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Publication Number
US-10500284-B2
Publication Date
2019-12-10
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 describes an injectable aqueous pharmaceutical composition that combines a soluble corticosteroid selected from soluble salts and esters of dexamethasone with at least one viscosity enhancing agent. The viscosity enhancing agent is sodium hyaluronate or hyaluronic acid, having a molecular weight between 1.0 MDa and 2.5 MDa and a concentration between 1.0% w/v and 1.5% w/v, and the composition excludes insoluble dexamethasone acetate.
The invention further describes aqueous local-injection corticosteroid formulations using sodium hyaluronate or hyaluronic acid to achieve sustained or local exposure. The disclosed formulation options include viscosity characterization and composition parameters such as buffering agents, pH, osmolality, and optional components including anesthetic, preservative, and surfactant.
The invention also describes packaging formats including vials and syringes, including two-compartment packaging. It additionally discloses administration for epidural, intra-articular, and intra-lesional injection, including characterization of injectability and reduction of needle stringing. Example formulations are described with varying sodium hyaluronate concentration and molecular weight, together with physical/chemical characterization, dissolution profile, accelerated stability, and in vivo pig epidural diffusion data.
Claims Coverage
The partial content provides two independent claims, covering an injectable aqueous pharmaceutical composition and a syringe containing that composition. Both claims share the core composition system: soluble dexamethasone plus sodium hyaluronate or hyaluronic acid with defined molecular-weight and concentration ranges, and both expressly exclude insoluble dexamethasone acetate.
Injectable aqueous pharmaceutical composition with soluble dexamethasone and hyaluronate viscosity enhancer excluding insoluble dexamethasone acetate
An injectable aqueous pharmaceutical composition comprising a soluble corticosteroid selected from soluble salts and esters of dexamethasone, and at least one viscosity enhancing agent, wherein the viscosity enhancing agent is sodium hyaluronate or hyaluronic acid with molecular weight between 1.0 MDa and 2.5 MDa and concentration between 1.0% w/v and 1.5% w/v, and wherein the composition does not comprise insoluble dexamethasone acetate.
Syringe containing injectable aqueous composition with soluble dexamethasone and hyaluronate viscosity enhancer excluding insoluble dexamethasone acetate
A syringe comprising an injectable aqueous pharmaceutical composition, wherein the injectable aqueous pharmaceutical composition comprises a soluble corticosteroid selected from soluble salts and esters of dexamethasone and at least one viscosity enhancing agent, wherein the viscosity enhancing agent is sodium hyaluronate or hyaluronic acid with molecular weight between 1.0 MDa and 2.5 MDa and concentration between 1.0% w/v and 1.5% w/v, and wherein the composition does not comprise insoluble dexamethasone acetate.
Across both independent claims, the inventive concept is an injectable aqueous formulation or syringe formulation containing soluble dexamethasone plus sodium hyaluronate or hyaluronic acid defined by molecular-weight and concentration ranges, while excluding insoluble dexamethasone acetate.
Stated Advantages
Prolonged residency, including epidural residency half-life data in pigs compared to commercial products.
Reduction of needle stringing.
Histopathology findings showing no infection or hemorrhage.
Documented Applications
Epidural injection, including characterized epidural diffusion and residency behavior in pigs.
Intra-articular injection.
Intra-lesional injection.
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