pH-Dependent Softgel Shell Composition for Targeted GI Release
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Solution Overview
Problem
Existing delayed release dosage forms face issues with uneven coating, cracking, flaking, and leakage due to pH-dependent coatings, leading to unintended release of active agents at stomach pH variations and instability, especially above the typical gastric pH of 1.2, and do not effectively target release at specific gastrointestinal locations.
Innovation Solution
Development of delayed release softgel capsules using a pH-dependent shell composition comprising gelatin, gellan gum, and pectin, optionally with a plasticizer and dextrose, which does not require a pH-dependent coating, ensuring the capsules do not rupture at gastric pH levels and allow targeted release at specific pH ranges within the gastrointestinal tract.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional pH dependent coatings are applied to capsule surfaces, then delayed release function is achieved, but the coating is prone to cracking or flaking off and appears rough
Solution Approach 1:
The patent merges the pH-dependent coating function directly into the capsule shell composition by incorporating pH-dependent polymers during shell formation. This integration eliminates the separate coating step and ensures the pH-dependent properties are inherent to the shell structure, preventing cracking and flaking while maintaining delayed release function.
Solution Approach 2:
The patent uses composite materials by combining gelatin with pH-dependent polymers (such as cellulose acetate phthalate, hydroxypropyl methyl cellulose phthalate, or polyvinyl acetate phthalate) to create a shell that inherently resists cracking and flaking. This composite approach provides both structural integrity and pH-dependent release characteristics.
2Reliability
If pH dependent coatings are applied through spraying and drying at elevated temperatures, then delayed release function is achieved, but the process is very inefficient
Solution Approach 1:
The patent combines the shell formation and pH-dependent coating steps into a single process by incorporating pH-dependent polymers during shell preparation. This eliminates the separate spraying and drying steps, significantly improving process efficiency while maintaining delayed release functionality.
Solution Approach 2:
The patent performs the pH-dependent coating action preliminarily during shell formation rather than as a subsequent step. By incorporating the pH-dependent polymers into the shell composition before capsule formation, the coating function is established in advance, eliminating the need for post-formation coating processes.
3Reliability
If conventional pH dependent polymers are added in the capsule shell, then delayed release function is achieved, but the capsules are prone to leaking due to insufficient sealing
Solution Approach 1:
The patent uses composite materials by combining gelatin with specifically selected pH-dependent polymers that provide both delayed release function and adequate sealing. The composite shell composition is designed to maintain structural integrity and prevent leakage while achieving pH-dependent release characteristics.
Solution Approach 2:
The patent adjusts the composition parameters of the shell by controlling the ratio and type of pH-dependent polymers incorporated during shell formation. By optimizing these parameters, the shell achieves both sufficient sealing to prevent leakage and the necessary pH-dependent release properties.
4Reliability
If typical delayed release formulations release active agents at pH slightly above stomach pH, then delayed release function is achieved, but patient variability in stomach pH causes unintentional release
Solution Approach 1:
The patent changes the pH threshold parameter of the shell composition by incorporating specific pH-dependent polymers that maintain shell integrity at a wider range of pH values. This allows the capsule to withstand variability in stomach pH and ensure release only at the intended target pH, improving both delayed release function and adaptability to patient variability.
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 capsules provide controlled release of active agents at targeted gastrointestinal locations, minimizing stomach irritation and belching, and maintaining stability across varying pH levels, including those above the typical gastric pH, thus enhancing therapeutic efficacy and patient compliance.
Implementation Method 1
the gelatin-based shell compositions comprise pectin and gellan gum... do not release or do not substantially release the active agent at certain pH levels above the pH of the stomach
Data Source
AI summary
Disclosed in certain embodiments is a delayed release softgel capsules comprise a fill material that is encapsulated in a pH dependent shell composition, the pH dependent shell composition including pectin and gellan gum. Also disclosed are methods of preparing any of the delayed release softgel capsules described herein and methods of use thereof.