OCULAR IMPLANT CONTAINING A TYROSINE KINASE INHIBITOR
The invention relates to a sustained release biodegradable ocular implant containing a tyrosine kinase inhibitor dispersed in a hydrogel for the treatment of a retinal disease for an extended period of time.
1 - 30 . (canceled)
31 . A sustained release biodegradable ocular implant comprising a therapeutically effective amount of axitinib dispersed in a hydrogel, wherein the implant comprises, on a dry weight basis, about 50% by weight or more axitinib, about 40% by weight or less polyethylene glycol (PEG) and one or more phosphate salts, and wherein on a dry weight basis the axitinib to PEG ratio in the implant is from about 1:1 to about 3:1.
32 . The sustained release biodegradable ocular implant of claim 31 , comprising from about 200 g to about 600 g axitinib.
33 . The sustained release biodegradable ocular implant of claim 32 , wherein the implant in a dried state contains from about 50% to about 75% by weight axitinib and from about 20% to about 40% by weight polyethylene glycol units.
34 . The sustained release biodegradable ocular implant of item 33, wherein the implant in a dried state contains from about 50% to about 65% by weight axitinib and from about 25% to about 40% by polyethylene glycol units.
35 . The sustained release biodegradable ocular implant of item 34, wherein the implant in a dried state contains from about 50% to about 55% by weight axitinib and from about 37% to about 40% by weight polyethylene glycol units.
36 . The sustained release biodegradable ocular implant of claim 35 , wherein the implant in its dry state has a length from about 6 mm to about 17 mm.
37 . The sustained release biodegradable ocular implant of claim 36 , wherein the implant in its dry state has a length from about 6 mm to about 10 mm.
38 . The sustained release biodegradable ocular implant of claim 37 , wherein the implant in its dry state has a length from about 6 mm to about 9 mm.
39 . The sustained release biodegradable ocular implant of claim 38 , wherein the implant in its dry state has a diameter from about 0.1 mm to about 0.5 mm.
40 . The sustained release biodegradable ocular implant of claim 39 , wherein the implant in its dry state has a diameter from about 0.2 mm to about 0.4 mm.
41 . The sustained release biodegradable ocular implant of claim 40 , wherein the implant in its dry state has a diameter from about 0.3 mm to about 0.4 mm.
42 . The sustained release biodegradable ocular implant of claim 41 , wherein the implant in its dry state has a a total implant weight of about 0.2 mg to about 1.5 mg.
43 . The sustained release biodegradable ocular implant of claim 42 , wherein the implant in its dry state has a total implant weight of about 0.2 mg to about 1.2 mg.
44 . The sustained release biodegradable ocular implant of claim 42 , wherein the implant in its dry state has a total implant weight of about 0.75 mg to about 1.25 mg.
45 . The sustained release biodegradable ocular implant of claim 44 , wherein the implant in its wet state has a length from about 6 mm to about 12 mm.
46 . The sustained release biodegradable ocular implant of claim 45 , wherein the implant in its wet state has a length from about 6 mm to about 10 mm.
47 . The sustained release biodegradable ocular implant of claim 46 , wherein the implant in its wet state has a length from about 6 mm to about 8 mm.
48 . The sustained release biodegradable ocular implant of claim 47 , wherein the implant in its wet state has a diameter from about 0.5 mm to about 0.8 mm.
49 . The sustained release biodegradable ocular implant of claim 48 , wherein the cross-sectional area of the fiber is round, essentially round, oval, oblong, cross-shaped, star shaped, rectangular or triangular.
50 . The sustained release biodegradable ocular implant of claim 49 , wherein the fiber is cylindrical or essentially cylindrical.
51 . The sustained release biodegradable ocular implant of claim 50 , wherein the fiber is non-cylindrical.
52 . The sustained release biodegradable ocular implant of claim 49 , wherein the cross-sectional geometry of the fiber enables loading the implant into a needle suitable for injection into the vitreous humor.
53 . The sustained release biodegradable ocular implant of claim 52 , wherein the needle has a gauge size of from 22 to 30.
54 . The sustained release biodegradable ocular implant of claim 53 , wherein the tip of the needle is occluded with a water soluble biocompatible material.
55 . The sustained release biodegradable ocular implant of claim 54 , wherein the material comprises polyethylene glycol, poloxamer; crystallized sugar, salt, agarose, cellulose, polyvinyl alcohol, poly(lactic-co-glycolic acid), UV-curing polymer, chitosan or combinations thereof
56 . The sustained release biodegradable ocular implant of claim 55 , wherein the material comprises polyethylene glycol.
57 . The sustained release biodegradable ocular implant of claim 56 , wherein the tip of the needle is occluded with polyethylene glycol by dipping the tip into a molten polyethylene glycol.
58 . The sustained release biodegradable ocular implant of claim 56 , wherein the tip of the needle is occluded with polyethylene glycol by placing molten polyethylene glycol into the needle tip lumen.
59 . The sustained release biodegradable ocular implant of claim 56 , wherein the polyethylene glycol has a melting point between about 33° C. and about 40° C.
60 . The sustained release biodegradable ocular implant of claim 56 , wherein the polyethylene glycol melts at body temperature when the needle is injected into the eye.