Prednisolone Acetate Oral Suspension Formulation
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Solution Overview
Problem
Prednisolone acetate's poor aqueous solubility limits its use in oral formulations due to bitter taste and stability issues, leading to variable dosage and patient compliance problems.
Innovation Solution
A novel oral liquid suspension of prednisolone acetate with a pharmaceutically acceptable vehicle and thickening agent, such as glycerin and carbomer, maintaining a specific particle size and pH range to prevent taste interaction and ensure stability, including excipients like poloxamer, sucralose, and antimicrobial agents.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If prednisolone acetate is used in oral liquid formulations, then bitter taste perception is prevented due to poor aqueous solubility, but stability and uniform dosage are compromised because the active agent settles out over time
Solution Approach 1:
The patent introduces a surfactant as an intermediary substance that mediates between the hydrophobic prednisolone acetate particles and the aqueous vehicle. The surfactant adsorbs at the particle-liquid interface, reducing interfacial tension and preventing particle aggregation and settling, thereby maintaining suspension stability without requiring the prednisolone acetate to dissolve in the aqueous environment.
Solution Approach 2:
The patent modifies physical parameters of the suspension system, specifically adjusting the particle size of prednisolone acetate to a fine range (1-10 μm) and optimizing the concentration of surfactant and thickening agent. These parameter changes enhance suspension stability by increasing surface area for surfactant coverage and providing viscous support to prevent settling, while maintaining the insoluble state that prevents bitter taste.
2Object-affected harmful factors
If prednisolone acetate is made insoluble in aqueous environment to prevent bitter taste, then taste advantage is achieved, but solubility and uniform distribution are reduced
Solution Approach 1:
The surfactant acts as a mediator that enables uniform distribution of insoluble prednisolone acetate particles throughout the aqueous vehicle. By adsorbing onto particle surfaces and providing steric or electrostatic repulsion, the surfactant prevents particle aggregation and promotes homogeneous dispersion, achieving uniform dosage delivery without requiring dissolution.
Solution Approach 2:
The patent creates a composite suspension system combining prednisolone acetate particles with surfactant molecules and thickening agents. This composite formulation leverages the hydrophobic drug particles for potency, the surfactant for dispersion and stabilization, and the thickening agent for viscosity control, achieving uniform distribution while maintaining insolubility and taste advantage.
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 formulation provides a stable, palatable, and effective oral delivery of prednisolone acetate with uniform particle distribution, preventing bitter taste perception and maintaining bioavailability, stability, and antimicrobial properties, meeting regulatory standards and demonstrating bioequivalence with commercial tablets.
Implementation Method 1
The present invention is to a pharmaceutical composition for oral delivery comprising a pharmaceutically effective amount of prednisolone acetate, pharmaceutically acceptable vehicle and a thickening agent
Implementation Method 2
The excipients include wetting agents, spreading agents, stabilizers, sweeteners and flavoring agents
Implementation Method 3
The aqueous vehicle may be comprised of glycerin, and the preferred thickening agent is carbomer
Data Source
AI summary
The present invention relates to novel oral suspension formulation comprising prednisolone acetate, a pharmaceutically acceptable vehicle and a thickening agent. The present invention further provides a method of treating patients in need of prednisolone with the novel formulation.