Enteric-Coated Omeprazole Microgranules in Triglyceride Suspension
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Solution Overview
Problem
Current formulations of omeprazole for oral administration are unstable in acidic environments, leading to degradation, and existing liquid suspensions have short shelf lives and are inconvenient for patients, making it difficult to provide a stable and palatable dosage form.
Innovation Solution
A stable suspension formulation of omeprazole using enteric-coated microgranules (400-1200 microns) suspended in a triglyceride ester with a disintegrant, sealing, and control release layers, including a preservative like potassium sorbate, and optional sweeteners and flavorings, to maintain stability and palatability for at least one month.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If omeprazole is provided in liquid suspension form for oral administration, then ease of administration is improved, but stability in acidic environment deteriorates leading to degradation
Solution Approach 1:
The omeprazole is segmented into microgranules (400-1200 microns) with enteric coating layers, separating the drug from direct contact with stomach acid until the coating dissolves in the intestine, thus maintaining stability while enabling liquid suspension administration
Solution Approach 2:
An enteric coating layer acts as an intermediary barrier between the omeprazole and the acidic stomach environment, protecting the drug from degradation while allowing controlled release in the less acidic intestinal environment
2Ease of operation
If existing liquid suspension formulations are used, then ease of administration is improved, but shelf life deteriorates to less than one month
Solution Approach 1:
The enteric coating is applied in advance to the microgranules before suspension formulation, providing pre-established protection that enables long-term stability (at least one month shelf life) while maintaining the convenience of liquid suspension administration
3Reliability
If enteric coating is applied to protect omeprazole from acid, then stability is improved, but device complexity increases
Solution Approach 1:
A thin enteric coating film is applied to the microgranules, providing effective acid protection while maintaining a simple overall formulation structure that does not significantly increase manufacturing complexity
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 provides a stable and palatable liquid suspension of omeprazole that maintains its active content for extended periods, allowing for convenient and effective administration of the drug, suitable for treating gastric-related disorders with improved patient compliance.
Implementation Method 1
An enteric coating is a polymer coating barrier which is applied to the granules or capsules to protect the omeprazole from the acid in the stomach
Implementation Method 2
the coating includes one or more layers selected from a disintegrant layer, a sealing layer and a control release layer
Data Source
AI summary
A suspension comprising: microgranules having bead sizes in the range of 100 to 1200 microns of a benzimidazole derivative; said derivative being suspended in a triglyceride ester of a fatty acid; said suspension being stable for a least 1 month.