Intravitreal corticosteroid extended release implant and methods of use
AssigneeEyedea Bio, LLC
InventorsAndres Garcia, Xunpei Liu
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Abstract
Corticosteroid compositions including a corticosteroid drug substance (e.g., fluocinolone, fluocinolone acetonide, dexamethasone, dexamethasone phosphate, dexamethasone sodium phosphate, triamcinolone, and triamcinolone acetonide) or a or a salt or derivative thereof and one or more irregular-shaped particulate fatty acid or keto-enol tautomer complexation agents admixed in a dispersal medium, having a release profile with one or more phases of drug release. These compositions are extended release corticosteroid compositions may release a clinically useful level of corticosteroid for more than 1 to 12 months within the body. Also described herein are methods of forming and methods of using these compositions.
Claims17
A multiphasic colloidal suspension composition, the composition comprising:
- a corticosteroid drug substance and one or more complexation agents, admixed in a dispersal medium so that the corticosteroid drug substance has a release profile having one or more phases of release of the corticosteroid drug substance into the extracellular environment, wherein the one or more complexation agents is formulated as an irregular-shaped particulate having a Braunauer-Emmett-Teller (BET) surface area greater than about 2.0 m2 g−1 that forms corticosteroid drug substance-complex particulates by noncovalent, reversible binding to the corticosteroid drug substance, and wherein the one or more complexation agents comprises magnesium stearate and a tocopherol compound or calcium stearate and a tocopherol compound;
- wherein the corticosteroid drug substance is any of:
- fluocinolone, fluocinolone acetonide, dexamethasone, dexamethasone phosphate, dexamethasone sodium phosphate, triamcinolone, and triamcinolone acetonide, or a salt thereof;
- further wherein the dispersal medium is a fatty acid methyl esters.
A multiphasic colloidal suspension composition, the composition comprising:
- a corticosteroid drug substance or a salt thereof and one or more complexation agents, admixed in a dispersal medium so that the corticosteroid drug substance has a release profile having one or more phases of drug release, wherein the one or more complexation agents is formulated as an irregular-shaped particulate having a Braunauer-Emmett-Teller (BET) surface area greater than about 2.0 m2 g−1 that forms corticosteroid drug substance-complex particulates by noncovalent, reversible binding to the corticosteroid drug substance, and wherein the one or more complexation agents comprises magnesium stearate and alpha-tocopherol;
- wherein the corticosteroid drug substance is any of:
- fluocinolone, fluocinolone acetonide, dexamethasone, dexamethasone phosphate, dexamethasone sodium phosphate, triamcinolone, and triamcinolone acetonide, or a salt thereof;
- further wherein the dispersal medium is a methyl laurate.
A multiphasic colloidal suspension composition, the composition comprising:
- a corticosteroid drug substance and one or more complexation agents, admixed in a dispersal medium so that the corticosteroid drug substance has a release profile having one or more phases of release of the drug corticosteroid drug substance into the extracellular environment,
- wherein the corticosteroid drug substance is fluocinolone, fluocinolone acetonide or a salt thereof, between about 10% and 60% by weight of the multiphasic colloidal suspension composition,
- wherein the one or more complexation agents is formulated as an irregular-shaped particulate having a Braunauer-Emmett-Teller (BET) surface area greater than about 2.0 m2 g−1 and is between about 1% and 50% by weight of the multiphasic colloidal suspension composition and forms drug corticosteroid drug substance-complex particulates by noncovalent, reversible binding to the corticosteroid drug substance, and wherein the one or more complexation agents is magnesium stearate and a tocopherol or calcium stearate and a tocopherol,
- further wherein the dispersal medium is a hydrophobic liquid oil comprising methyl dodecanoate (methyl laurate) between 1% and 90% by weight of the multiphasic colloidal suspension composition.
Dependencies are inferred from the claim text.