Cranberry Extract Phospholipid Complex for Urinary Bioavailability
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Solution Overview
Problem
Current pharmaceutical and nutraceutical compositions containing American cranberry extracts for treating and preventing urinary tract infections face challenges due to variable efficacy, low active ingredient content, and unsuitable formulations that fail to promote absorption and achieve effective concentrations of active metabolites in the urine.
Innovation Solution
A composition comprising 20-50% American cranberry extract combined with 50-80% phospholipids, along with optional adjuvants, is developed to enhance bioavailability and ensure effective urinary concentrations of active metabolites, using a process involving solubilization and drying to create a stable solid form for oral administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If traditional American cranberry extract formulations are used, then the composition is simple and easy to manufacture, but the bioavailability is poor and effective urinary concentrations are not achieved
Solution Approach 1:
Phospholipids are introduced as intermediary substances that mediate between the American cranberry extract and the gastrointestinal tract. The phospholipids form complexes with the extract components, facilitating absorption across the intestinal membrane and enabling effective urinary concentrations to be achieved, thus resolving the bioavailability problem without requiring complex formulation systems
Solution Approach 2:
The invention creates a composite material system combining American cranberry extract with phospholipids. This composite formulation leverages the complementary properties of both components: the antibacterial activity of the extract and the membrane-permeabilizing, absorption-enhancing properties of phospholipids, achieving improved bioavailability through a relatively simple composite structure
2Reliability
If higher doses of American cranberry extract are used to ensure effective urinary concentrations, then the preventive effect is improved, but the cost and potential side effects increase
Solution Approach 1:
The invention changes the pharmacokinetic parameters of American cranberry extract absorption by introducing phospholipids. This parameter change enables the same or lower doses of extract to achieve higher and more consistent urinary concentrations, thereby improving the preventive effect without requiring increased quantities of the extract, thus reducing cost and potential side effects
3Quantity of substance
If conventional extract formulations are used, then the manufacturing process is simple, but the active ingredient content is low and variable
Solution Approach 1:
Phospholipids serve as intermediary substances that form complexes with the active ingredients in the American cranberry extract. This intermediary complex formation protects the active ingredients from degradation during manufacturing and storage, maintaining consistent and higher active ingredient content without complicating the manufacturing process, as the phospholipids can be mixed with the extract using conventional techniques
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 achieves measurable and effective levels of active metabolites in the urine, providing a longer-lasting antibacterial action and improved preventive effects against urinary tract infections, even with reduced doses of American cranberry extract compared to traditional formulations.
Implementation Method 1
The invention relates to a composition, typically in solid form, comprising: a) a Vaccinium macrocarpon extract... b) at least one phospholipid... The compositions are characterised by high stability during transport and storage, and ease of incorporation in various dosage forms for the pharmaceutical, nutrition and cosmetic industries. It also states that the compositions are characterised by good solubility and wettability, which guarantee high bioavailability of the active plant ingredient.
Implementation Method 2
The American cranberry contains numerous organic substances, including proanthocyanidins (PACs), flavonols, polyphenols and hydroxycinnamic acids which, together with their active metabolites, possess both direct and indirect bactericidal activity. The latter is due to their ability to prevent adherence to the urothelial mucosa, thereby preventing the formation of biofilms by said pathogens.
Data Source
AI summary
The present invention relates to compositions comprising an American cranberry extract combined with phospholipids, and the use thereof in the prevention and treatment of urinary tract infections. The invention also relates to processes for the preparation of said compositions, and formulations for oral administration comprising said compositions.