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Details for Patent: 6,051,576

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Details for Patent: 6,051,576

Title: Means to achieve sustained release of synergistic drugs by conjugation
Abstract:A codrug composition of at least two drug compounds covalently linked to one another via a labile bond to form a single codrug composition, or ionically linked to one another to form a single workings composition, and methods of use of the codrug for the treatment of various medical conditions. The codrug may be administered by itself or in the form of a bioerodible or nonbioerodible substance.
Inventor(s): Ashton; Paul (Boston, MA), Crooks; Peter Anthony (Lexington, KY), Cynkowski; Tadeusz (Lexington, KY), Cynkowska; Grazyna (Lexington, KY), Guo; Hone (Malden, MA)
Assignee: University Of Kentucky Research Foundation (Lexington, KY)
Filing Date:Jan 29, 1997
Application Number:08/791,071
Claims:1. A sustained release, and substantially inactive codrug, comprising at least two drugs ionically or covalently linked to one another wherein each active drug is regenerated upon bond cleavage.

2. A codrug according to claim 1, wherein said codrug comprises suramin ionically linked to amiloride.

3. A codrug according to claim 1, wherein said codrug is in injectable form.

4. A codrug according to claim 3, wherein said injectable form is selected from the group consisting of liposomes, suspensions, microsphere and nanoparticles.

5. A codrug according to claim 1, wherein said codrug is in solid form.

6. A codrug according to claim 1, wherein said codrug is applied topically.

7. A codrug according to claim 1, wherein said codrug applied topically is in a form selected from the group consisting of a transdermal patch, ointment, cream, suspension, liquid, elixir and eye drop.

8. A codrug according to claim 1, wherein said codrug is administered by a method selected from the group consisting of injection, inhalation, implantation, applied as a nasal spray, applied rectally, applied vaginally, ingested orally and applied topically.

9. A codrug according to claim 1, wherein said codrug is fixed to an implantable device.

10. A codrug according to claim 1, wherein said codrug is a coating on an implantable device.

11. A codrug according to claim 10, wherein said implantable device is or is attached to a suture.

12. A codrug according to claim 1, wherein said codrug is in the form of a nonerodible delivery vehicle.

13. A codrug according to claim 12, wherein said nonerodible delivery vehicle comprises polyvinyl alcohol.

14. A codrug according to claim 12, wherein said codrug comprises from 0.1 to up to about 100% of said nonerodible delivery vehicle.

15. A codrug according to claim 1, wherein said codrug is in the form of an erodible delivery vehicle.

16. A codrug according to claim 1, wherein said codrug comprises one molecule of suramin ionically linked to six molecules of amiloride.

17. A codrug according to claim 15, wherein said codrug comprises from 0.1 to up to about 100% of said erodible delivery vehicle.

18. A codrug according to claim 1, wherein said codrug comprises ethacrynic acid covalently linked to atenolol.

19. A codrug according to claim 1, wherein said codrug comprises 17.alpha.-21-trihydroxy-5.beta. pregnane-20-one (THS) covalently linked to form a codrug with 5FU and diethylene glycol.

20. A codrug according to claim 1, wherein said codrug comprises 17.alpha.-21-trihydroxy-5.beta. pregnane-20-one (THS) covalently linked to form a codrug with 5FU and tetraethylene glycol.

21. A codrug according to claim 1, wherein said codrug comprises prostaglandin F2 alpha (PGF2.alpha.) covalently linked to form a codrug with timolol (TM).

22. A method of inhibiting angiogenesis comprising administering an effective amount of a codrug according to claim 2 to a patient in need of angiogenesis inhibition.

23. A codrug according to claim 1, which is essentially insoluble in body fluids.

24. A codrug according to claim 1, wherein each drug is released in equimolar amounts.

25. A codrug according to claim 1, wherein at least three drugs are ionically or covalently linked to one another via an ionic bond or covalent bond.

26. A codrug according to claim 1, wherein release of the active drugs follows pseudo zero order kinetics.

27. A codrug according to claim 1, wherein the drugs are ionically linked and release of the active drugs follows pseudo zero order kinetics for about 10 days to about 6 weeks.

28. A codrug according to claim 27, wherein release of each active drug follows pseudo zero order kinetics for about 3 weeks.

29. A codrug according to claim 1, which is soluble in body fluids.

30. A composition comprising a codrug according to claim 1, and a pharmaceutically acceptable carrier.

31. A sustained release, and substantially inactive codrug, comprising at least two drugs covalently linked to one another wherein each active drug is regenerated upon bond cleavage.

32. A codrug according to claim 31, wherein said codrug is a coating on an implantable device.

33. A codrug according to claim 32, wherein said implantable device is a suture.

34. A codrug according to claim 31, wherein said codrug is in the form of a nonerodible delivery vehicle.

35. A codrug according to claim 34, wherein the nonerodible delivery vehicle comprises polyvinyl alcohol.

36. A codrug according to claim 31, wherein each drug is released in equimolar amounts.

37. A codrug according to claim 31, wherein release of each active drug follows pseudo zero order kinetics for about three weeks.
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