Solid Triglyceride Composition for Sustained GI Release
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Solution Overview
Problem
Current liquid dosage forms of triglycerides, such as triheptanoin, are difficult to administer, handle, and cause gastric upset, diarrhea, and other adverse effects due to rapid hydrolysis and low miscibility with food or drinks, limiting their therapeutic efficacy for fatty acid oxidation disorders and related diseases.
Innovation Solution
A solid composition comprising triglycerides with odd-numbered carbon fatty acids or phenylalkanoic/alkenoic acids adsorbed onto a solid substance, such as fumed silica, with a sustained release polymer, forming a stable powder that delays gastric release and improves absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If liquid dosage form of triglycerides is used, then therapeutic effect for fatty acid oxidation disorders can be achieved, but patient compliance deteriorates due to difficulty in administration and handling
Solution Approach 1:
The patent transforms the triglyceride formulation from liquid state to solid state by incorporating it into a solid carrier matrix. This phase change enables the medication to be administered as a solid dosage form (capsule, tablet, or bar) rather than liquid, significantly improving ease of handling, portability, and patient compliance while maintaining the therapeutic efficacy of the triglyceride active ingredient
Solution Approach 2:
The patent creates a composite formulation by combining the triglyceride active ingredient with a solid carrier material. This composite structure allows the liquid triglyceride to be encapsulated or embedded within a solid matrix, providing both the therapeutic benefits of the triglyceride and the handling advantages of a solid dosage form
2Reliability
If liquid oil formulation is used, then therapeutic dosage can be administered, but gastric upset and diarrhea occur due to rapid hydrolysis in the stomach
Solution Approach 1:
The patent applies preliminary protection by encapsulating the triglyceride active ingredient within a solid carrier matrix before administration. This pre-encapsulation prevents premature hydrolysis in the stomach by protecting the triglyceride from gastric enzymes until it reaches the small intestine, where absorption occurs, thereby preventing gastric upset and diarrhea
Solution Approach 2:
The solid carrier acts as an intermediary between the triglyceride active ingredient and the gastrointestinal environment. This carrier material protects the triglyceride from direct contact with gastric enzymes and acidic conditions, allowing controlled release in the appropriate location (small intestine) and preventing harmful effects in the stomach
3Reliability
If high dose of triglycerides is administered to achieve therapeutic effect, then treatment efficacy improves, but adverse effects increase due to dose-limiting toxicity
Solution Approach 1:
By pre-encapsulating the triglyceride in a solid carrier formulation, the patent enables administration of higher doses without the gastrointestinal adverse effects that normally limit dosing. The protective matrix allows the full therapeutic dose to reach the absorption site intact, improving treatment efficacy while avoiding dose-limiting toxicity
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 solid composition enhances patient compliance, reduces gastric stress and diarrhea, allows higher doses, and improves therapeutic efficacy by providing sustained release and improved absorption in the gastrointestinal tract.
Implementation Method 1
A solid composition comprising triglycerides with odd-numbered carbon fatty acids or phenylalkanoic/alkenoic acids adsorbed onto a solid substance
Data Source
AI summary
The present invention includes solid compositions of triglycerides with one or more fatty acids, such as triheptanoin and glycerol phenylbutyrate, and therapeutic use thereof. The solid compositions can be prepared by spray-drying or other processes.