You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 19, 2024

Details for Patent: 6,051,576


✉ Email this page to a colleague

« Back to Dashboard


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.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.