Pharmaceutical Formulation Stability with 2-Mercaptobenzimidazole
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Solution Overview
Problem
Formulations containing an active pharmaceutical ingredient, ethyl cellulose, and a solvent often experience impurity generation during long-term storage, compromising stability.
Innovation Solution
Incorporating 2-mercaptobenzimidazole into the formulation with ethyl cellulose and a solvent, ensuring a minimum of 0.1 part by weight of solvent per part by weight of ethyl cellulose, to suppress impurity generation and enhance storage stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If a formulation comprises an active pharmaceutical ingredient, ethyl cellulose, and a solvent, then the formulation can be prepared with basic functional components, but impurities are generated during long-term storage
Solution Approach 1:
2-mercaptobenzimidazole acts as an intermediary substance that mediates between the formulation components and oxygen, preventing oxidation reactions. The compound serves as a sacrificial antioxidant that reacts with oxygen before it can oxidize the active pharmaceutical ingredient or other sensitive components, thereby maintaining formulation stability during storage.
Solution Approach 2:
The invention changes the chemical composition parameter of the formulation by introducing 2-mercaptobenzimidazole at specific concentrations (0.1-10% by weight). This parameter change transforms the formulation from one that is prone to oxidation into a stable system resistant to impurity generation during storage.
2Stability of the object's composition
If 2-mercaptobenzimidazole is added as an antioxidant, then storage stability is improved, but formulation complexity increases
Solution Approach 1:
2-mercaptobenzimidazole serves multiple functions simultaneously: it acts as an antioxidant to prevent oxidation, provides long-term storage stability, and maintains compatibility with various active pharmaceutical ingredients including nitrogen-containing compounds. This multi-functionality reduces the need for multiple separate additives, thereby limiting the increase in formulation 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 addition of 2-mercaptobenzimidazole effectively prevents impurity formation, maintaining formulation stability over extended storage periods.
Implementation Method 1
2-mercaptobenzimidazole has been known as an antioxidant or an oxidation inhibitor in pharmaceutical formulations
Data Source
AI summary
It is an object of the present invention to provide a formulation comprising ethyl cellulose, an active pharmaceutical ingredient, and a solvent, which is a stable formulation in which generation of impurities is suppressed even during the long-term storage. According to the present invention, provided is a formulation comprising (a) an active pharmaceutical ingredient, (b) ethyl cellulose, (c) 2-mercaptobenzimidazole, and (d) 0.1 part by weight or more of solvent with respect to 1 part by weight of the ethyl cellulose.