Enteric Capsule Coating for Oral Peptide Bioavailability
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Solution Overview
Problem
The oral bioavailability of peptides and proteins is limited due to poor absorbance from the gastrointestinal tract, necessitating injection for systemic exposure, and there is a desire for improved pharmacokinetic properties and higher doses of therapeutic agents.
Innovation Solution
An oral dosage form comprising a capsule coated with a first coating of polyvinyl alcohol and a second coating of methacrylic acid and ethyl acrylate copolymer dispersion, optionally with a third coating of talc, to enhance delivery of therapeutic agents like polypeptides.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If oral administration is used for peptide therapy, then patient convenience and dosing flexibility are improved, but bioavailability remains poor due to gastrointestinal absorption limitations
Solution Approach 1:
The patent introduces a permeation enhancer as an intermediary substance that facilitates peptide absorption across the gastrointestinal tract. This mediator enables oral delivery by improving membrane permeability, thus resolving the contradiction between oral administration convenience and poor bioavailability
Solution Approach 2:
The patent modifies the formulation parameters by incorporating specific excipients and coating materials (such as enteric coatings and permeation enhancers) to change the physical and chemical properties of the peptide delivery system, thereby improving absorption while maintaining oral administration
2Reliability
If injection is used for peptide delivery, then systemic exposure is achieved, but patient convenience and dosing flexibility are reduced
Solution Approach 1:
The permeation enhancer acts as an intermediary that enables oral delivery to achieve systemic exposure comparable to injection, thereby maintaining therapeutic effectiveness while improving patient convenience
Solution Approach 2:
The patent replaces the mechanical injection system with an oral formulation system that uses chemical permeation enhancers to achieve the same systemic exposure effect, eliminating the need for invasive administration
3Productivity
If higher doses of therapeutic agents are administered, then therapeutic efficacy is improved, but safety and tolerability concerns increase
Solution Approach 1:
The patent optimizes formulation parameters including coating composition, permeation enhancer concentration, and excipient ratios to improve the safety profile and tolerability at higher doses, allowing dose escalation without proportional increase in adverse effects
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 coating system improves the absorption of polypeptides, enabling higher doses and broader therapeutic applications, including treatments for conditions such as acromegaly and carcinoid syndrome, by providing controlled release and enhanced bioavailability.
Implementation Method 1
The oily suspension is filled into hard gelatin capsules which are then banded with gelatin and film-coated by an enteric coating system, enabling delivery of the capsule contents to the intestine
Implementation Method 2
Chiasma's proprietary technology, the Transient Permeability Enhancer (TPE®), enables oral delivery of peptides
Data Source
AI summary
The present invention relates generally to encapsulated pharmaceutical compositions enabling improved oral delivery and methods of using such compositions.