Ophthalmic Suspension Stabilization with Ionic and Non-Ionic Agents
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Solution Overview
Problem
Current ophthalmic formulations of fluoroquinolone antibiotics, such as gatifloxacin and moxifloxacin, face challenges with stability and distribution due to their properties, leading to issues like flocculation, coagulation, and reduced efficacy, particularly when combined with corticosteroids like triamcinolone acetonide, and there is a need for formulations that provide broad-spectrum antibiotic activity and anti-inflammatory effects while minimizing inflammation risk.
Innovation Solution
A pharmaceutical composition comprising gatifloxacin, prednisolone, and bromfenac in a stable suspension form, utilizing a combination of non-ionic and ionic suspension agents, along with a pharmaceutically acceptable chelating agent, to enhance stability and reduce flocculation, coagulation, and clumping, while maintaining therapeutic efficacy.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If fluoroquinolone antibiotics are combined with corticosteroids in ophthalmic formulations, then broad-spectrum antibiotic activity and anti-inflammatory effects are provided, but stability issues arise leading to flocculation, coagulation, and reduced efficacy
Solution Approach 1:
The patent introduces non-ionic and ionic suspension agents as intermediary substances that mediate between the fluoroquinolone antibiotic and corticosteroid components. These suspension agents prevent direct interaction that causes flocculation and coagulation, thereby maintaining formulation stability while preserving the therapeutic benefits of the combination.
Solution Approach 2:
The patent modifies physical and chemical parameters of the formulation by adjusting pH, ionic strength, and suspension agent concentrations. These parameter changes optimize the compatibility between fluoroquinolone and corticosteroid, preventing instability issues while maintaining broad-spectrum antibiotic activity and anti-inflammatory effects.
2Reliability
If fluoroquinolone antibiotics are used in ophthalmic formulations, then effective treatment of bacterial infections is achieved, but flocculation and coagulation occur reducing distribution and efficacy
Solution Approach 1:
Suspension agents serve as intermediary substances that prevent flocculation and coagulation of fluoroquinolone antibiotic particles. These agents maintain uniform distribution of the antibiotic throughout the formulation, ensuring reliable treatment efficacy while preventing aggregation that would reduce distribution and effectiveness.
Solution Approach 2:
The patent creates a composite ophthalmic formulation that integrates fluoroquinolone antibiotic with suspension agents and other excipients. This composite structure prevents flocculation and coagulation while maintaining uniform distribution, thereby ensuring reliable treatment efficacy through consistent drug delivery.
3Ease of operation
If multiple active ingredients are combined in a single formulation, then treatment complexity is reduced, but formulation stability and compatibility become more difficult to maintain
Solution Approach 1:
Suspension agents act as intermediary substances that facilitate compatibility between multiple active ingredients including fluoroquinolone antibiotics and corticosteroids. These intermediaries prevent adverse interactions and maintain formulation stability, enabling simplified multi-ingredient treatment while ensuring ingredient compatibility.
Solution Approach 2:
The patent optimizes formulation parameters such as pH, ionic strength, and concentration ratios to maintain stability and compatibility of multiple active ingredients. These parameter adjustments enable the coexistence of different therapeutic agents in a single formulation, achieving treatment simplicity without sacrificing multi-ingredient compatibility.
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 achieves improved stability and uniform distribution of active ingredients, providing broad-spectrum antibiotic and anti-inflammatory effects with reduced inflammation risk, enhancing the treatment of ophthalmic infections and inflammatory conditions.
Implementation Method 1
utilizing a combination of non-ionic and ionic suspension agents, along with a pharmaceutically acceptable chelating agent, to enhance stability and reduce flocculation, coagulation, and clumping
Implementation Method 2
A pharmaceutical composition comprising gatifloxacin, prednisolone, and bromfenac in a stable suspension form, utilizing a combination of non-ionic and ionic suspension agents
Data Source
AI summary
Provided here are new ophthalmologically suitable pharmaceutical compositions comprising an effective amount of gatifloxacin, prednisolone, and bromfenac. In aspects, the compositions are suspensions that include a suspension component comprising one or more suspension agents. In aspects, the suspension component includes an ionic suspension agent. In aspects, the composition also or alternatively comprises a non-ionic surfactant, non-ionic suspension agent, or both, or an agent that provides both functions. In aspects, such compositions further comprise an effective amount of a chelating agent/component. Further described are related compositions and methods of making and using such compositions, e.g., in the treatment of eye infections.