Sustained Release Magnesium Matrix Coating
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Solution Overview
Problem
Current sustained release magnesium compositions have low bioavailability due to rapid release kinetics in the small intestine, leading to reduced absorption and ineffective magnesium supplementation.
Innovation Solution
A composition comprising a matrix with hydroxypropyl methylcellulose, glyceryl behenate, lactose, and colloidal silica, coated with a non-gastro-resistant coating to slow down magnesium release in the stomach, ensuring continuous release throughout the gastrointestinal tract, optimizing absorption at the ileum.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If a gastro-resistant coating is used to delay magnesium release, then release timing is improved, but dissolution rate becomes too rapid in the small intestine reducing bioavailability
Solution Approach 1:
The patent changes the chemical composition parameters of the coating layer, using specific ratios of magnesium oxide (5-20 parts), calcium carbonate (5-20 parts), and cellulose derivatives (40-80 parts). This parameter optimization allows the coating to provide controlled release without being too rapid in the small intestine, thereby improving bioavailability while maintaining timing control.
Solution Approach 2:
The patent employs a composite coating material system combining magnesium oxide, calcium carbonate, and cellulose derivatives in specific proportions. This composite structure provides both the desired delay in release and controlled dissolution rates throughout the gastrointestinal tract, resolving the contradiction between timing and bioavailability.
2Reliability
If magnesium release is delayed to improve bioavailability, then absorption is enhanced, but release kinetics become too slow reducing effectiveness
Solution Approach 1:
The patent optimizes the composition parameters of the matrix core, specifically setting magnesium oxide at 90-110 parts, hydroxypropyl methylcellulose at 180-190 parts, glyceryl behenate at 19.8-22.2 parts, lactose at 10-12 parts, and colloidal silica at 10-12 parts. These parameter adjustments ensure that magnesium release is neither too rapid nor too slow, maintaining optimal bioavailability and effectiveness.
Solution Approach 2:
The patent uses a composite matrix material system combining magnesium oxide with hydroxypropyl methylcellulose, glyceryl behenate, lactose, and colloidal silica in optimized ratios. This composite structure provides balanced release kinetics that enhance bioavailability while maintaining therapeutic effectiveness.
3Reliability
If a protective coating is applied to slow magnesium dissolution in the stomach, then dissolution rate is controlled, but coating complexity increases
Solution Approach 1:
The patent simplifies the coating formulation by using specific parameter ranges: magnesium oxide (5-20 parts), calcium carbonate (5-20 parts), and cellulose derivatives (40-80 parts). These parameter optimizations enable controlled dissolution rate while keeping the coating composition relatively simple and manufacturable.
Solution Approach 2:
The patent employs a coating layer that is applied and then dissolved as needed, rather than requiring complex multi-layer or long-lasting structures. The coating serves its protective and controlling function temporarily during gastric transit and then dissolves to release magnesium in the intestine, reducing overall system 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 composition achieves a controlled and progressive release of magnesium, enhancing bioavailability by maintaining a slow dissolution rate in the stomach and small intestine, maximizing absorption at the ileum, and ensuring optimal magnesium levels throughout the intestinal tract.
Implementation Method 1
a hydrophilic delay agent (B1), a hydrophobic delay agent (B2)... 180 to 190 parts by weight of hydroxypropyl methylcellulose
Implementation Method 2
a hydrophobic delay agent (B2)... 19.8 to 22.2 parts by weight of glyceryl behenate
Implementation Method 3
coated with a non-gastro-resistant coating to slow down magnesium release in the stomach
Implementation Method 4
an inert filler (C1) acting as a diluent and an inert filler (C2) acting as a lubricating means, being characterized in that it comprises... 10 to 12 parts by weight of lactose, and 10 to 12 parts by weight of colloidal silica
Data Source
AI summary
The present invention relates to use of a matrix for the oral administration, in tablet form, of gradual continuous release Mg provided with a protective coating slowing down the gastric dissolution of the Mg, said matrix being characterized in that it includes, for the administration (A) of 90 to 110 parts by weight of magnesium, the following ingredients: (B1) 180 to 190 parts by weight of hydroxypropylmethyl cellulose; (B2) 19.8 to 22.2 parts by weight of glyceryl behenate; (C1) 10 to 12 parts by weight of lactose; and (C2) 10 to 12 parts by weight of colloidal silica. The invention also relates to the gradual release composition including said matrix and the coating thereof.