Phosphatidylcholine Solubilization for Lipophilic Agents
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Solution Overview
Problem
Current methods for solubilizing poorly water-soluble dietary supplements and pharmaceutically active agents are limited by high development costs, lengthy development times, and the need for costly equipment, as well as concerns over the use of solubilizers like polysorbates, which have adverse health effects and reduce the efficacy of preservatives.
Innovation Solution
A method involving the use of phosphatidylcholine, medium-chained triglycerides, lysophosphatidylcholine, C2-C4 alcohols, and glyceryl stearate or saturated/unsaturated fatty acids to solubilize dietary supplements or active agents, with controlled heating to achieve a clear solubilisate that can be easily diluted for use, avoiding the need for polysorbates and reducing production costs.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If polysorbates are used as solubilizers, then solubility of poorly water-soluble agents is improved, but adverse health effects occur and preservative efficacy is reduced
Solution Approach 1:
The patent removes polysorbates from the solubilization system entirely and replaces them with phospholipids (lecithin) and medium-chain triglycerides. This extraction of the harmful substance while maintaining the solubilization function through alternative benign ingredients directly resolves the contradiction between achieving solubility and avoiding adverse health effects.
Solution Approach 2:
The patent employs food-grade phospholipids and medium-chain triglycerides that are naturally occurring, biodegradable, and generally recognized as safe. These replace the problematic polysorbates with substances that have no adverse health effects and do not interfere with preservative systems, thereby resolving the harmful factors while maintaining solubility enhancement.
2Quantity of substance
If standard solubilization techniques are used, then solubility is improved, but development costs and time increase
Solution Approach 1:
The patent uses phospholipids and medium-chain triglycerides that naturally form micellar structures capable of solubilizing lipophilic substances without requiring complex preliminary formulation steps. The solubilization mechanism is inherent to the ingredient system, eliminating lengthy development cycles associated with optimizing polysorbate-based formulations.
Solution Approach 2:
The patent changes the fundamental parameters of the solubilization system by using phospholipids with specific HLB values and medium-chain triglycerides that provide effective solubilization at straightforward concentration ratios. This simplifies the formulation parameters and reduces the iterative development time typically required to optimize solubilizer concentrations and combinations.
3Reliability
If micelle and liposome technologies are used, then bioavailability is improved, but production costs and equipment requirements increase
Solution Approach 1:
The patent employs phospholipids and medium-chain triglycerides that serve multiple functions simultaneously: they act as solubilizers, emulsifiers, and bioavailability enhancers in a single ingredient system. This multi-functionality eliminates the need for separate micelle or liposome preparation steps and associated costly equipment, while still achieving improved bioavailability through natural micellar formation.
Solution Approach 2:
The phospholipid and medium-chain triglyceride system self-assembles into micellar structures that solubilize lipophilic substances without requiring external processing equipment or complex manufacturing steps. The ingredients automatically form the solubilization structure upon contact with water, eliminating the need for specialized micelle or liposome production equipment and reducing manufacturing costs.
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
This method provides a cost-effective, easy-to-handle solution for solubilizing a broad range of poorly water-soluble substances, enhancing bioavailability and allowing for stable, clear solutions with extended shelf life, free from the drawbacks of existing technologies.
Implementation Method 1
A micelle-based solubilisate for solubilizing dietary supplements is known for ubiquinone Q10 (WO 03/007907 A1) or curcumin (WO2014/094921 A1). Therein an emulsifier with a HLB (hydrophilic-lipophilic balance) value of 9-16 or 13-18 is used, respectively.
Implementation Method 2
When given into an aqueous medium these molecules tend to associate by aggregating to spherical structures by orienting the polar head group towards the surrounding medium and the nonpolar chain towards the interior of the spheres.
Implementation Method 3
c) Cautiously heating the resulting mixture by continuously increasing the temperature with a continuous temperature increment of 0.5° C./min to 3° C./min over a period of 20 to 60 minutes; d) Stopping the temperature increase in a temperature range of 30° C. to 125° C. as soon as a clear solution is reached
Data Source
AI summary
The present invention relates to a method for solubilizing poorly water-soluble dietary supplements and pharmaceutically active agents, to the solubilisate produced by this method and respective uses as a dietary supplement or pharmaceutical dosage form. A phosphatidylcholine-based solubilization method is disclosed.