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Publication Number
US-10117938-B2
Publication Date
2018-11-06
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 aqueous injectable pharmaceutical composition that combines a soluble corticosteroid with at least one viscosity enhancing agent. The viscosity enhancing agent is sodium hyaluronate or hyaluronic acid, and the composition is designed so that the viscosity enhancing agent prolongs local corticosteroid residency and provides slow release. The aqueous pharmaceutical composition is substantially free of insoluble corticosteroids.
In one described embodiment, the soluble corticosteroid is selected from soluble salts and esters of dexamethasone, including dexamethasone sodium phosphate. The composition further includes at least one viscosity enhancing agent 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. The formulation is described as suitable for local injection to treat inflammation and/or pain.
The document describes providing injectable compositions for local routes including epidural space delivery, and also describes injection concepts such as syringeability and injectability, including reducing a stringing effect. Experimental support is provided using SP-102 (dexamethasone sodium phosphate with sodium hyaluronate), showing increased viscosity with higher hyaluronate levels and decreased release rate with higher hyaluronate levels. Stability and in vivo localization are described using an epidural contrast study and histopathology after injection.
Claims Coverage
The independent claim is directed to a method for treating inflammation and/or pain by injecting a specific aqueous pharmaceutical composition into the epidural space. Across the dependent claims, inventive features mainly cover (i) specific corticosteroid/viscosity-enhancer selections with defined molecular weight and concentration ranges, (ii) the composition being substantially free of insoluble corticosteroids, and (iii) selected constraints on injection force, injection route, and formulation characteristics such as viscosity and optional additional components.
Injecting an aqueous pharmaceutical composition into the epidural space with soluble corticosteroid and a viscosity enhancing agent
Injecting an aqueous pharmaceutical composition into the epidural space of the individual for treating inflammation and/or pain, wherein the aqueous pharmaceutical composition comprises a soluble corticosteroid selected from the group consisting of soluble salts and esters of dexamethasone, and at least one viscosity enhancing agent.
Sodium hyaluronate or hyaluronic acid viscosity enhancing agent with defined molecular weight and concentration
Wherein the at least one viscosity enhancing agent is sodium hyaluronate or hyaluronic acid, the molecular weight of the 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.
Aqueous pharmaceutical composition substantially free of insoluble corticosteroids
And wherein the aqueous pharmaceutical composition is substantially free of insoluble corticosteroids.
The claim set centers on epidural injection of an aqueous formulation containing a soluble dexamethasone corticosteroid and a sodium hyaluronate/hyaluronic acid viscosity enhancer with specified molecular weight and concentration ranges, while excluding insoluble corticosteroids. Dependent claims further narrow the method with route and/or injection-force constraints and additional formulation limitations such as viscosity and optional preservative/anesthetic.
Stated Advantages
Prolongs local corticosteroid residency and provides slow release.
Enables sustained treatment of inflammation and/or pain via local injections.
Supports syringeability and injectability, including reduced stringing effect.
In vivo epidural contrast studies show longer localization/residency half-life compared to commercial products.
Histopathology shows no infection/hemorrhage after injection.
Documented Applications
Local injection into the epidural space (epidural space delivery) for treating inflammation and/or pain in an individual in need thereof.
Local injection routes described include interlaminar injection, caudal injection, and transforaminal injection within the epidural context.
In vivo epidural contrast localization studies using contrast dye and histopathology after injection.
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