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Publication Number
US-11020485-B2
Publication Date
2021-06-01
Expiration Date
Abstract
Disclosed are aqueous pharmaceutical compositions which provide sustained released delivery of corticosteroid compounds. The pharmaceutical composition comprises a soluble corticosteroid and at least one viscosity enhancing agent. Also provided are methods for using the pharmaceutical compositions in an epidural injection, intra-articular injection, or an intra-lesional injection.
Core Innovation
The invention relates to an injectable aqueous pharmaceutical composition comprising a soluble corticosteroid selected from the group consisting of soluble salts and esters of dexamethasone, together with at least one viscosity enhancing agent. The viscosity enhancing agent is sodium hyaluronate or hyaluronic acid, with defined molecular weight and concentration, to provide controlled viscosity and a sustained-release/local injectable corticosteroid composition.
A specific exclusion is used: the injectable aqueous pharmaceutical composition does not comprise insoluble dexamethasone acetate. The disclosed formulations further specify defined ranges for the amount of soluble corticosteroid per dose and defined parameters for the viscosity enhancing agent, including molecular weight between about 1.0 MDa and 2.5 MDa and viscosity-enhancing agent concentration between about 1.0% w/v and 1.5% w/v.
The disclosed compositions are intended for local injectable administration including epidural injection, intra-articular injection, and intra-lesional injection. The document reports that higher viscosity-enhancing agent levels reduce the release rate, and that the injectable compositions exhibit stability under ambient conditions.
Claims Coverage
The provided claim set includes one main inventive concept centered on a defined injectable aqueous composition using a soluble dexamethasone salt or ester with sodium hyaluronate or hyaluronic acid viscosity enhancement, while excluding insoluble dexamethasone acetate. Dependent claims further specify the corticosteroid form, the viscosity agent identity, narrower molecular weight and concentration ranges, a target dexamethasone concentration, and a preservative-free composition.
Injectable aqueous composition with soluble dexamethasone salt or ester
An injectable aqueous pharmaceutical composition comprising a soluble corticosteroid selected from the group consisting of soluble salts and esters of dexamethasone, wherein the soluble corticosteroid is present between 2 mg and 20 mg per dose.
Viscosity enhancement using sodium hyaluronate or hyaluronic acid with defined molecular weight and concentration
An injectable aqueous pharmaceutical composition wherein at least one viscosity enhancing agent is sodium hyaluronate or hyaluronic acid, the molecular weight is between 1.0 MDa and 2.5 MDa, and the concentration is between 1.0% w/v and 1.5% w/v.
Exclusion of insoluble dexamethasone acetate
An injectable aqueous pharmaceutical composition wherein the composition does not comprise insoluble dexamethasone acetate.
Dexamethasone sodium phosphate as the soluble corticosteroid
The injectable aqueous pharmaceutical composition wherein the soluble corticosteroid is dexamethasone sodium phosphate.
Sodium hyaluronate as the viscosity enhancing agent
The injectable aqueous pharmaceutical composition wherein the viscosity enhancing agent is sodium hyaluronate.
Sodium hyaluronate viscosity-agent molecular weight and concentration constraints
An injectable aqueous pharmaceutical composition including dexamethasone sodium phosphate and sodium hyaluronate as a viscosity-enhancing agent, with sodium hyaluronate having a molecular weight between 1.0 MDa and 2.0 MDa and a concentration of about 1.25% w/v.
Target dexamethasone concentration
An injectable aqueous pharmaceutical composition formulated with a soluble dexamethasone salt or ester such that the resulting dexamethasone concentration is about 5 mg/mL.
Preservative-free injectable composition
The injectable aqueous pharmaceutical composition is preservative-free.
The inventive coverage centers on a defined injectable aqueous formulation: a soluble dexamethasone salt or ester, including dexamethasone sodium phosphate, combined with sodium hyaluronate or hyaluronic acid viscosity enhancement having specified molecular weight and concentration parameters, while explicitly excluding insoluble dexamethasone acetate.
Stated Advantages
Prolonged epidural residency half-life relative to commercial products.
Reduced release rate with increased viscosity-enhancing agent level.
Ambient stability of the compositions.
Histopathology indicates no hemorrhage/necrosis after injection.
Documented Applications
Local administration by epidural injection.
Local administration by intra-articular injection.
Local administration by intra-lesional injection.
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