Danegaptide Formulation for Application in the Eye
AssigneeBreye Therapeutics ApS
InventorUlrik Mouritzen
Life of this patent
Estimating the term…
Abstract
The present disclosure relates to a slow and extended release formulation of danegaptide.
Claims36
A biodegradable intraocular implant comprising:
- a hydrophilic compound of formula (I),
- or a hydrophilic pharmaceutically acceptable salt thereof;
- and an extended-release or sustained release biodegradable polymer matrix.
The implant according to any one of the preceding claims, wherein the implant comprises about 21 μg, about 22 μg, about 23 μg, about 24 μg, about 25 μg, about 26 μg, about 27 μg, about 28 μg, about 29 μg, about 30 μg, about 31 μg, about 32 μg, about 33 μg, about 34 μg, about 35, about 36 μg, about 37 μg, about 38 μg, about 39 μg, or about 40 μg of the compound or a pharmaceutically acceptable salt thereof.
The implant of any one of claims 24 to 27, wherein upon placement in the vitreous of the eye or other posterior segments of the eye, the implant maintains a concentration of at least 50 nM of the compound in the retinal tissue.
The implant of any one of claims 24 to 29, wherein upon placement in the vitreous of the eye or other posterior segments of the eye, the implant is configured to release from about 0.1 μg per day to about 2 μg per day of the compound or a pharmaceutically acceptable salt thereof.
The implant of any one of claims 24 to 30, wherein upon placement in the vitreous of the eye or other posterior segments of the eye, the implant is configured to provide an initial burst release of the compound or a pharmaceutically acceptable salt thereof followed by a lower steady state concentration of the compound or a pharmaceutically acceptable salt thereof.
The implant of claim 31, wherein the initial burst release provides a concentration of from about 10 to 50 ng/mL of the compound or a pharmaceutically acceptable salt thereof in the ocular compartment.
The implant of claim 31 or 32, wherein the lower steady state concentration of the compound or a pharmaceutically acceptable salt thereof is from about 50 nM to about 125 nM steady state concentration.
The implant of any one of claims 31 to 33, wherein the initial burst release provides a dose of from about 150 to about 300 ng of the compound or a pharmaceutically acceptable salt thereof over two days from the time the implant is placed in the vitreous of the eye.
The implant of any one of claims 24 to 34, wherein upon placement the vitreous of the eye or other posterior segments of the eye, the implant is configured to release the compound or a pharmaceutically acceptable salt thereof for at a period of time of least one month to three months.
Dependencies are inferred from the claim text.