Enteric Coated Dosage Forms for Intestinal Enterokine Release
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Solution Overview
Problem
Existing pharmaceutical compositions face challenges in achieving controlled and reproducible enterokine release by enteroendocrine cells, particularly in conditions like type 2 diabetes mellitus and obesity, due to variability in gastric emptying mechanisms and inefficient delivery to specific intestinal regions.
Innovation Solution
A pharmaceutical composition comprising multiple dosage forms with enteric coatings and gelling agents, designed to bypass gastric emptying mechanisms, ensuring targeted release of enterokines like GLP-1 and PYY in the small intestine, particularly in the jejunum, using specific size and surface area optimization and inclusion of gelling agents to enhance swallowability and safety.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional pharmaceutical compositions are used, then delivery to intestine is achieved, but variability in gastric emptying mechanisms causes inconsistent enterokine release
Solution Approach 1:
The composition is divided into multiple dosage forms (tablets, capsules, granules) with different sizes, allowing independent control of release timing and location. This segmentation enables the system to overcome variability in gastric emptying by ensuring at least some dosage forms reach the intestine reliably, providing consistent enterokine release despite individual differences in gastric motility.
Solution Approach 2:
The patent utilizes pH-sensitive enteric coatings that change their properties based on pH conditions. The coating dissolves or degrades at specific pH levels in the small intestine, ensuring release of the active compound at the correct location regardless of gastric emptying rate. This parameter change mechanism guarantees reliable enterokine release timing independent of gastric variability.
2Speed
If dosage forms are made small for direct intestinal entry, then independent of gastric emptying delivery is achieved, but swallowability and safety are compromised
Solution Approach 1:
The composition includes multiple dosage forms with varying sizes, allowing patients to select or receive forms that are easy to swallow while still achieving the desired small-dosage-form effect for direct intestinal entry. The segmentation enables optimization of both swallowability and intestinal delivery independence from gastric emptying.
Solution Approach 2:
The enteric coating acts as an intermediary layer that protects the small dosage forms during passage through the stomach and facilitates their release in the small intestine. This coating enables small dosage forms to be swallowed easily while still achieving rapid intestinal entry and targeted release, resolving the contradiction between size and swallowability.
3Manufacturing precision
If enteric coating is used for targeted release, then delivery to specific intestinal region is improved, but manufacturing complexity increases
Solution Approach 1:
The patent employs pH-sensitive enteric coatings that automatically respond to pH changes in the gastrointestinal tract. This parameter-based response mechanism provides precise control over release location without requiring complex manufacturing processes, as the coating self-regulates its dissolution based on the natural pH gradient of the GI tract.
Solution Approach 2:
The enteric coating provides local quality differentiation by being pH-sensitive and dissolving at specific locations in the small intestine. This local response mechanism enables targeted release precision while maintaining relatively simple formulation, as the coating's properties are inherently tuned to the specific pH environment of the target intestinal region.
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 provides consistent and reproducible enterokine release with low variability, improved patient compliance, especially in pediatric and elderly populations, by ensuring safe and easy ingestion and targeted delivery to enteroendocrine cells, enhancing therapeutic efficacy.
Implementation Method 1
the coating comprises a pH sensitive polymer being selected such that the coating substantially dissolves and/or is substantially degraded in the jejunum of a subject
Implementation Method 2
the composition further comprises one or more gelling agents
Data Source
Figure 1
AI summary
The present invention relates to pharmaceutical compositions and pharmaceutical articles comprising such compositions wherein the compositions comprise multiple dosage forms each comprising a core and an enteric coating, wherein the core comprises at least one compound stimulating enteroendocrine cells to release at least one enterokine, wherein the size of the dosage forms, with respect to the largest dimension of the dosage forms, provides for entry of the dosage forms into the intestine of a subject independent of gastric emptying mechanisms, and wherein the composition further comprises one or more gelling agents. The invention also relates to the treatment and/or prevention of conditions amenable to stimulation of enterokine release by enteroendocrine cells.