Nitrite Formulation with Ascorbic Acid for Cardiovascular NO Prodrugs
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Solution Overview
Problem
Current treatments for cardiovascular diseases, particularly those related to nitric oxide insufficiency, face challenges due to the short half-life of nitrite, which limits its therapeutic window and effectiveness in acute conditions like heart attacks and strokes.
Innovation Solution
A composition comprising a nitrite salt, a nitrate salt, and ascorbic acid is administered to extend the half-life of nitrite, converting it into nitric oxide in vivo, while L-arginine enhances NO production, thereby providing prolonged cardiovascular benefits and protective effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If nitrite salt is administered alone, then rapid nitric oxide release occurs, but the therapeutic window is limited due to short half-life
Solution Approach 1:
The patent combines nitrite salt with nitrate salt and ascorbic acid in advance to create a formulation that pre-establishes a sustained-release system. The nitrate salt serves as a reservoir that converts to nitrite over time, while ascorbic acid stabilizes the nitrite, thereby extending the therapeutic duration without compromising the initial rapid release
Solution Approach 2:
The invention creates a composite formulation combining nitrite salt, nitrate salt, and ascorbic acid. This composite approach allows the formulation to exhibit both rapid-acting properties (from nitrite) and sustained-release properties (from nitrate conversion and ascorbic acid stabilization), resolving the contradiction between speed and duration
2Reliability
If nitrite is converted to nitric oxide in vivo, then cardiovascular protection is achieved, but carcinogenic compounds may form
Solution Approach 1:
The patent converts the potential harmful reaction of nitrite into carcinogenic compounds by utilizing the beneficial role of ascorbic acid. Ascorbic acid acts as an antioxidant that prevents nitrite from forming carcinogenic nitrosamines, while simultaneously supporting the nitrite-to-nitric-oxide conversion pathway needed for cardiovascular protection
Solution Approach 2:
Ascorbic acid serves as an intermediary substance that mediates between nitrite and potential carcinogenic pathways. It intercepts the harmful reaction pathway while allowing the beneficial nitric oxide generation to proceed, thereby protecting against carcinogenesis without compromising therapeutic effectiveness
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The combination significantly increases nitric oxide bioavailability, extends the therapeutic window for cardiovascular protection, and reduces the formation of carcinogenic compounds, offering both preventive and therapeutic benefits for cardiovascular diseases.
Implementation Method 1
The ascorbic acid blocks the metabolism of nitrite to other compounds (including potentially carcinogenic compounds)
Implementation Method 2
The sodium nitrate, which is converted to nitrite in vivo, provides a longer lasting source of nitrite
Implementation Method 3
converting it into nitric oxide in vivo
Data Source
AI summary
Compositions comprising a nitrite salt, a nitrate salt, and ascorbic acid are provided in several embodiments. A method of enhancing cardiovascular performance or treating adverse cardiovascular event in a mammal is also provided.