Nanoparticulate benidipine compositions
First Claim
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1. A stable nanoparticulate benidipine composition comprising:
- (a) particles of at least one benidipine 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 relates to nanoparticulate benidipine compositions having improved bioavailability. The compositions comprise benidipine particles having an effective average particle size of less than about 2000 nm and may be useful in the prevention and treatment of hypertension, renal parenchymal hypertension and angina pectoris.
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Citations
22 Claims
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1. A stable nanoparticulate benidipine composition comprising:
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(a) particles of at least one benidipine 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, 14)
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- 15. A benidipine composition comprising at least one benidipine or derivative or a salt thereof, wherein upon administration to a human the at least one benidipine or derivative or salt thereof does not produce significantly different absorption levels when administered under fed as compared to fasting conditions.
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17. A stable nanoparticulate benidipine composition comprising:
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(a) particles of at least one benidipine 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 benidipine.
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18. A nanoparticulate benidipine composition comprising at least one benidipine or derivative or a salt thereof, wherein the composition has:
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(a) a Cmax for the benidipine 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 benidipine, administered at the same dosage;
(b) an AUC for the benidipine 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 benidipine, administered at the same dosage;
(c) a Tmax for the benidipine 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 benidipine, administered at the same dosage;
or(d) any combination thereof.
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- 19. A method for the preparation of a nanoparticulate benidipine or a derivative or salt thereof comprising contacting particles of the benidipine with at least one surface stabilizer for a time and under conditions sufficient to provide a nanoparticulate benidipine composition having an effective average particle size of less than about 2000 nm.
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21. A method for the treatment of a hypertension, renal parenchymal hypertension, angina pectoris or a combination thereof comprising administering a stable nanoparticulate benidipine composition comprising:
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(a) particles of at least one benidipine 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 (22)
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Specification