Plant Fat Matrix Encapsulating Macrogol for Colon-Targeted Laxative Delivery
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Solution Overview
Problem
Existing osmotic laxative formulations, particularly those using macrogol, require high daily doses to maintain osmotic pressure until reaching the colon, leading to side effects like bloating, gas, and stomach cramps due to moisture contact in the digestive tract, and lack effective methods to reduce these doses while maintaining efficacy.
Innovation Solution
A hydrophobic matrix based on plant fats with a melting point of 36° C. to 38° C. is used to encapsulate macrogol, forming an anhydrous hydrophobic lipid coating that protects macrogol from moisture until it reaches the colon, allowing for reduced daily doses of 5 to 15 g and minimizing side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high doses of macrogol are administered to maintain osmotic pressure until reaching the colon, then laxative efficacy is improved, but side effects such as bloating, gas, and stomach cramps increase
Solution Approach 1:
The patent introduces a hydrophobic matrix as an intermediary carrier that protects macrogol from premature contact with moisture in the digestive tract. This matrix acts as a protective barrier, allowing macrogol to reach the colon intact while eliminating the need for high doses that cause side effects in the upper gastrointestinal tract.
Solution Approach 2:
The patent changes the physical state and protective environment of macrogol by incorporating it into a hydrophobic matrix with specific melting properties. This parameter change allows macrogol to maintain its osmotic pressure until reaching the colon, enabling effective laxative action at reduced doses (5-15g/day) without the harmful side effects associated with conventional high doses.
2Ease of operation
If macrogol is exposed to moisture in the digestive tract, then absorption and distribution improve, but osmotic pressure is reduced before reaching the colon
Solution Approach 1:
The hydrophobic matrix serves as a protective intermediary that prevents premature interaction between macrogol and moisture in the stomach and small intestine. This barrier ensures macrogol maintains its osmotic pressure until reaching the colon, where it is then released to exert its laxative effect.
Solution Approach 2:
The patent employs a hydrophobic matrix that forms a protective coating around macrogol particles. This matrix acts as a flexible barrier that protects macrogol from moisture while allowing controlled release in the colon, maintaining osmotic pressure integrity throughout the digestive tract.
3Device complexity
If conventional formulations are used without hydrophobic protection, then formulation simplicity is maintained, but reduced doses of macrogol cannot be achieved
Solution Approach 1:
The patent creates a composite formulation combining macrogol with a hydrophobic matrix made of plant-based fats and waxes. This composite structure provides the necessary protective properties to enable reduced dosing (5-15g/day) while maintaining formulation feasibility through the use of natural, readily available materials.
Solution Approach 2:
The patent modifies the physical parameters of the formulation by incorporating macrogol into a hydrophobic matrix with specific melting characteristics (36-38°C). This parameter change enables the matrix to protect macrogol in the upper GI tract while releasing it in the colon, making reduced doses effective and eliminating the need for conventional high doses.
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 effectively reduces daily macrogol doses to 5 to 15 g, minimizing side effects by maintaining osmotic pressure and releasing macrogol only in the colon, thus enhancing the efficacy of the laxative while using plant-origin compounds.
Implementation Method 1
A hydrophobic matrix based on plant fats with a melting point of 36° C. to 38° C. is used to encapsulate macrogol, forming an anhydrous hydrophobic lipid coating that protects macrogol from moisture until it reaches the colon
Implementation Method 2
Osmotic laxatives, such a macrogol, are part of a category of laxatives that retain water, increasing the volume of the stools, making them softer and easier to pass
Implementation Method 3
a hydrophobic matrix based on plant fats with a melting point at the temperature of the human body, and more specifically ranging from 36° C. to 38° C.
Data Source
AI summary
Oral medicament comprising an osmotic laxative incorporated into a matrix based on plant fats. The present invention relates to an oral pharmaceutical composition comprising: between 30 and 55% by weight of said pharmaceutical composition of micronized anhydrous macrogol; and between 45 and 70% by weight of the pharmaceutical composition of a carrier consisting of an anhydrous hydrophobic lipid coating based on fatty compounds of plant origin, having a melting point of between 36 and 38° C., and to the use thereof as laxative. Said composition enables the reduction in the daily dosage of macrogol by preserving the osmotic pressure thereof as far as the colon, the site of therapeutic action of osmotic laxatives; said carrier protects the macrogol from a reduction, due to the moisture in the digestive tract, in the osmotic pressure.