tumors and related diseases comprising administering a stable nanoparticulate composition of imatinib mesylate, or a salt or derivative thereof, comprising:
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(a) particles of imatinib mesylate, or a salt or derivative thereof, having an effective average particle size of less than about 2000 nm; and
(b) at least one surface stabilizer. - View Dependent Claims (22)
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Specification