Oral Polypeptide Composition with Protease Inhibition for GI Stability
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Solution Overview
Problem
Polypeptide drugs have low bioavailability and require injection administration, which is associated with side effects and poor patient compliance due to fear of needles and harsh gastrointestinal environment limits oral absorption.
Innovation Solution
A polypeptide composition comprising a polypeptide, fish oil, a protease inhibitor, and an absorption enhancer, with specific ratios and synergistic components to enhance oral bioavailability and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If polypeptide drugs are administered by injection, then bioavailability is improved, but side effects such as infection and inflammation occur and patient compliance deteriorates
Solution Approach 1:
The patent uses a specially designed oral delivery system comprising protective coatings and absorption enhancers as intermediaries to facilitate polypeptide absorption through the gastrointestinal tract without direct contact with harsh digestive enzymes, thereby maintaining bioavailability while eliminating injection-related side effects
Solution Approach 2:
The patent modifies the physical and chemical parameters of the polypeptide formulation by adjusting pH, using protective polymers, and incorporating absorption enhancers to stabilize the polypeptide in the gastrointestinal environment, enabling oral administration with maintained efficacy
2Reliability
If polypeptide drugs are administered by injection, then bioavailability is improved, but patient compliance deteriorates due to fear of needles
Solution Approach 1:
The oral delivery system acts as an intermediary that bridges the gap between polypeptide stability requirements and gastrointestinal absorption needs, enabling non-invasive administration that patients can self-administer without needle fear while maintaining therapeutic efficacy
3Ease of operation
If polypeptide drugs are administered orally, then patient compliance is improved, but absorption is limited by the harsh gastrointestinal environment
Solution Approach 1:
The patent employs pH-modifying agents and protective polymers to create a favorable microenvironment for polypeptide stability in the gastrointestinal tract, protecting against enzymatic degradation and facilitating absorption while maintaining ease of oral administration
Solution Approach 2:
The patent uses composite formulations combining polypeptides with protective polymers, absorption enhancers, and pH-modifying agents to create a multifunctional delivery system that simultaneously protects the polypeptide from degradation and enhances its absorption through the gastrointestinal barrier
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 high stability, long shelf life, and improved bioavailability for oral administration of polypeptides, overcoming the limitations of injection and gastrointestinal barriers.
Implementation Method 1
the fish oil is present in an amount of 0.01 to 800 parts by weight
Implementation Method 2
the oral polypeptide composition comprises a polypeptide and a protease inhibitor
Implementation Method 3
the oral polypeptide composition comprises a polypeptide and an absorption enhancer
Implementation Method 4
the surfactant(s) is/are present in an amount of 1 to 800 parts by weight
Data Source
AI summary
An oral polypeptide composition comprising a polypeptide, fish oil, a protease inhibitor, at least one absorption enhancer, and at least one surfactant, and use thereof for treating a disease.