Stable MCT Emulsion for High Drug Loading
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Solution Overview
Problem
There is a challenge in developing a ready-to-use, preservative-free liquid pharmaceutical composition of medium chain triglycerides (MCTs) that maintains long-term stability for pharmaceutical use, as existing formulations often face issues with physico-chemical and microbiological stability.
Innovation Solution
A liquid pharmaceutical composition comprising at least 30% caprylic triglyceride and one or more emulsion forming excipients such as lecithin, Polyoxyl 40 castor oil, caprylate esters, and glycerol, which form a stable emulsion with a mean particle diameter of less than 0.5 μm for at least one month at ambient conditions, ensuring stability and bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If MCTs are formulated as liquid dosage form at room temperature, then ease of operation and bioavailability are improved, but physico-chemical stability deteriorates
Solution Approach 1:
Emulsion-forming excipients act as intermediaries between the MCT oil phase and aqueous environment, creating stable emulsion structures that prevent phase separation and maintain physico-chemical stability while preserving the liquid dosage form characteristics
Solution Approach 2:
The formulation combines MCTs with emulsion-forming excipients to create a composite emulsion system that integrates the benefits of liquid dosage form with enhanced stability properties, achieving both ease of operation and improved physico-chemical stability
2Ease of operation
If MCTs are formulated as liquid dosage form without preservatives, then ease of operation is improved, but microbiological stability deteriorates
Solution Approach 1:
The emulsion structure created by excipients serves as a protective barrier that limits microbial access to the MCT oil phase, providing microbiological stability without requiring preservatives and maintaining the preservative-free liquid dosage form advantage
3Quantity of substance
If high drug loading of MCTs is achieved, then quantity of substance is improved, but emulsion stability deteriorates
Solution Approach 1:
The formulation optimizes the concentration and type of emulsion-forming excipients to achieve the appropriate HLB balance, enabling high MCT drug loading (at least 30% by weight) while maintaining emulsion stability through adjusted excipient parameters
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 long-term stability and enhanced bioavailability of MCTs, allowing for effective treatment of diseases associated with reduced cognitive function by elevating ketone body concentrations, such as Alzheimer's disease and Age-Associated Memory Impairment.
Implementation Method 1
one or more emulsion forming excipients present at a concentration sufficient to form stable emulsion for at least one month under ambient conditions
Implementation Method 2
the one or more emulsion forming excipients are selected from the group consisting of lecithin, hydrogenated castor oils including Polyoxyl 40 castor oil, caprylate esters, sodium oleate, glycerol
Data Source
AI summary
This invention relates to high drug load compositions of medium chain triglycerides (MCT), and to methods for treatment with such compositions at amounts effective to elevate ketone body concentrations so as to treat conditions associated with reduced neuronal metabolism, for example Alzheimer's disease.