Multiparticulate L-menthol enteric coating for IBS
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Solution Overview
Problem
Current enteric-coated peppermint oil capsules for treating irritable bowel syndrome (IBS) face issues such as premature release in the stomach, unpredictable absorption, and frequent dosing due to their single-unit formulation, leading to gastric irritation and variable bioavailability.
Innovation Solution
A multiparticulate formulation of high purity L-menthol with an enteric coating that prevents release in gastric pH and facilitates release in intestinal pH, using a core composition of at least 80% L-menthol with a methacrylic acid-based copolymer coating, ensuring controlled and prolonged release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If single-unit enteric-coated peppermint oil capsules are used, then the oil is protected from premature release in the stomach, but the capsules may get attached to the esophagus or fail to pass through the pylorus valve due to their size and muco-adhesive properties
Solution Approach 1:
The single-unit capsule is divided into multiple smaller particulates (microcapsules, granules, or pellets) that can pass through the pylorus valve more easily. Each particulate is individually enteric-coated, maintaining the protective function while improving passage through gastrointestinal constrictions.
Solution Approach 2:
The invention transitions from a single large-unit formulation to a distributed multi-particulate system, changing the dimensional approach from one large object to many small objects of similar size, enabling better passage through physiological constrictions while maintaining enteric protection.
2Device complexity
If single-unit enteric capsules are used, then the formulation structure is simple, but the amount of peppermint oil absorbed by the intestines varies from dose to dose due to unpredictable gastric emptying and coating rupture
Solution Approach 1:
The single-unit capsule is segmented into multiple smaller enteric-coated particulates. This segmentation ensures more predictable gastric emptying behavior and reduces the risk of coating rupture, leading to more consistent release and absorption of peppermint oil in the intestines.
Solution Approach 2:
The invention changes the physical parameters of the formulation by reducing particle size and increasing the number of particulates. This parameter change affects gastric emptying rate and distribution, improving the consistency of drug absorption while maintaining enteric protection.
3Reliability
If high doses of peppermint oil are administered to achieve efficacious concentration, then the therapeutic effect is improved, but gastric irritation and heartburn increase due to premature release
Solution Approach 1:
By dividing the total dose into multiple smaller enteric-coated particulates, the invention ensures that the full therapeutic dose reaches the intestines without premature release in the stomach. This maintains therapeutic efficacy while eliminating gastric irritation associated with premature oil release.
Solution Approach 2:
The invention uses multiple disposable enteric-coated particulates that are designed to dissolve only in the intestinal environment. Each particulate serves its protective function briefly in the stomach and then dissolves in the intestine, delivering the full dose without gastric exposure.
4Object-affected harmful factors
If enteric-coated capsules are used to delay release until intestines, then gastric irritation is reduced, but the capsules may prematurely crack or rupture due to swelling of the gelatin seal coat against the thinner outer enteric coat
Solution Approach 1:
The invention segments the formulation into multiple small enteric-coated particulates with adequate coating thickness on each particle. This segmentation reduces the mechanical stress on individual coatings during gastric swelling, preventing premature rupture while maintaining gastric protection.
Solution Approach 2:
The enteric coating is applied as a flexible, pH-sensitive film that can accommodate gastric swelling without cracking. The coating material and thickness are optimized to provide mechanical flexibility during gastric residence while maintaining integrity until intestinal pH triggers dissolution.
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 provides reduced gastric irritation, improved bioavailability, and prolonged duration of action, allowing for effective treatment of gastrointestinal disorders with reduced side effects and increased patient convenience.
Implementation Method 1
The enteric coating is effective to substantially prevent release of the L-menthol from the core into a gastric pH environment and to release L-menthol from the core into an intestinal pH environment
Implementation Method 2
The enteric coating is effective to substantially prevent release of the L-menthol from the core into a gastric pH environment and to release L-menthol from the core into an intestinal pH environment
Data Source
AI summary
An L-menthol pharmaceutical dosage form includes an effective amount of L-menthol for treating a gastrointestinal disorder. The L-menthol is within a plurality of particulates having a core and an enteric coating over the core. The core includes an L-menthol source that is at least 80% pure L-menthol. The dosage form may be used to treat gastrointestinal disorders, such as irritable bowel syndrome.