Ibuprofen Soft Gelatin Capsule Solubilization via Polyoxysorbitan Esters
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Solution Overview
Problem
Current soft gelatin capsules containing ibuprofen have a release rate and onset of pharmaceutical effect that is not sufficiently quick, with ongoing efforts to improve speed of action.
Innovation Solution
A composition for soft gelatin capsules comprising ibuprofen, one or more polyoxysorbitan esters, and a base, with specific weight ratios of these components, along with optional polyethylene glycol and water, to enhance solubility and release rate of ibuprofen in simulated gastric fluid.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If conventional soft gelatin capsules containing ibuprofen are used, then the basic pharmaceutical effect is achieved, but the release rate and onset of action are not sufficiently quick
Solution Approach 1:
The patent changes the chemical parameters of the solvent system by using a specific mixture of diethylene glycol monoethyl ether (20-40% w/w) and polyglycerol oleate (60-80% w/w), along with controlled amounts of base (0.5-5% w/w). This parameter optimization enables rapid solubilization of ibuprofen while maintaining formulation stability during encapsulation and storage.
Solution Approach 2:
The invention uses a composite solvent system combining two different solvents (diethylene glycol monoethyl ether and polyglycerol oleate) with complementary properties. This composite approach leverages the solubilizing power of the ether and the emulsifying properties of the polyglycerol ester to achieve both fast release and stable encapsulation.
2Speed
If the amount of base is increased to improve solubility, then the release rate improves, but the stability of the composition during encapsulation deteriorates due to gelatin degradation
Solution Approach 1:
The patent precisely controls the base concentration parameter, limiting it to 0.5-5% w/w of the total composition. This parameter optimization ensures sufficient solubility enhancement while preventing excessive alkalinity that would degrade gelatin during the encapsulation process, thus maintaining both release rate and compositional stability.
3Speed
If ibuprofen is encapsulated in soft gelatin capsules, then quick dissolution and onset of effect are achieved, but further improvement in speed of action is limited by conventional formulations
Solution Approach 1:
The patent employs a composite solvent system with two main components (diethylene glycol monoethyl ether and polyglycerol oleate) in specific ratios. This composite approach achieves enhanced solubilization and faster onset of effect without excessive complexity, as the synergistic interaction between the two solvents provides superior performance compared to single-solvent systems.
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 allows for rapid solubilization of ibuprofen, with at least 5% of the dose solubilized within 5 minutes in simulated gastric fluid, significantly improving the release rate compared to existing capsules.
Implementation Method 1
The composition allows for rapid solubilization of ibuprofen, with at least 5% of the dose solubilized within 5 minutes in simulated gastric fluid
Implementation Method 2
A composition for soft gelatin capsules comprising ibuprofen, one or more polyoxysorbitan esters, and a base
Data Source
AI summary
The present invention relates to a composition for encapsulation in a soft gelatin shell which comprises ibuprofen, one or more polyoxysorbitan esters and a base wherein the weight ratio of the one or more polyoxysorbitan esters to ibuprofen is from 0.0025:1 - 1.5:1, the weight ratio of the base to ibuprofen is from 1:3 - 1:12 and the weight ratio of the one or more polyoxysorbitan esters to base is 0.009:1 - 11: 1.