Budesonide Capsule Coating With Integrated Acid for Stability
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Solution Overview
Problem
The existing Budesonide formulation for TARPEYO® has stability issues due to direct contact between the drug substance and the alkaline ethyl cellulose layer, requiring an additional intermediate citric acid layer for protection, which increases manufacturing complexity and cost.
Innovation Solution
Integrating the organic acid directly into the Budesonide layer prevents direct contact with the alkaline ethyl cellulose layer, eliminating the need for an intermediate layer and simplifying the manufacturing process while maintaining stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Stability of the object's composition
If an intermediate citric acid layer is added to protect the drug substance from the alkaline ethyl cellulose layer, then the stability of the drug substance is improved, but the manufacturing complexity and cost increase
Solution Approach 1:
The patent combines the protective acid layer and the drug substance layer into a single integrated layer. The Budesonide is formulated together with citric acid and hypromellose in one coating layer, eliminating the need for separate intermediate layers. This merging approach maintains drug stability while simplifying the manufacturing process to only two coating steps (first coating with Budesonide/hypromellose/PEG, second coating with ethyl cellulose/medium chain triglycerides/oleic acid/hypromellose/PEG).
Solution Approach 2:
The single coating layer serves multiple functions simultaneously: it provides the sustained release profile through hypromellose and PEG, protects the Budesonide from degradation through citric acid buffering, and maintains physical barrier properties. This multi-functional design eliminates the need for separate protective layers while achieving both release control and stability protection.
2Stability of the object's composition
If an intermediate citric acid layer is added to prevent direct contact with the alkaline layer, then the drug substance stability is improved, but the manufacturing time and cost increase
Solution Approach 1:
By merging the protective acid layer and drug substance layer into one integrated coating, the patent reduces the number of coating steps from three to two. The first coating step applies Budesonide, hypromellose, and PEG together with citric acid, eliminating the need for a separate intermediate citric acid layer application step, thus reducing manufacturing time while maintaining stability protection.
3Stability of the object's composition
If an additional coating layer is added to protect the drug substance, then the stability is improved, but the cost of goods and product cost increase
Solution Approach 1:
The patent merges multiple protective and functional layers into a single integrated coating formulation. By combining Budesonide, citric acid, hypromellose, and PEG in one layer, the patent eliminates the need for additional intermediate coating layers, thereby reducing material costs, manufacturing overhead, and overall product cost while maintaining comprehensive stability protection.
Solution Approach 2:
The single coating layer performs multiple functions including sustained release, protective buffering, and physical barrier properties, eliminating the need for separate protective layers. This multi-functional approach reduces the total number of materials and process steps required, directly lowering manufacturing costs while achieving the same stability protection.
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
This approach ensures stability without an intermediate layer, reducing manufacturing time and costs while maintaining the desired release profile, ensuring bioequivalence to the commercial formulation.
Implementation Method 1
Integrating the organic acid directly into the Budesonide layer prevents direct contact with the alkaline ethyl cellulose layer, eliminating the need for an intermediate layer and simplifying the manufacturing process while maintaining stability
Implementation Method 2
The coating of the capsules with methacrylate copolymer provides the delayed release feature to the drug product
Implementation Method 3
a first coating layer made of Budesonide, hypromellose and polyethylene glycol
Implementation Method 4
sustained release component comprises a first layer with Budesonide
Data Source
AI summary
The present invention relates to a Budesonide formulation with one or more layers comprising organic acid and Budesonide in the same layer.