Intravenous omega-3 fatty acid compositions and method of use
Inventors
Assignees
United States Department of the Army
Publication Number
US-9675572-B2
Publication Date
2017-06-13
Expiration Date
2031-04-22
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Abstract
The invention encompasses intravenous pharmaceutical compositions containing omega-3 fatty acids and methods of treating traumatic brain injury, traumatic spinal cord injury and/or stroke using these pharmaceutical compositions.
Core Innovation
The invention provides intravenous pharmaceutical compositions comprising omega-3 essential fatty acids and methods for treating subjects undergoing traumatic brain injury, spinal cord injury, or stroke by intravenously administering these compositions. The compositions are stable, highly bioavailable, and comprise a 20% oil-in-water emulsion that includes omega-3 fatty acids such as α-linolenic acid (ALA), eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA), combined with medium chain triglycerides (MCTs), emulsifiers, antioxidants, and osmotic agents. The administration is designed to start as soon as possible following injury and to continue for an extended period to mitigate secondary inflammatory damage.
The problem being solved addresses the lack of effective anti-inflammatory treatments for secondary brain damage caused by the neuroinflammatory response following traumatic brain injury, spinal cord injury, or stroke. Current emergency treatments focus on life-saving maneuvers but do not provide pharmaceutical interventions to modulate inflammation or promote neural repair. Existing parenteral lipid emulsions approved in the United States are insufficient due to their omega-6 fatty acid content, which promotes proinflammatory states. The invention proposes an intravenous omega-3 fatty acid composition absent of omega-6 fatty acids to reduce inflammation and improve outcomes.
Claims Coverage
The patent includes two independent claims focusing on methods of treating subjects with traumatic brain injury, spinal cord injury, and/or stroke by intravenously administering specific stable intravenous pharmaceutical compositions containing omega-3 fatty acids, medium chain triglycerides, emulsifiers, and aqueous components.
Stable intravenous pharmaceutical composition with high omega-3 content
The composition comprises an oil phase with about 5 to 15 g/L α-linolenic acid (ALA) and about 100 to 125 g/L combined eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), at least one medium chain triglyceride (MCT), about 12 g/L egg yolk phospholipids as an emulsifier, and an aqueous phase with about 25 g/L glycerol and about 100 mg/L α-tocopherol, forming a 20% oil-in-water emulsion with omega-3 fatty acids comprising about 50% to 90% by weight of the oil phase, and notably absent of omega-6 fatty acids.
Method of treatment with specified dosage and timing
Intravenous administration of the pharmaceutical composition is performed within about 60 to 120 minutes of trauma or injury, at a dosage ranging from about 0.03 g/kg/day to about 0.3 g/kg/day of omega-3 essential fatty acids. Initial administration involves about 0.2 g to 5 g over 1 to 10 minutes, followed by a continuous infusion for a minimum of 5 to 21 days post trauma or injury.
Use of specific medium chain triglycerides and emulsifier concentrations
The medium chain triglycerides used include caprylic acid and capric acid preferably in a weight ratio of about 3:2. The emulsifier concentration ranges from 0.5% to 4%, with specific embodiments around 1.2% of egg yolk phospholipids, contributing to a stable emulsion suitable for intravenous infusion.
Treatment applicability and subject scope
The methods apply to human subjects suffering from mild, moderate, or severe traumatic brain injury; incomplete spinal cord injury; and mild, moderate, or severe stroke, including both hemorrhagic and ischemic origin strokes.
The claims collectively cover stable intravenous omega-3 fatty acid pharmaceutical compositions free of omega-6 fatty acids, specific formulations including MCTs and emulsifiers, and methods of treatment administering these compositions within defined dosages and timeframes to reduce inflammation and treat traumatic brain injury, spinal cord injury, and stroke in human subjects.
Stated Advantages
Provides a stable and highly bioavailable intravenous formulation of omega-3 fatty acids suitable for emergency and continuous administration.
Offers an anti-inflammatory therapy for traumatic brain injury and spinal cord injury that addresses the secondary inflammatory response not targeted by current treatments.
Reduces proinflammatory effects by absence of omega-6 fatty acids, thereby minimizing secondary brain damage.
Enables early intravenous administration within a critical post-injury window to improve neurologic outcomes.
Documented Applications
Treatment of traumatic brain injury of all severity levels including mild, moderate, and severe cases.
Treatment of spinal cord injury, including incomplete injuries.
Treatment of stroke, including ischemic and hemorrhagic strokes, across mild, moderate, and severe presentations.
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