Nanoparticulate and Controlled Release Compositions Comprising Prostaglandin Derivatives
First Claim
1. A stable nanoparticulate prostaglandin derivative composition comprising:
- (a) particles of a prostaglandin derivative; and
(b) associated with the surface thereof at least one surface stabilizer, wherein the prostaglandin derivative particles have an effective average particle size of less than about 2000 nm in diameter.
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Abstract
The present invention is directed to compositions comprising a nanoparticulate prostaglandin derivative, preferably limaprost or a salt or derivative thereof, having improved bioavailability. The nanoparticulate prostaglandin derivative particles of the composition have an effective average particles size of less than about 2000 nm and are useful in the treatment of ischemic symptoms. The invention also relates to a controlled release composition comprising a prostaglandin derivative, such as limaprost alfadex, or a nanoparticulate prostaglandin derivative, such as limaprost or a salt or derivative thereof, that in operation delivers the drug in a pulsed or bimodal manner for the treatment of ischemic symptoms.
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Citations
37 Claims
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1. A stable nanoparticulate prostaglandin derivative composition comprising:
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(a) particles of a prostaglandin derivative; and (b) associated with the surface thereof at least one surface stabilizer, wherein the prostaglandin derivative particles have an effective average particle size of less than about 2000 nm in diameter. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 24, 25, 26)
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- 15. A method of preparing a nanoparticulate prostaglandin derivative comprising contacting particles of said prostaglandin derivative with at least one surface stabilizer for a time and under conditions sufficient to provide a nanoparticulate prostaglandin derivative composition having an effective average particle size of less than about 2000 nm in diameter.
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17. A method of treatment of ischemic symptoms comprising the administration of an oral nanoparticulate prostaglandin derivative comprising particles of said prostaglandin derivative having at least one surface stabilizer associated with the surface thereof, wherein the particles have an effective particle size of less than about 2000 nm in diameter.
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18. A controlled release composition comprising:
- (A) a first population of prostaglandin derivative-containing particles which allows for the immediate or delayed immediate release of said prostaglandin derivative therefrom; and
(B) at least one subsequent population of prostaglandin-containing particles which allows for the modified release of said prostaglandin derivative therefrom;
said composition allowing the delivery of the prostaglandin derivative in a pulsatile or zero order manner. - View Dependent Claims (19, 20, 22)
- (A) a first population of prostaglandin derivative-containing particles which allows for the immediate or delayed immediate release of said prostaglandin derivative therefrom; and
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21. The dosage form according to claim 59 wherein the composition is contained in a hard gelatin or soft gelatin capsule.
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23. A composition comprising:
- (A) prostaglandin derivative-containing particles which allow for the modified release of prostaglandin derivative therefrom; and
(B) a layer of prostaglandin derivative coated on top of said particles which allows for the immediate release of said prostaglandin derivative.
- (A) prostaglandin derivative-containing particles which allow for the modified release of prostaglandin derivative therefrom; and
- 27. A pharmaceutical composition of an immunosuppressive agent comprising solid particles of the agent coated with one or more surface stabilizers, wherein the particles have an average effective particle size of from less than about 50 nm to less than about 2 microns.
Specification