Nanoparticulate clopidogrel and aspirin combination formulations
First Claim
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1. A stable nanoparticulate clopidogrel and aspirin composition comprising:
- (a) particles of a clopidogrel, or a salt or derivative thereof, having an effective average particle size of less than about 2000 nm;
(b) particles of aspirin, or a salt or derivative thereof; and
(c) at least one surface stabilizer.
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Abstract
The present invention is directed to compositions comprising a nanoparticulate clopidogrel and aspirin combination, or salts or derivatives thereof, having improved clopidogrel bioavailability. The nanoparticulate clopidogrel particles, and optionally the nanoparticulate aspirin 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 and aspirin particles may also be formulated as a controlled release polymeric coating or matrix drug delivery system.
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Citations
28 Claims
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1. A stable nanoparticulate clopidogrel and aspirin composition comprising:
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(a) particles of a clopidogrel, or a salt or derivative thereof, having an effective average particle size of less than about 2000 nm;
(b) particles of aspirin, or a salt or derivative thereof; and
(c) at least one surface stabilizer. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 22)
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21. A method of preparing a nanoparticulate clopidogrel and aspirin combination, comprising:
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(a) contacting particles of clopidogrel, or a salt or derivative thereof, 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, and;
(b) combining the resultant nanoparticulate clopidogrel with aspirin, or a salt or derivative thereof.
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23. A stable nanoparticulate clopidogrel composition comprising:
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(a) particles of a clopidogrel, or a salt or derivative thereof, having an effective average particle size of less than about 2000 nm;
(b) at least one surface stabilizer; and
(c) an enteric coating encasing the clopidogrel particles. - View Dependent Claims (24)
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25. A composition comprising:
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(a) a clopidogrel, or a salt or derivative thereof; and
(b) an enteric coating encasing the clopidogrel for inhibiting release of the clopidogrel to the stomach. - View Dependent Claims (26, 27, 28)
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Specification