N-acetylcysteine Controlled-Release Granules for Vascular Inflammation
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Solution Overview
Problem
Current therapies for reducing C-reactive protein (CRP) levels, a key marker for atherosclerosis, are limited in effectiveness and associated with undesirable side effects, and there is a need for a sustained delivery method of N-acetylcysteine (NAC) to manage vascular inflammation and atherosclerosis.
Innovation Solution
A controlled-release composition of N-acetylcysteine, comprising both immediate and sustained release components, designed to provide a therapeutically effective plasma concentration over a prolonged period, utilizing a combination of matrix, osmotic, and multiparticulate delivery systems to enhance absorption and bioavailability in the gastrointestinal tract.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current therapies are used to reduce CRP levels, then CRP reduction is achieved, but undesirable side effects occur and effectiveness is limited
Solution Approach 1:
The patent changes the delivery parameters of NAC by implementing controlled-release mechanisms that maintain steady plasma concentrations over extended periods (12-24 hours), avoiding the peaks and troughs of conventional dosing. This parameter change in delivery kinetics improves therapeutic effectiveness while reducing side effects associated with fluctuating drug levels
Solution Approach 2:
The patent uses controlled-release formulations as an intermediary system that mediates between the administered NAC and the body's metabolic processes. This intermediary delivery system ensures gradual release and absorption, improving reliability of CRP reduction while minimizing harmful effects from rapid concentration changes
2Duration of action of moving object
If conventional NAC administration is used, then immediate availability is achieved, but plasma concentration is not maintained over prolonged period
Solution Approach 1:
The patent segments the NAC dosage into controlled-release formulations that release the drug gradually over time. This segmentation of the dosing strategy extends the duration of therapeutic plasma concentration from hours to 12-24 hours, reducing the frequency of administration required while maintaining continuous therapeutic effect
Solution Approach 2:
The patent implements preliminary action through controlled-release formulations that are designed to release NAC over an extended period before complete elimination. This preliminary sustained release maintains plasma concentrations throughout the dosing interval, eliminating the need for frequent re-administration and extending the effective duration of action
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 controlled-release composition effectively maintains therapeutic levels of N-acetylcysteine, reducing vascular inflammation and CRP levels, thereby addressing atherosclerosis and related inflammatory conditions with improved efficacy and reduced side effects.
Implementation Method 1
utilizing a combination of matrix, osmotic, and multiparticulate delivery systems to enhance absorption and bioavailability in the gastrointestinal tract
Implementation Method 2
A controlled-release composition of N-acetylcysteine, comprising both immediate and sustained release components, designed to provide a therapeutically effective plasma concentration over a prolonged period
Implementation Method 3
N-acetylcysteine (NAC) is an antioxidant and a thiol donor
Data Source
AI summary
The present invention provides a controlled-release composition which provides a therapeutically effective plasma concentration of N-acetylcysteine over prolonged period of time. The present invention also includes the use of the controlled-release composition, either alone or in combination with at least one additional active agent, for reduction of vascular inflammation marker and treatment of diseases, conditions, and/or symptoms associated with systemic and/or vascular inflammation in a patient. Furthermore, the present invention provides a process of making granules comprising N-acetylcysteine, or a salt, solvate, prodrug, and/or analog thereof.