Nanoparticulate clopidogrel formulations
First Claim
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1. A stable nanoparticulate clopidogrel composition comprising:
- (a) particles of clopidogrel or a derivative or a salt 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 compositions comprising a nanoparticulate clopidogrel, or a salt or derivative thereof, having improved bioavailability. The nanoparticulate clopidogrel particles of the composition have an effective average particle size of less than about 2000 nm and are useful in the prevention and treatment of pathologies induced by platelet aggregation. The clopidogrel particles may also be formulated as a controlled release polymeric coating or matrix drug delivery system.
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Citations
22 Claims
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1. A stable nanoparticulate clopidogrel composition comprising:
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(a) particles of clopidogrel or a derivative or a salt 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, 13)
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14. A stable nanoparticulate clopidogrel composition comprising:
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(a) particles of clopidogrel or a derivative or a salt 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 clopidogrel.
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15. A clopidogrel composition comprising clopidogrel or a derivative or a salt thereof, wherein the composition has:
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(a) a Cmax for clopidogrel 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 clopidogrel, administered at the same dosage;
(b) an AUC for clopidogrel 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 clopidogrel, administered at the same dosage;
(c) a Tmax for clopidogrel 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 clopidogrel, administered at the same dosage;
or(d) any combination of (a), (b), and (c).
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- 16. A method for the preparation of nanoparticulate clopidogrel or a derivative or salt thereof comprising contacting particles of clopidogrel with at least one surface stabilizer for a time and under conditions sufficient to provide a nanoparticulate clopidogrel composition having an effective average particle size of less than about 2000 nm.
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18. A method for the treatment of pathologies induced by platelet aggregation in a subject comprising administering to a subject a stable nanoparticulate clopidogrel composition comprising:
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(a) particles of at least one clopidogrel or a derivative or a salt thereof having an effective average particle size of less than about 2000 nm; and
(b) at least one surface stabilizer. - View Dependent Claims (19, 20, 21, 22)
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Specification