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Publication Number
US-9833460-B2
Publication Date
2017-12-05
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 combining an insoluble corticosteroid and a soluble corticosteroid together with at least one viscosity enhancing agent. The viscosity enhancing agent is sodium hyaluronate or hyaluronic acid, and the insoluble corticosteroid and soluble corticosteroid are dexamethasone. The insoluble form of the corticosteroid has an average particle size of less than 10 μm, and the composition has a viscosity between 10 kcP and 200 kcP.
The composition is characterized by quantitative formulation constraints including the molecular weight of at least one viscosity enhancing agent between 1.0 MDa and 2.0 MDa and the concentration of the at least one viscosity enhancing agent between 1.0% w/v and 1.5% w/v. The formulation concept uses a soluble fraction associated with quick onset and an insoluble fraction associated with prolonged duration, while maintaining desirable local formulation and physical characteristics.
The described pharmaceutical compositions further encompass optional inclusion of an anesthetic and/or a preservative, and can be provided as unit-dose forms such as a syringe. The document describes evaluation of formulation parameters including particle size, spreadability/transport, in vitro dissolution behavior, centrifugation stability, extrusion/injectability force and stringing effect, and settling estimates based on Stoke’s law.
Methods are described for treating inflammation and/or pain in an individual by injecting the aqueous pharmaceutical composition. The document further specifies compatible local administration routes including epidural, intra-articular, intra-lesional, and intra-ocular administration.
Claims Coverage
The partial content includes two independent claims: an aqueous pharmaceutical composition claim with defined formulation parameters and an injection method claim for treating inflammation and/or pain. Both independent claims share the same core compositional constraints, including insoluble and soluble dexamethasone corticosteroids with sodium hyaluronate or hyaluronic acid, defined molecular-weight and concentration ranges, particle size, and viscosity ranges.
Defined aqueous composition of insoluble and soluble dexamethasone with sodium hyaluronate or hyaluronic acid
An aqueous pharmaceutical composition comprising an insoluble corticosteroid and a soluble corticosteroid with at least one viscosity enhancing agent, wherein the at least one viscosity enhancing agent is sodium hyaluronate or hyaluronic acid and the insoluble corticosteroid and soluble corticosteroid are dexamethasone.
Molecular weight and concentration constraints for the viscosity enhancing agent
The molecular weight of at least one viscosity enhancing agent is between 1.0 MDa and 2.0 MDa, and the concentration of the at least one viscosity enhancing agent is between 1.0% w/v and 1.5% w/v.
Particle-size and viscosity constraints for the insoluble corticosteroid and the composition
The insoluble form of the corticosteroid has an average particle size of less than 10 μm, and the pharmaceutical composition has a viscosity of between 10 kcP and 200 kcP.
Injecting the defined aqueous corticosteroid depot composition to treat inflammation and/or pain
A method for treating inflammation and/or pain in an individual in need thereof, comprising injecting an aqueous pharmaceutical composition into the individual, wherein the aqueous pharmaceutical composition comprises an insoluble corticosteroid, a soluble corticosteroid, and at least one viscosity enhancing agent with the same stated constraints for sodium hyaluronate or hyaluronic acid, dexamethasone, molecular weight, concentration, particle size, and viscosity.
Across both independent claims, the coverage centers on an aqueous injectable pharmaceutical composition using an insoluble corticosteroid and a soluble corticosteroid (dexamethasone) combined with sodium hyaluronate or hyaluronic acid under defined molecular-weight and concentration constraints for the viscosity enhancing agent, together with defined insoluble particle-size and overall composition viscosity ranges.
Stated Advantages
The soluble fraction is associated with quick onset and the insoluble fraction is associated with prolonged duration.
The formulation maintains desirable local formulation and physical characteristics.
Optional inclusion of an anesthetic and/or a preservative is supported.
Documented Applications
Treating inflammation and/or pain in an individual by injecting the aqueous pharmaceutical composition.
Local administration routes include epidural, intra-articular, intra-lesional, and intra-ocular administration.
Unit-dose forms such as a syringe are described.
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