Proton Pump Inhibitor Formulation Without Enteric Coating
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Solution Overview
Problem
Proton pump inhibitors, such as omeprazole and esomeprazole, are unstable in acidic environments, leading to rapid decomposition in the stomach, which delays their efficacy and requires excessive enteric coatings that can be cumbersome and prone to loss, necessitating a formulation that enhances stability and rapid onset without excessive additives.
Innovation Solution
A pharmaceutical composition combining a proton pump inhibitor with an antacid like magnesium hydroxide or magnesium oxide, eliminating the need for an enteric coating by neutralizing gastric acid and ensuring rapid absorption and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If an enteric coating layer is applied to prevent decomposition of proton pump inhibitors in gastric acid, then the stability of the drug is improved, but the onset time of drug efficacy is delayed and the device complexity increases
Solution Approach 1:
The invention removes the enteric coating layer from the formulation, extracting the problematic protective barrier that caused delayed onset. Instead of coating the drug to protect it from acid, the patent uses a different approach that allows immediate drug release while preventing decomposition through alternative mechanisms.
Solution Approach 2:
The invention introduces an intermediary substance (such as saponin or other surfactants) that mediates between the proton pump inhibitor and gastric acid environment. This intermediary protects the drug from acid decomposition without forming a physical barrier like enteric coating, allowing rapid drug release and immediate efficacy.
2Stability of the object's composition
If an enteric coating layer is applied to protect proton pump inhibitors from gastric acid, then the stability is improved, but the device complexity and amount of additives increase
Solution Approach 1:
The invention eliminates the enteric coating layer and associated complex formulation requirements, simplifying the overall drug delivery system while maintaining stability through alternative protective mechanisms.
Solution Approach 2:
The invention changes the formulation parameters by incorporating specific additives (surfactants, dispersants) that alter the chemical environment to protect the proton pump inhibitor from acid degradation, replacing the need for complex physical barriers.
3Stability of the object's composition
If enteric polymer is used to coat the drug, then the stability in acidic environment is improved, but the amount of additive required increases and manufacturing cost increases
Solution Approach 1:
The invention changes the approach from using large quantities of enteric polymer to using small amounts of functional additives that modify the chemical environment. These additives (surfactants, dispersants) are used in much smaller quantities while achieving similar or better protective effects.
Solution Approach 2:
The invention alters the chemical parameters of the formulation by introducing substances that change the local pH or chemical reactivity around the drug molecule, providing protection without requiring excessive amounts of protective material.
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 improves the stability and rapid absorption of proton pump inhibitors, achieving equivalent blood levels to enteric formulations while minimizing additives and side effects, with a reduced tablet weight for enhanced patient convenience.
Implementation Method 1
an antacid selected from magnesium hydroxide, magnesium oxide, and a mixture thereof... the antacid neutralizes the gastric acid and prevents decomposition of the proton pump inhibitors
Data Source
AI summary
One aspect provides a pharmaceutical composition and a pharmaceutical combination formulation contains the same, the pharmaceutical composition containing as active ingredients: a proton pump inhibitor or a pharmaceutically acceptable salt thereof; and an antacid selected from magnesium hydroxide, magnesium oxide, or a mixture thereof.