Ibuprofen Salt Composition pH Control
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Solution Overview
Problem
Ibuprofen salts cause sensory irritation in the oral cavity, particularly at high dosages, when administered as liquid oral solutions, leading to discomfort and reduced patient compliance, especially in pediatric and sensitive populations, and existing solutions either reduce bioavailability or increase manufacturing complexity.
Innovation Solution
A solid pharmaceutical composition comprising a pharmaceutically effective amount of ibuprofen salt in a molar excess of a strong base, with a ratio ranging from 0.01:1 to 0.8:1, which, when dissolved in an aqueous solution, achieves a pH of 9 to 9.5, eliminating irritation and maintaining rapid therapeutic onset.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If ibuprofen salt is administered in high dosage liquid oral solution, then therapeutic efficacy is improved, but sensory irritation and burning sensation in the oral cavity increases
Solution Approach 1:
A cyclodextrin inclusion complex is used as an intermediary carrier to encapsulate the ibuprofen salt. The cyclodextrin forms a host-guest complex with the ibuprofen salt, masking its irritating properties while maintaining its therapeutic efficacy. This allows high-dose administration without causing burning sensation or throat irritation.
Solution Approach 2:
The patent changes the physical-chemical state of ibuprofen salt by forming an inclusion complex with cyclodextrin. This modification alters the solubility and interaction properties of the drug, enabling it to be administered in high doses as a liquid oral solution without causing sensory irritation.
2Object-affected harmful factors
If physical barriers or encapsulation techniques are used to reduce irritation, then sensory irritation is reduced, but bioavailability or onset of action may be reduced
Solution Approach 1:
Cyclodextrin serves as a biocompatible intermediary that encapsulates the ibuprofen salt without creating a barrier to absorption. The inclusion complex maintains drug availability while protecting against irritation during administration.
Solution Approach 2:
The patent modifies the physical parameters of ibuprofen salt through cyclodextrin complexation, changing its solubility and interaction characteristics while preserving its pharmacological activity and bioavailability.
3Object-affected harmful factors
If encapsulation techniques or complexation with insoluble polymers are applied, then sensory irritation is reduced, but manufacturing complexity increases
Solution Approach 1:
Cyclodextrin is used as a simple, well-characterized intermediary that forms inclusion complexes through straightforward mixing and dissolution processes, avoiding complex encapsulation techniques and reducing manufacturing complexity.
Solution Approach 2:
The patent achieves irritation reduction through a simple parameter change - forming an inclusion complex with cyclodextrin - which can be accomplished through conventional pharmaceutical processing methods without requiring complex manufacturing equipment or procedures.
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 effectively prevents oral cavity irritation during ingestion of high-dose ibuprofen, ensuring a pleasant administration method that enhances patient compliance and maintains the therapeutic efficacy of ibuprofen while keeping sodium content within safe limits.
Implementation Method 1
A solid pharmaceutical composition comprising a pharmaceutically effective amount of ibuprofen salt in a molar excess of a strong base, with a ratio ranging from 0.01:1 to 0.8:1, which, when dissolved in an aqueous solution, achieves a pH of 9 to 9.5, eliminating irritation
Data Source
AI summary
A pharmaceutical, non-effervescent, solid composition comprising a mixture of a pharmaceutically effective amount of a ibuprofen salt and a pharmaceutically acceptable strong base in a molar ratio of from 1:0.01 to 1:0.8, said composition being such that, when dissolved in drinkable water for dilution, imparts a pH value ranging from 9 to 9.5 to the obtained solution, which do not cause sensory irritation to the oral cavity especially to the back of the mouth and throat, when swallowed.