Oral Polypeptide Composition Using Fatty Acid Salts for GI Absorption
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Solution Overview
Problem
Existing drug delivery methods, particularly for oral administration, suffer from low bioavailability and inefficiency in crossing biological barriers, such as the gastrointestinal tract, leading to inadequate therapeutic effects for many therapeutic agents.
Innovation Solution
A pharmaceutical composition comprising a therapeutic agent and a medium chain fatty acid salt, formulated in a hydrophobic medium, is produced by lyophilization and encapsulated in a pH-sensitive coating for oral delivery, enhancing absorption by unsealing tight junctions between GI epithelial cells.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If oral delivery is used to avoid invasive administration, then patient convenience and compliance are improved, but bioavailability remains very low
Solution Approach 1:
The patent introduces medium chain fatty acid salts as intermediary substances that facilitate the transport of therapeutic agents across the gastrointestinal barrier. These salts act as carriers or enhancers that enable the therapeutic agent to cross the intestinal wall, thereby improving bioavailability while maintaining oral administration convenience.
2Ease of operation
If conventional oral formulations are used, then administration is non-invasive, but absorption across the gastrointestinal barrier is inefficient
Solution Approach 1:
The patent modifies the chemical and physical parameters of the formulation by incorporating medium chain fatty acid salts, which change the permeability characteristics of the gastrointestinal barrier. This parameter change enables more efficient absorption of therapeutic agents while maintaining non-invasive oral administration.
3Ease of operation
If therapeutic agents with low bioavailability are administered orally, then oral delivery is achieved, but therapeutic goals are not met
Solution Approach 1:
The medium chain fatty acid salts serve as intermediary substances that enable therapeutic agents with inherently low bioavailability to achieve sufficient absorption when administered orally. The salts facilitate the crossing of the intestinal barrier, making the therapeutic agent effective while maintaining oral delivery simplicity.
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 improved bioavailability, with absorption levels up to 30% or more, compared to parenteral administration, facilitating therapeutic levels for conditions like acromegaly, abnormal GI motility, and diarrhea.
Implementation Method 1
a composition described herein may facilitate absorption by permeating the GI wall/barrier primarily via unsealing of the tight junctions between GI epithelial cells
Implementation Method 2
drying (e.g. by lyophilization) the water soluble composition to obtain a solid powder
Data Source
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AI summary
The invention relates to a composition comprising a suspension which comprises an admixture of a hydrophobic medium and a solid form wherein the solid form comprises a therapeutically effective amount of a therapeutic agent and at least one salt of a medium chain fatty acid, and wherein the medium chain fatty acid salt is present in the composition at an amount of 10% or more by weight, wherein the therapeutic agent is a polypeptide. The invention also relates to compositions for use in treating or preventing diseases by administration of the compositions to affected subj ects.