Enteric-Coated Benzgalantamine Tablets for pH-Dependent Release
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing oral formulations of benzgalantamine suffer from gastrointestinal adverse effects due to premature cleavage in the acidic stomach environment, leading to reduced bioavailability and patient adherence.
Innovation Solution
A pharmaceutical composition in the form of an enteric-coated tablet, where the tablet core contains benzgalantamine or its salt, and an enteric coating configured to dissolve at pH 5.5 and above, ensuring controlled release in the small intestine and minimizing gastrointestinal adverse effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If oral formulations of benzgalantamine are administered, then the drug can be delivered to the brain for treating cognitive impairment, but premature cleavage in the acidic stomach environment causes gastrointestinal adverse effects and reduced bioavailability
Solution Approach 1:
An enteric coating layer is applied as an intermediary between the benzgalantamine tablet and the gastric environment. This coating acts as a protective mediator that prevents direct contact between the drug and acidic stomach conditions, thereby avoiding premature cleavage and gastrointestinal side effects while allowing the drug to reach the intestine intact for subsequent absorption and brain delivery
Solution Approach 2:
The invention changes the pH environment parameter by using an enteric coating that remains stable at low pH (stomach conditions) but dissolves at higher pH (intestine conditions). This parameter change protects the benzgalantamine from acidic degradation in the stomach and enables drug release in the more favorable intestinal environment for absorption
2Object-affected harmful factors
If the tablet is coated with enteric material to protect from stomach acid, then gastrointestinal adverse effects are reduced, but the coating must dissolve at specific pH to ensure drug release
Solution Approach 1:
The enteric coating utilizes pH-dependent solubility parameter changes to achieve protective function. The coating material is selected to be insoluble at gastric pH but soluble at intestinal pH, enabling automatic activation of drug release based on the physiological pH gradient without requiring complex mechanical or chemical triggering mechanisms
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 enteric-coated formulation achieves improved pharmacokinetic properties with reduced gastrointestinal adverse events, maintaining bioavailability comparable to immediate and extended-release reference formulations.
Implementation Method 1
an enteric coating, wherein said enteric coating is configured for dissolution at pH 5.5 and above
Data Source
AI summary
The invention relates to a pharmaceutical composition in the form of a tablet, said tablet comprising a tablet core, wherein said core comprises benzgalantamine (ALPHA-1062) or salt thereof, and an enteric coating, wherein said enteric coating is configured for dissolution at pH 5.5 and above. Further the invention relates to the pharmaceutical composition for use in the treatment of a brain disease associated with cognitive impairment and/or with a cholinergic deficit. The invention further relates to a method for preparing the pharmaceutical composition.