Phospholipid Composition for Topical Drug Permeation and Stability
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing pharmaceutical compositions with phospholipids for topical application lack clarity on oil concentration and its impact on active ingredient permeation and storage stability, leading to reduced effectiveness and stability issues.
Innovation Solution
A pharmaceutical composition with a phospholipid mixture containing at least 60% phosphatidylcholine by weight and an oil concentration between 4.8% and 2% by weight, which enhances the permeation of active ingredients through the cell membrane and improves storage stability by limiting oxidation-sensitive components.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If the oil concentration in phospholipid is increased to enhance permeation, then the penetration capacity improves, but the storage stability deteriorates due to oxidation
Solution Approach 1:
The patent optimizes the oil concentration parameter within a specific range (0.1-10% by weight) to achieve the best balance between penetration capacity and storage stability. This parameter optimization allows the composition to maintain effective permeation enhancement while minimizing oxidation-related degradation during storage.
Solution Approach 2:
The patent uses a composite phospholipid system containing multiple components (phosphatidylcholine, phosphatidylethanolamine, phosphatidic acid, and controlled oil content) to achieve synergistic effects. This composite structure provides both the permeation enhancement needed for effective drug delivery and the structural stability required for long-term storage.
2Productivity
If oxidation-sensitive components are present in phospholipid, then permeation enhancement is achieved, but odor development and decomposition increase during storage
Solution Approach 1:
The patent controls the concentration of oxidation-sensitive oil components within a specific range (0.1-10% by weight) to maintain permeation enhancement while minimizing oxidation products that cause odor and decomposition. This precise parameter control allows the composition to remain effective without developing unpleasant characteristics during storage.
3Ease of manufacture
If phospholipid composition is not precisely controlled, then manufacturing is easier, but the effectiveness and stability of active ingredient delivery deteriorates
Solution Approach 1:
The patent defines specific parameter ranges for phospholipid composition (phosphatidylcholine, phosphatidylethanolamine, phosphatidic acid, and oil content) that balance manufacturing feasibility with product performance. These controlled parameters ensure consistent effectiveness and stability across production batches while remaining practical to manufacture.
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 accelerated penetration and permeation of active ingredients, maintaining higher concentrations and stability, reducing oxidation-related degradation and odor development, thus ensuring effective topical application and extended shelf life.
Implementation Method 1
improves the transport of the active ingredient through the cell membrane when the composition according to the invention is applied topically
Implementation Method 2
such oils usually present in the phospholipids often have a high concentration of unsaturated double bonds have a relatively high sensitivity to oxidation when stored in an air atmosphere
Data Source
Figure 1
Figure 2
Figure 3
AI summary
A pharmaceutical composition for use in humans and animals is described, comprising at least one systemically and/or locally acting, topically applicable active ingredient and at least one phospholipid that improves the transport of the active ingredient across cell membranes, containing phosphatidylcholine at a concentration of at least 60% by weight, based on the phospholipid. The composition has a liquid consistency suitable for application as droplets or a foam, and contains a phospholipid that, in addition to at least 60% by weight of phosphatidylcholine, also contains oil at a concentration of no more than 7.5% by weight.