Fermented Red Rice Composition for Hyperlipidaemia Bioavailability
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Solution Overview
Problem
Current compositions for treating hyperlipidaemia face challenges due to low bioavailability and bioaccessibility of active ingredients like Monacolin K from fermented red rice extract and Coenzyme Q10, exacerbated by adverse effects and regulatory concerns, as well as hindered delivery by co-administered substances in the gut.
Innovation Solution
A solid composition combining fermented red rice extract, Coenzyme Q10, tocotrienols, and tocopherols with a mono- or polyunsaturated fatty acid and basic L-arginine, forming an extemporaneous emulsion to enhance enteric bioaccessibility, using a specific ratio of solid and liquid fractions and excipients to improve absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If fermented red rice extract is used to treat hyperlipidaemia, then cholesterol-lowering action is achieved, but bioavailability is limited due to poor solubility and interference from co-administered substances
Solution Approach 1:
The patent creates a composite delivery system combining fermented red rice extract with solubilizing agents (polysorbate 80, lecithin), co-factors (tocotrienols, tocopherols, CoQ10), and excipients in a standardized formulation. This composite approach enhances the bioavailability of monacolin K while maintaining therapeutic effectiveness, directly addressing the solubility and absorption limitations of pure RYR extract.
2Object-affected harmful factors
If dosage of Monacolin K is reduced to avoid adverse effects, then safety is improved, but therapeutic effectiveness decreases
Solution Approach 1:
The patent changes the physical and chemical parameters of monacolin K delivery through standardization (defining monacolin K content as 1.5-3.0% of total weight) and solubilization (using polysorbate 80 and lecithin). These parameter changes allow for reduced dosing while maintaining therapeutic effectiveness by improving absorption efficiency, thus reducing adverse effects without sacrificing efficacy.
Solution Approach 2:
The patent introduces solubilizing agents (polysorbate 80, lecithin) and co-factors (tocotrienols, tocopherols, CoQ10) as intermediaries that facilitate the absorption and utilization of monacolin K. These intermediaries enhance bioavailability, allowing lower doses to achieve the same therapeutic effect, thereby reducing adverse effects while maintaining effectiveness.
3Reliability
If CoQ10 is administered to counteract statin effects, then mitochondrial function is protected, but bioavailability remains low due to hydrophobicity
Solution Approach 1:
The patent formulates CoQ10 in a composite system with tocotrienols, tocopherols, and solubilizing agents (polysorbate 80, lecithin). This composite formulation addresses the hydrophobicity of CoQ10 by combining it with lipophilic vitamins and surfactants, enhancing its solubility and bioavailability while maintaining its mitochondrial protective function.
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 significantly increases the bioavailability and bioaccessibility of active ingredients, promoting effective gastro-enteric dispersion and dissolution, thereby enhancing the therapeutic efficacy for hyperlipidaemia treatment.
Implementation Method 1
forming an extemporaneous emulsion to enhance enteric bioaccessibility
Implementation Method 2
Lovastatin is a lactone which is activated into its active form β-hydroxy-carboxylic (pro-drug) following hydrolysis by specific hydrolases (serum and tissue lactases)
Data Source
Figure 1
Figure 2
AI summary
Solid composition comprising A) a solid fraction containing: a fermented red rice extract having a total monacolin titre comprised between 1% and 5% by weight of the total weight of the fermented red rice extract, coenzyme Q10, basic L-arginine, a bulking agent selected from the group consisting of at least one polyol, maltodextrins, polydextrose, fructooligosaccharides, polysaccharides or mixtures of the foregoing; B) a liquid fraction which contains: at least one mono- or polyunsaturated fatty acid having free carboxylic function, a plant extract containing tocotrienols and tocopherols, having a tocotrienol and tocopherol titre comprised between 50% and 75% by weight of the total weight of the plant extract.