Colon-Targeting Hydrogel Matrix with pH-Dependent Coating
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Solution Overview
Problem
Current pharmaceutical compositions for treating colon-related diseases, such as colitis or colon cancer, often result in premature release of active ingredients before reaching the colon, leading to increased doses and side effects, and the preparation process is complex due to the need for layered particles and hydrogel protection.
Innovation Solution
A pharmaceutical composition with a core matrix comprising a cross-linked hydrogel and high active ingredient loading (65-95 wt%), where the active ingredient is dispersed within the hydrogel, formed through a fluid bed granulation process, allowing for high drug loading and efficient colon targeting without a core-shell structure, and protected by a pH-dependent coating film for controlled release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If high dose of active ingredients is used to ensure enough amounts reach the colon, then the amount of active ingredient reaching the colon is sufficient, but side effects increase and active ingredient waste occurs
Solution Approach 1:
The patent applies preliminary action by pre-coating the active ingredient with a protective coating film before administration. This coating prevents premature release in the stomach and small intestine, ensuring the active ingredient reaches the colon intact. The coating is designed to dissolve or degrade specifically in the colon environment, releasing the active ingredient only at the target site.
Solution Approach 2:
The patent implements local quality by creating a pH-dependent coating system with different properties at different gastrointestinal locations. The coating remains intact in acidic stomach environment and neutral small intestine environment, but dissolves in the basic colon environment (pH 6.8-7.5). This localized property change ensures precise delivery to the colon while preventing side effects in other areas.
2Reliability
If layered particles with hydrogel protection are used to achieve colon targeting, then the active ingredient is protected from premature release, but the preparation process becomes very complicated
Solution Approach 1:
The patent merges the protective function and the colon-targeting function into a single integrated coating system. Instead of using separate layered particles and hydrogel particles that need to be mixed and coated multiple times, the invention uses one coating film applied directly to the active ingredient particles. This single coating provides both protection from premature release and pH-dependent colon targeting, eliminating the need for complex multi-step processes.
Solution Approach 2:
The coating film serves multiple functions simultaneously: it acts as a protective barrier against premature release, provides pH-dependent solubility for colon targeting, and eliminates the need for separate hydrogel protection layers. This multi-functional design simplifies the overall formulation and preparation process while maintaining reliable colon delivery.
3Reliability
If two particles (multi-layered drug particles and hydrogel particles) are mixed to achieve colon targeting, then the composition can reach the colon successfully, but it is difficult to prepare the compositions
Solution Approach 1:
The patent extracts the hydrogel protection layer from the formulation, eliminating the need to prepare and mix separate hydrogel particles. The protective and targeting functions are achieved through the pH-dependent coating film alone, which dissolves in the colon environment to release the active ingredient. This extraction of the hydrogel component dramatically simplifies the manufacturing process while maintaining colon delivery reliability.
4Reliability
If conventional core-shell structure with low drug loading is used, then the active ingredient is protected, but the drug loading is less than 40% and recycle rate is low
Solution Approach 1:
The patent changes the structural parameters of the formulation by transitioning from a core-shell structure with a protective coating to a matrix structure where the active ingredient is dispersed throughout the coating material. This parameter change allows significantly higher drug loading (65-95 wt%) because the active ingredient is distributed throughout the entire coating volume rather than being confined to a small core region. The pH-dependent solubility parameter is maintained to ensure protection and colon-targeting functionality.
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 effectively increases the recycling rate of active ingredients, achieves high drug loading, and ensures controlled release of the active ingredient in the colon, reducing side effects and improving treatment efficacy while simplifying the preparation process.
Implementation Method 1
a core matrix comprising: a cross-linked hydrogel and an active ingredient, wherein the active ingredient is dispersed in the cross-linked hydrogel
Implementation Method 2
a core matrix comprising: a cross-linked hydrogel and an active ingredient
Data Source
AI summary
A pharmaceutical composition for colon targeting, a method for treating a colon-related disease using the same and a preparation method thereof are disclosed. The pharmaceutical composition of the present disclosure comprises: a core matrix comprising a cross-linked hydrogel and an active ingredient, wherein the active ingredient is dispersed in the cross-linked hydrogel, and a content of the active ingredient is 65 wt % to 95 wt % based on a total weight of the core matrix.