Co-micronized PEA and Rutin Composition for Vascular Disease Treatment
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Solution Overview
Problem
Vascular remodeling diseases, such as restenosis, hypertension, and atherosclerosis, are characterized by vascular smooth muscle cell growth, endothelial cell proliferation, and oxidative stress, leading to vascular damage and complications like plaque rupture and endothelial dysfunction, which current treatments inadequately address.
Innovation Solution
A composition of palmitoyl-ethanolamide and Rutin in co-micronized form, combined with a triterpene molecule and phytochemical compounds of high antioxidant activity, is developed to treat vascular diseases by enhancing antioxidant capacity and improving vascular tone regulation.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional treatments are used for vascular remodeling diseases, then treatment simplicity is maintained, but therapeutic effectiveness is insufficient
Solution Approach 1:
The patent combines multiple active ingredients (N-palmitoyl-ethanolamide and Rutin) into a single co-micronized composition, merging multiple therapeutic functions into one formulation. This resolves the contradiction by providing enhanced therapeutic effectiveness through synergistic action while maintaining treatment simplicity through single-product administration.
Solution Approach 2:
The invention uses co-micronized composite material comprising N-palmitoyl-ethanolamide and Rutin in specific ratios (1:4 to 4:1). This composite approach enhances therapeutic effectiveness by leveraging the complementary mechanisms of action of both ingredients while delivering them as a unified formulation, thus resolving the effectiveness-complexity contradiction.
2Reliability
If single-ingredient treatments are used, then treatment simplicity is maintained, but synergistic therapeutic effects are not achieved
Solution Approach 1:
The patent merges N-palmitoyl-ethanolamide and Rutin into a co-micronized composition where the ingredients work synergistically. This resolves the contradiction by achieving enhanced therapeutic effects through combination while maintaining formulation simplicity through co-micronization technology that creates a unified delivery system.
Solution Approach 2:
The invention optimizes the concentration parameters of the components, specifying N-palmitoyl-ethanolamide at 0.1-10 mg/kg and Rutin at 0.1-10 mg/kg in various ratios. This parameter optimization enables synergistic therapeutic effects while controlling composition complexity through defined concentration ranges.
3Reliability
If larger particle size compounds are used, then manufacturing ease is maintained, but bioavailability and absorption are reduced
Solution Approach 1:
The patent applies micronization to reduce particle size of both N-palmitoyl-ethanolamide and Rutin to the micrometer range. This parameter change in particle size dramatically improves bioavailability and absorption while the co-micronization process manages manufacturing complexity by treating both ingredients through the same size-reduction methodology.
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 composition demonstrates a synergistic effect in improving vascular reactivity and reducing oxidative stress, effectively treating conditions like atherosclerosis, vasculitic neuropathies, and neointimal hyperplasia, as shown in animal models, with potential for oral, buccal, parenteral, or transdermal administration.
Implementation Method 1
The composition demonstrates a synergistic effect in improving vascular reactivity and reducing oxidative stress
Implementation Method 2
improving vascular tone regulation
Data Source
AI summary
Described herein is a composition based on N-palmitoyl-ethanolamide and Rutin in co-micronized form. In particular, a composition includes a mixture of palmitoyl-ethanolamide (PEA) and Rutin in co-micronized form in which the PEA/Rutin ratio is between 10:1 and 1:1. Pharmaceutical formulations for the treatment of humans and animals are also described. The composition is useable for the treatment of diseases of arteries and arterioles.