Enteric Granules with Intermediate Coating for Benzimidazole Stability
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Solution Overview
Problem
Benzimidazole compounds used as antiulcer agents are unstable, especially in acidic environments and when formulated into preparations, leading to reduced stability and difficulty in administration, particularly for elderly and pediatric patients due to their acidic instability and interaction with other components.
Innovation Solution
Development of enteric granules with a high content of benzimidazole compounds and a basic inorganic salt, such as magnesium or calcium, with an intermediate coating layer to prevent direct contact with the enteric coating, and an average particle size of 600 μm or more, enhancing stability and ease of administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If benzimidazole compounds are formulated into preparations with stabilizing agents, then stability is improved, but the content of the active ingredient is reduced due to interactions with other components
Solution Approach 1:
The preparation is segmented into distinct functional layers: a core layer containing the benzimidazole compound and basic inorganic salt for stabilization, an intermediate coating layer providing additional protection, and an enteric coating layer for targeted release. This segmentation allows each layer to perform its specific function without interfering with the active ingredient content in the core layer.
Solution Approach 2:
The intermediate coating layer acts as an intermediary between the core layer containing the active ingredient and the enteric coating layer. This intermediate layer prevents direct contact and potential interactions between the stabilizing agents in the core and the enteric coating materials, while still allowing the core to maintain stability.
2Reliability
If enteric coating is applied to benzimidazole compounds, then acid instability is resolved, but capsule size increases making administration difficult for elderly and pediatric patients
Solution Approach 1:
The invention optimizes the particle size parameters of the granules to be within a specific range that allows them to be filled into smaller capsules (No. 3 or smaller). The granule size, coating thickness, and density are adjusted to achieve the right balance between maintaining enteric coating integrity and fitting into administration-friendly capsule sizes.
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 granules maintain stability at high concentrations, allowing for a higher content of the active ingredient, reducing the size of capsules, and improving patient compliance by facilitating easier swallowing, especially for elderly and pediatric patients.
Implementation Method 1
an intermediate coating layer which is formed on the principal ingredient layer; and an enteric coating layer which is formed on the intermediate coating layer
Data Source
AI summary
It is intended to provide preparations such as capsules containing an acid-unstable medicament (in particular, a benzimidazole compound having an antiulcer effect, etc.) at a high concentration which are prepared by using about 12% by weight or more (based on the total granules) of the acid-unstable chemical and blending a basic inorganic salt therewith to give granules of about 600 μm or more in the average particle size.