Methods of treating inflammation and/or pain
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Publication Number
US-12016867-B2
Publication Date
2024-06-25
Expiration Date
Abstract
Disclosed are aqueous pharmaceutical compositions which provide sustained released delivery of corticosteroid compounds. The pharmaceutical composition comprises an insoluble corticosteroid; 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, intra-lesional injection, or an intra-ocular injection.
Core Innovation
The invention relates to an aqueous pharmaceutical composition for injection that combines an insoluble corticosteroid with a soluble corticosteroid, together with at least one viscosity enhancing agent. The viscosity enhancing agent is sodium hyaluronate or hyaluronic acid, and the insoluble and soluble corticosteroids are selected from salts and esters of dexamethasone.
The composition is defined by specific viscosity-enhancing agent parameters, including a molecular weight between 1.0 MDa and 2.5 MDa and a concentration between 1.0% w/v and 1.5% w/v. The formulation concept uses the presence of both insoluble corticosteroid and soluble corticosteroid within the same aqueous pharmaceutical composition.
The invention provides methods of treating inflammation and/or pain by injecting the aqueous pharmaceutical composition into an intra-articular space of an individual in need thereof. The document also describes injection-based treatment of epidural, intra-lesional, and intra-ocular spaces, linking delivery to anti-inflammatory and analgesic effects.
Claims Coverage
The partial content includes one independent method claim and dependent refinements that add specific selections for corticosteroid types, viscosity-enhancing agent constraints, and injection administration constraints.
Intra-articular injection using an insoluble and soluble corticosteroid with a hyaluronate viscosity enhancer
A method of treating inflammation and/or pain by injecting an aqueous pharmaceutical composition into an intra-articular space, wherein the composition comprises an insoluble corticosteroid, a soluble corticosteroid, and at least one viscosity enhancing agent, with the viscosity enhancing agent being sodium hyaluronate or hyaluronic acid, and the insoluble and soluble corticosteroids being selected from salts and esters of dexamethasone.
Molecular weight and concentration limits for the hyaluronate viscosity enhancing agent
The method wherein the molecular weight of at least one viscosity enhancing agent is between 1.0 MDa and 2.5 MDa and the concentration of the at least one viscosity enhancing agent is between 1.0% w/v and 1.5% w/v.
Dexamethasone sodium phosphate and dexamethasone acetate selection
The method wherein the insoluble and soluble corticosteroids include dexamethasone sodium phosphate and dexamethasone acetate.
Viscosity enhancing agent defined by molecular weight and concentration
The method wherein sodium hyaluronate is used as the viscosity enhancing agent with molecular weight between 1.0 MDa and 2.0 MDa and a concentration of about 1.25% w/v.
Dexamethasone concentration constraint
The method in which dexamethasone sodium phosphate and dexamethasone acetate are present in amounts to achieve a dexamethasone concentration of about 5 mg/mL.
Injection force constraint for intra-articular administration
The method wherein the aqueous pharmaceutical composition is injected using less than 27 N of force.
Injection rate constraint for intra-articular administration
The method wherein the aqueous pharmaceutical composition is injected into the intra-articular space at a rate of about 0.5 in³/min.
Administration interval constraint
The method wherein an individual in need is injected with the aqueous pharmaceutical composition once every 4 to 24 weeks.
Across the independent claim and dependent refinements, the inventive method is anchored on intra-articular injection of an aqueous pharmaceutical composition containing both insoluble and soluble dexamethasone salts/esters with sodium hyaluronate or hyaluronic acid, constrained by hyaluronate molecular-weight and concentration limits. Additional dependent features further specify corticosteroid forms and injection and dosing constraints.
Stated Advantages
Reduced settling, shelf stability, and improved injection/syringeability are described in the partial content.
The soluble and insoluble corticosteroid fractions are described as providing quick onset and long duration anti-inflammatory and analgesic effects.
Documented Applications
Treating inflammation and/or pain by injecting an aqueous pharmaceutical composition into an intra-articular space.
Epidural injection is described for treating inflammation and/or pain in the document.
Intra-lesional injection is described for treating inflammation and/or pain in the document.
Intra-ocular injection is described for treating inflammation and/or pain in the document.
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