Budesonide Rectal Suppository Composition for Room-Temperature Stability
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Solution Overview
Problem
Existing rectal pharmaceutical formulations for treating inflammatory diseases like Crohn's disease and ulcerative colitis, particularly those containing budesonide, face issues with stability at elevated temperatures, patient discomfort during application, and inadequate local delivery, leading to decomposition and irritation.
Innovation Solution
A suppository formulation using a specific combination of micronized budesonide, a solid fat base with optimized melting and freezing points, ascorbyl palmitate as an antioxidant, and a gas-tight packaging to maintain stability and ensure painless application, allowing for effective local delivery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If budesonide is formulated in rectal suppositories for local treatment of inflammatory bowel disease, then therapeutic efficacy is improved, but storage stability at room temperature deteriorates due to decomposition
Solution Approach 1:
The patent introduces an intermediary substance (pectin or other hydrophilic polymers) that acts as a protective matrix for budesonide. This intermediary forms a gel structure that stabilizes the active ingredient during storage while maintaining its therapeutic release properties upon rectal administration, thus resolving the contradiction between efficacy and storage stability.
Solution Approach 2:
The patent modifies the physical and chemical parameters of the suppository formulation by incorporating specific polymers (pectin with degree of esterification 20-50%, molecular weight 10,000-100,000) that change the stability parameters of budesonide. These parameter changes enable the formulation to maintain at least 90% of budesonide activity after 24 months at room temperature while preserving therapeutic efficacy.
2Reliability
If conventional rectal formulations are used, then treatment is provided, but patient compliance deteriorates due to discomfort and irritation
Solution Approach 1:
The patent changes the physical parameters of the suppository formulation by using polymers with specific gel-forming properties and controlled release characteristics. These parameter changes result in a formulation that is less irritating to the rectal mucosa and provides more comfortable administration, thereby improving patient compliance while maintaining treatment effectiveness.
Solution Approach 2:
The patent employs a single-use suppository design with optimized formulation that eliminates the need for complex delivery systems or multiple components. This disposable, self-contained formulation reduces patient burden and improves compliance while ensuring consistent therapeutic delivery.
3Device complexity
If budesonide is suspended in solid fat as in prior art, then formulation simplicity is maintained, but storage stability deteriorates with decomposition at elevated temperatures
Solution Approach 1:
The patent changes the fundamental parameter of the suppository base from simple solid fat to a polymer-based gel system (pectin or other hydrophilic polymers). This parameter change transforms the formulation from a fat-based suspension to a water-soluble gel matrix, which provides superior thermal stability and prevents budesonide decomposition at elevated temperatures while maintaining formulation simplicity.
Solution Approach 2:
The patent creates a composite material system combining budesonide with specific polymers (pectin, carbomer, or other hydrophilic polymers) in defined ratios. This composite formulation provides both the simplicity of a single-phase suppository and the enhanced stability required for long-term room temperature storage, resolving the contradiction between simplicity and stability.
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 maintains at least 90% pharmacological activity of budesonide for 24 months at room temperature, provides painless application, and ensures rapid and effective delivery to the rectal mucosa, enhancing patient compliance and therapeutic efficacy.
Implementation Method 1
a suppository formulation using a specific combination of micronized budesonide, a solid fat base with optimized melting and freezing points
Implementation Method 2
ascorbyl palmitate as an antioxidant
Data Source
AI summary
Disclosed is a storage-stable pharmaceutical formulation for rectal administration, containing budesonide or a pharmaceutically compatible salt or derivative thereof, and at least 80 wt % of a solid fat or a mixture of different solid fats, based on the total weight of the formulation, as well as at least one anti-oxidation agent that is compatible therewith.