On-stent delivery of pyrimidines and purine analogs
First Claim
Patent Images
1. A medical device comprising:
- (a) a substrate having a surface; and
(b) a coating disposed on the surface, said coating comprising a polymer matrix including a nucleoside analog, or a codrug or prodrug thereof, which nucleoside analog is formulated to produce an effective concentration of said nucleoside analog in tissue or biological fluid in which the medical device is implanted over a period of at least 15 days.
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Abstract
Disclosed is a sustained release system that includes a polymer, a nucleoside analog or prodrug or codrug thereof, and optionally one or more additives that reduce the rate of release of the drug from the polymer. The device using such inventive system permits improved drug delivery in a localized manner over a prolonged period of time.
212 Citations
31 Claims
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1. A medical device comprising:
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(a) a substrate having a surface; and
(b) a coating disposed on the surface, said coating comprising a polymer matrix including a nucleoside analog, or a codrug or prodrug thereof, which nucleoside analog is formulated to produce an effective concentration of said nucleoside analog in tissue or biological fluid in which the medical device is implanted over a period of at least 15 days. - View Dependent Claims (6, 7, 8, 9, 13, 14, 15, 17, 23, 24, 25, 26, 27, 28, 29)
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2. A medical device comprising:
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(a) a substrate having a surface; and
(b) a coating disposed on the surface, said coating comprising a polymer matrix including a soluble nucleoside analog, and one or more additives which decrease the rate of release of the nucleoside analog into the biological fluid or tissue surrounding the device, wherein the nucleoside analog is released from said polymer matrix at a rate of release to produce an effective concentration of said nucleoside analog in tissue or biological fluid in which the medical device is implanted.
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3. A medical device comprising:
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(a) a substrate having a surface; and
(b) a coating disposed on the surface, said coating comprising a polymer matrix including a prodrug/codrug, wherein said prodrug/codrug is represented by the general formula A—
L—
B, in whichA represents a nucleoside analog or a prodrug thereof;
L represents a covalent bond or covalent linker linking A and B to form the prodrug/codrug, wherein the bond or linker is metabolized under physiological conditions; and
B represents a moiety which, when linked to A, results in a compound having an optimized solubility for sustained release of said nucleoside analog from the coated device at the implanted site. - View Dependent Claims (10, 11, 12, 16, 18, 19, 20, 21, 22)
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4. A medical device comprising:
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(a) a substrate having a surface; and
(b) a coating disposed on the surface, said coating comprising a polymer matrix including a reduced solubility prodrug/codrug, wherein said prodrug/codrug is represented by the general formula of A;
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B, in whichA represents a nucleoside analog or a derivative thereof;
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represents an ionic bond between A and B that dissociates under physiological conditions to generate said pharmaceutically active form of A; and
B represents a moiety which, when linked to A, results in a compound having an optimized solubility for sustained delivery in vivo from the coated device.
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5. A medical device comprising:
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(a) a substrate having a surface; and
(b) a coating disposed on the surface, said coating comprising a polymer matrix including 5-fluorouracil.
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30. A method of manufacturing a coating for a medical device, comprising admixing a polymer matrix and a pharmaceutically effective amount of a nucleoside analog, or a codrug or prodrug thereof, which nucleoside analog is formulated in a form having a solubility less than 0.1 mg/mL in water at 25°
- C.
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31. Use of a polymeric coating in the manufacture of a device to place in a patient for treatment of said patient with a sustained dosage regimen of a nucleoside analog, which nucleoside analog is formulated in a form having a solubility less than 0.1 mg/mL in water at 25°
- C.
Specification