Micronized Budesonide Ophthalmic Composition for Prolonged Action
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Solution Overview
Problem
Current pharmaceutical compositions for treating ocular inflammation, such as those containing budesonide, suffer from issues like frequent administration requirements due to short-acting formulations, causing discomfort and side effects, and lack effective, prolonged anti-inflammatory action without irritating the eye.
Innovation Solution
A composition comprising micronized budesonide powder with an average size distribution of 0.05 µm to 20 µm, suspended in an aqueous carrier with water-soluble carboxymethylcellulose (CMC) and other excipients, providing a prolonged anti-inflammatory effect through controlled delivery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If conventional budesonide formulations are used, then anti-inflammatory action is provided, but frequent administration is required due to short duration of action
Solution Approach 1:
The patent changes the physical state of budesonide from conventional forms to a specific micronized powder form with controlled particle size distribution (0.05-20 µm). This parameter change in particle morphology and size enables prolonged retention on the ocular surface, extending the duration of anti-inflammatory action and reducing administration frequency.
Solution Approach 2:
The invention creates a composite ophthalmic composition by combining micronized budesonide powder with specific excipients and suspending agents. This composite formulation enhances the pharmaceutical properties of budesonide, providing sustained release and prolonged therapeutic effect while minimizing the need for frequent dosing.
2Reliability
If frequent administration is required, then therapeutic effect is maintained, but patient discomfort and side effects increase
Solution Approach 1:
The micronized budesonide formulation provides continuous and sustained anti-inflammatory action through controlled release from the ocular surface. This continuous therapeutic effect maintains reliability of treatment while reducing the need for repeated administrations, thereby minimizing cumulative irritation and side effects.
Solution Approach 2:
The formulation dynamics are optimized through specific particle size distribution and excipient selection, enabling the composition to adapt to ocular surface conditions. The dynamic release profile maintains effective drug concentration over extended periods while reducing peak concentrations that cause irritation, thus balancing therapeutic reliability with reduced harmful effects.
3Reliability
If budesonide is administered topically, then local anti-inflammatory action is achieved, but formulation stability and suspension properties are challenging
Solution Approach 1:
The patent specifies precise parameter ranges for particle size (0.05-20 µm) and particle size distribution of the micronized budesonide powder. These controlled parameters ensure optimal suspension stability, prevent precipitation, and maintain uniform drug distribution in the ophthalmic formulation, simplifying the overall formulation complexity while ensuring reliable local efficacy.
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 offers a prolonged anti-inflammatory action with reduced irritation, minimizing the need for frequent applications and reducing side effects, thus improving patient tolerance and treatment efficacy.
Implementation Method 1
A composition comprising micronized budesonide powder with an average size distribution of 0.05 µm to 20 µm, suspended in an aqueous carrier with water-soluble carboxnymethylcellulose (CMC)
Implementation Method 2
suspended in an aqueous carrier with water-soluble carboxnymethylcellulose (CMC) and other excipients, providing a prolonged anti-inflammatory effect through controlled delivery
Data Source
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AI summary
The present invention relates to budesonide, or a salt thereof, or mixtures thereof for ophthalmic use in a method for the curative treatment of an eye disorder or ailment or disease in a subject in need. Further, the present invention relates to a composition comprising a mixture comprising or, alternatively, consisting of: (i) a budesonide, or a salt thereof, or mixtures thereof; (ii) at least one suspending/thickening agent, and optionally one or more physiologically and/or pharmacologically acceptable excipients; said composition being for use in a method for the curative treatment of an inflammation of the and ocular adnexa or inflammation of the eyeball in a subject in need.