Ibuprofen Eutectic Formulation for Smaller Soft Gelatin Capsules
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Solution Overview
Problem
Current soft gelatin capsules for ibuprofen are larger than desired, making them less consumer-friendly, and there is a need for a formulation that maintains or improves the therapeutic profile while being smaller and providing quicker onset of action.
Innovation Solution
A composition comprising ibuprofen, one or more polyoxysorbitan esters, and a base, with specific weight ratios, along with optional polyethylene glycol and water, encapsulated in a soft gelatin shell, which allows for controlled release and improved solubility in gastric fluid.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Volume of moving object
If conventional ibuprofen formulations are used in soft gelatin capsules, then the therapeutic profile is maintained, but the capsule size becomes large and less consumer-friendly
Solution Approach 1:
The patent changes the chemical parameters of the formulation by using a eutectic mixture of ibuprofen with benzoic acid or salicylic acid. This parameter change allows the active ingredient to be delivered in a smaller volume while maintaining the therapeutic profile, directly resolving the contradiction between capsule size and therapeutic effectiveness
Solution Approach 2:
The invention uses a composite material system consisting of ibuprofen combined with benzoic acid or salicylic acid in specific ratios. This composite approach creates a eutectic mixture that reduces the overall volume required to deliver the therapeutic dose, enabling smaller capsule sizes without compromising the therapeutic profile
2Speed
If conventional ibuprofen formulations are used, then the therapeutic dose is delivered, but the onset of action is slower
Solution Approach 1:
The patent changes the physical state parameters of ibuprofen by forming a eutectic mixture, which alters the dissolution characteristics. This parameter change enables faster onset of action while maintaining complete therapeutic effectiveness, as the eutectic mixture dissolves more rapidly in gastric fluid
Solution Approach 2:
The eutectic mixture acts as an intermediary system between the ibuprofen active ingredient and the gastric fluid. The presence of benzoic acid or salicylic acid as mediators facilitates faster dissolution and absorption of ibuprofen, accelerating onset of action while ensuring complete therapeutic delivery
3Volume of moving object
If higher concentrations of ibuprofen are used to reduce capsule size, then capsule volume decreases, but solubility in gastric fluid becomes problematic
Solution Approach 1:
The patent changes the solubility parameters by forming a eutectic mixture with benzoic acid or salicylic acid. This parameter change allows high concentrations of ibuprofen (50-75% w/w) to be incorporated into the capsule while maintaining excellent solubility in gastric fluid, simultaneously achieving reduced capsule volume and preserved solubility
Solution Approach 2:
The invention creates a composite material system where ibuprofen is combined with solubility-enhancing agents (benzoic acid or salicylic acid) in a eutectic ratio. This composite approach enables the formulation to achieve both high ibuprofen concentration for smaller capsule size and improved solubility characteristics for complete dissolution in gastric fluid
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 results in a smaller, more consumer-friendly capsule with a quicker release profile for ibuprofen, maintaining therapeutic effectiveness and stability, and allowing for a lower base content while enhancing solubilization in simulated gastric fluid.
Implementation Method 1
a stable highly concentrated solution of ibuprofen... the weight ratio of the one or more polyoxysorbitan esters to ibuprofen is from 0.1:1-0.9:1
Implementation Method 2
Soft gelatin capsules are also useful for protecting APIs from light and oxygen thus improving their stability
Implementation Method 3
They are easily digested and dissolve quickly in the stomach thus allowing quicker onset of the desired pharmaceutical effect
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 0.1:1-0.9:1, the weight ratio of the base to ibuprofen is from 1:6-1:20 and the weight ratio of the one or more polyoxysorbitan esters to base is 1:1-13:1 and wherein the ibuprofen is present at an amount of 50%-65% w/w.