PROLONGED DRUG-ELUTING PRODUCTS
A drug-eluting product is disclosed comprising an at least partially bioabsorbable element and an active pharmaceutical agent having a morphology, a solubility, and an average particle size which are selected so that the active pharmaceutical agent continues to dissolve during the biodegradation of the bioabsorbable element. The morphology is a crystalline, semi-crystalline or amorphous morphology, the solubility is less than 100 μg/ml and the average particle size is grater that about 100 nm.
1 . A drug-eluting product comprising an at least partially bioabsorbable element and including an active pharmaceutical agent having a morphology, a solubility and an average particle size which are selected so that said active pharmaceutical agent continues to dissolve during the biodegradation of said bioabsorbable element, said morphology comprising a crystalline, semi-crystalline, or amorphous morphology, said solubility comprising a solubility of less than 100 μg/ml and said average particle size being greater than about 100 nm.
2 . The drug-eluting product of claim 1 , wherein said active pharmaceutical agent has an average particle size of between about 1 and 10 μ.
3 . The drug-eluting product of claim 1 , wherein said active pharmaceutical agent has a solubility of less than about 75 μg/ml.
4 . The drug-eluting product of claim 1 , wherein said active pharmaceutical agent includes a first portion of said active pharmaceutical agent having a particle size of between about 1 and 4 μ, and a second portion of said active pharmaceutical agent having a particle size of between about 2 and 10 μ.
5 . The drug-eluting product of claim 1 , comprising a drug-eluting stent.
6 . The drug-eluting product of claim 1 , wherein said active pharmaceutical agent continues to dissolve for a period of at least about 3 months.
7 . The drug-eluting product of claim 1 , wherein said active pharmaceutical agent continues to dissolve for a period of at least about 6 months.
8 . The drug-eluting product of claim 1 , wherein said active pharmaceutical agent continues to dissolve for a period of at least about 9 months.
9 . The drug-eluting product of claim 1 , wherein said active pharmaceutical agent continues to dissolve for a period of at least about 12 months.
10 . The drug-eluting product of claim 1 , wherein said active pharmaceutical agent continues to dissolve for a period of at least about 18 months.
11 . The drug-eluting product of claim 1 , wherein said drug-eluting product includes a degradable component and a polymer coating disposed on said degradable component, wherein said at least partially bioabsorbable element comprises a bioabsorbable polymer coating disposed on said degradable component.
12 . The drug-eluting product of claim 11 , wherein said at least partially bioabsorbable element comprises a bioabsorbable polymer disposed on said degradable component, and said degradable component comprises a bioabsorbable substrate.
13 . The drug-eluting product of claim 12 , wherein said active pharmaceutical agent comprises a first active pharmaceutical agent, and including a second active pharmaceutical agent associated with said degradable component.
14 . The drug-eluting product of claim 13 , wherein said first and second active pharmaceutical agents comprise different active pharmaceutical agents.
15 . The drug-eluting product of claim 14 , wherein said first active pharmaceutical agent has a first drug elution profile and said second active pharmaceutical agent has a second drug elution profile.
16 . The drug-eluting product of claim 15 , wherein said first drug elution profile is shorter than said second drug elution profile.
17 . The drug-eluting product of claim 12 , wherein said bioabsorbable substrate comprise a bioabsorbable polymer or metal.
18 . The drug-eluting product of claim 1 , wherein said degradable component comprises a bioabsorbable polymer, a bioabsorbable metal, a degradable carrier, an excipient, or a pill core.
19 . A method of preparing a drug-eluting product comprising
providing an at least partially bioabsorbable element; and
including an active pharmaceutical agent in said at least partially bioabsorbable element, said active pharmaceutical agent having a morphology, a solubility and a predetermined configuration selected so that said active pharmaceutical agent will continue to dissolve during the entire biodegradation of said biodegradable element, said morphology comprising a crystalline, amorphous, or semi-crystalline morphology, said solubility comprising a solubility of less than 100 μg/ml, and said predetermined configuration comprising a soluble particle size large enough to permit said active pharmaceutical agent to continue to dissolve for a period of greater than about one year.
20 . The method of claim 19 , including selecting an active pharmaceutical agent having an average particle size large enough so that said active pharmaceutical agent continues to dissolve during the biodegradation of said biodegradable element.
21 . The method of claim 20 , wherein said active pharmaceutical agent has an average particle size greater than about 0.5 microns.
22 . The method of claim 20 , wherein said active pharmaceutical agent has an average particle size between about 1 and 10 microns.
23 . The method of claim 20 , wherein said active pharmaceutical agent includes a first portion of said active pharmaceutical agent having a particle size between about 0.5 and 10 microns, and a second portion of said active pharmaceutical agent having a particle size between about 0.5 and 100 microns.
24 . The method of claim 23 , wherein the second portion of said active pharmaceutical agent has a greater particle size than that of said first portion of said active pharmaceutical agent.
25 . The method of claim 1 , wherein said drug-eluting product comprises a drug-eluting stent.
26 . The method of claim 1 , wherein said drug-eluting product comprises a substrate and a polymer coating disposed on said substrate.
27 . The method of claim 26 , wherein said at least partially biodegradable element comprises a biodegradable polymer coating disposed on said substrate.
28 . The method of claim 26 , wherein said at least partially biodegradable element comprises a biodegradable polymer coating disposed on said substrate, and said substrate comprises a biodegradable substrate.
29 . The method of claim 28 , wherein said biodegradable substrate comprises a bioabsorbable polymer or metal.
30 . A drug-eluting product comprising a degradable component having a predetermined period of degradation of greater than about 100 days and including an active pharmaceutical agent having a morphology, a solubility and a particle size distribution so that said active pharmaceutical agent will be released over the entire predetermined period of degradation of said degradable component, said morphology comprising a crystalline, amorphous, or semi-crystalline morphology, said solubility comprising a solubility of less than 100 μg/ml, and said particle size distribution comprising greater than about 0.5 μm.
31 . The drug-eluting product of claim 30 , wherein said active pharmaceutical agent is released substantially continuously over the predetermined period of degradation of said degradable component.
32 . The drug-eluting product of claim 30 , wherein said degradable component comprises bioabsorbable polymers, bioabsorbable metals, degradable carriers, or excipients.
33 . The drug-eluting product of claim 30 , wherein said drug-eluting product comprises implants, oral pharmaceuticals, injectables, trans-mucosals, inhalants, or topicals.
34 . The drug-eluting product of claim 30 , wherein said drug-eluting product comprises a drug-eluting stent.
35 . The drug-eluting product of claim 34 , wherein said substrate comprises a bioabsorbable polymer or a bioabsorbable metal.
36 . The drug-eluting product of claim 30 , wherein said active pharmaceutical agent has an average particle size between about 0.5 μm and 100 μm.
37 . The drug-eluting product of claim 30 , wherein said active pharmaceutical agent has an average particle size of greater than about 100 nm.
38 . The drug-eluting product of claim 30 , wherein said active pharmaceutical agent includes a first portion of said active pharmaceutical agent having a particle size of between about 1 and 4 microns, and a second portion of said active pharmaceutical agent having a particle size of between about 2 and 10 microns.
39 . The drug-eluting product of claim 30 , including a polymer coating disposed on said degradable component.
40 . The drug-eluting product of claim 39 , wherein said polymer coating comprises a bioabsorbable polymer.
41 . The drug-eluting product of claim 30 , wherein said substrate includes an at least partially bioabsorbable polymer.
42 . The drug-eluting product of claim 41 , wherein said bioabsorbable polymer is disposed on said degradable component.
43 . The drug-eluting product of claim 41 , wherein said bioabsorbable polymer is mixed with said degradable component.