Enteric-Coated Oral Polypeptide Delivery for Intestinal Targeting
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Solution Overview
Problem
Current treatments for inflammatory bowel disease using pharmaceutically active binding polypeptides, such as anti-TNF-alpha antibodies, involve systemic administration with significant side effects, high costs, and accessibility issues due to parenteral routes and systemic exposure.
Innovation Solution
Development of solid pharmaceutical compositions with a compressed core coated with a pH-sensitive enteric coating for oral administration, providing delayed and sustained release of pharmaceutically active binding polypeptides directly to the intestinal tract, reducing systemic exposure and immunogenicity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If parenteral administration of anti-TNF-alpha antibodies is used, then therapeutic efficacy is achieved, but systemic side effects and immunogenicity increase
Solution Approach 1:
The invention extracts the therapeutic action from systemic circulation and localizes it to the intestinal tract through enteric-coated oral formulations. The active polypeptide is released specifically in the intestine, separating the therapeutic effect from systemic exposure and thereby reducing side effects while maintaining efficacy.
Solution Approach 2:
The enteric coating acts as an intermediary that protects the polypeptide from degradation in the upper GI tract and controls its release location. This mediator enables targeted delivery to the intestine, achieving local therapeutic effect without requiring systemic administration.
2Reliability
If parenteral administration of anti-TNF-alpha antibodies is used, then therapeutic efficacy is achieved, but treatment cost increases
Solution Approach 1:
The invention employs oral formulations with enteric coatings that are designed for single-use disposal after delivering their therapeutic payload. This approach replaces expensive, reusable parenteral administration systems with affordable, disposable oral dosage forms, significantly reducing treatment costs.
3Ease of manufacture
If oral administration is used, then cost and accessibility are improved, but release profile control becomes more difficult
Solution Approach 1:
The invention controls the release profile by changing the pH parameter - the enteric coating remains intact in acidic stomach environment and dissolves at higher pH in the intestine. This parameter-based control mechanism simplifies the formulation while achieving precise spatial and temporal release control.
4Object-affected harmful factors
If oral administration is used, then systemic exposure is reduced, but ensuring sustained release to target region becomes more challenging
Solution Approach 1:
The enteric coating is applied in advance to protect the polypeptide during transit through the upper GI tract and to pre-position the drug for sustained release in the intestine. This preliminary protective action ensures both reduced systemic exposure and sustained local availability of the therapeutic agent.
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
Achieves targeted and sustained delivery of polypeptides to the intestinal tract, reducing side effects, costs, and systemic exposure, while maintaining therapeutic efficacy and improving thermal stability.
Implementation Method 1
coated with a pH sensitive enteric coating
Data Source
AI summary
There is provided a solid pharmaceutical composition for delivering by oral administration a pharmaceutically active binding polypeptide to a region of the intestinal tract comprising a compressed core, wherein the compressed core comprises a pharmaceutically active binding polypeptide and wherein the compressed core is coated with a pH sensitive enteric coating.