Coated Oral Peptide Tablet Structure for Stable Gastric Absorption
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Solution Overview
Problem
Existing oral peptide drugs face challenges such as large molecular weight, poor absorption through gastrointestinal cells, destruction by pepsin in the stomach, and unstable plasma drug concentration leading to side effects in patients requiring long-term treatment.
Innovation Solution
A tablet formulation comprising a tablet body mixed with a first penetration accelerator and coated with a layer containing a second penetration accelerator and peptide, designed to settle quickly at the stomach bottom, attach to the stomach wall, and alter local pH to enhance peptide absorption.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If the peptide is mixed evenly with excipient to form a tablet, then the peptide can be absorbed by the human body, but the absorption time is short and the medicinal effects cannot continue
Solution Approach 1:
The tablet is divided into two distinct parts: a tablet body containing excipient and penetration accelerator, and a coating layer containing peptide and penetration accelerator. This segmentation allows the tablet body to provide sustained release while the coating layer ensures rapid absorption, resolving the contradiction between absorption stability and duration.
Solution Approach 2:
Penetration accelerator is used as an intermediary substance in both the tablet body and coating layer. It facilitates the peptide's penetration through the gastrointestinal tract and cell membranes, extending the absorption duration while maintaining stability throughout the gastrointestinal environment.
2Reliability
If the peptide is mixed evenly with excipient in a tablet, then the peptide can be absorbed, but the plasma drug concentration fluctuates greatly causing side effects
Solution Approach 1:
The coating layer provides a localized high-concentration peptide region that releases steadily, while the tablet body provides a sustained release matrix. This local quality differentiation ensures smooth plasma concentration curves, reducing fluctuations and side effects while maintaining absorption reliability.
3Reliability
If the peptide is taken orally in tablet form, then it can be absorbed by the human body, but the peptide is easily damaged by pepsin in the stomach
Solution Approach 1:
Penetration accelerator serves as a protective intermediary that shields the peptide from pepsin degradation in the stomach while still allowing the peptide to be absorbed. The accelerator facilitates peptide transport through the gastrointestinal tract without exposing the peptide to harmful enzymatic breakdown.
Solution Approach 2:
The coating layer acts as a protective thin film around the peptide, shielding it from pepsin in the stomach. This flexible coating allows the peptide to remain intact during gastric transit while enabling absorption at the intestinal level.
4Quantity of substance
If the peptide has large molecular weight, then it can be effective, but it is not easily absorbed by human body through gastrointestinal cells
Solution Approach 1:
Penetration accelerator acts as a molecular bridge or intermediary that facilitates the transport of large molecular weight peptides through the gastrointestinal cell membrane. The accelerator interacts with both the peptide and the cell membrane, enabling effective absorption despite the peptide's large size.
Solution Approach 2:
The penetration accelerator changes the physical or chemical parameters of the peptide-membrane interaction, such as charge, hydrophobicity, or molecular size, to enable effective absorption of large molecular weight peptides through the gastrointestinal tract.
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 formulation enables stable peptide absorption, reducing gastric enzyme destruction and fluctuations in plasma drug concentration, thereby minimizing side effects and maintaining effective medicinal action.
Implementation Method 1
enabling the tablet body containing the peptide to quickly settle to a bottom of a stomach
Implementation Method 2
to quickly attach to the bottom of the stomach flatly, the peptide is attached to a stomach wall
Implementation Method 3
Finally, a pH value of local areas in the stomach can be changed
Implementation Method 4
a permeability of cells can be increased, thereby enabling the peptide to be stably absorbed through the stomach
Data Source
AI summary
The invention is an oral peptide drug structure mainly comprising: a tablet body and a coating layer covering an outer layer of the tablet body, the tablet body is made of a first excipient mixing with a first penetration accelerator, and the coating layer is made of a second penetration accelerator mixing with a peptide. Through the tablet body design of coating the excipient with the peptide, the oral peptide can be stably absorbed.