Chewable Phenylephrine Tablet Aldehyde-Free Matrix
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Solution Overview
Problem
Phenylephrine-based pharmaceutical compositions are susceptible to degradation in excipient compositions, leading to the formation of isoquinoline degradants, especially in solid forms, which are more prone to degradation than liquid forms and are not suitable for chewable dosage forms due to instability and misuse concerns.
Innovation Solution
A chewable oral pharmaceutical composition comprising phenylephrine, an artificial sweetener, and a substantially aldehyde-free matrix, manufactured using roller compaction without liquid water or heat, minimizing degradation pathways and maintaining low levels of isoquinolines for extended periods.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If phenylephrine is formulated in a solid chewable dosage form, then ease of ingestion is improved for patients including young children and older persons, but phenylephrine degradation occurs leading to formation of isoquinoline degradants
Solution Approach 1:
The patent changes the chemical parameters of the excipient composition by eliminating aldehydes and using specific antioxidants (vitamin C, vitamin E, BHT) to create a formulation environment that prevents phenylephrine degradation while maintaining chewable tablet form. This resolves the contradiction by modifying the compositional parameters rather than the physical form.
Solution Approach 2:
The patent introduces intermediary substances (antioxidants such as vitamin C, vitamin E, and BHT) that mediate between phenylephrine and the excipient environment, preventing direct degradation reactions while allowing the chewable tablet to function properly.
2Adaptability or versatility
If phenylephrine is formulated in solid forms, then dosage form versatility is improved, but degradation susceptibility increases compared to liquid forms
Solution Approach 1:
The patent modifies the chemical parameter profile of the solid formulation by removing aldehyde-containing excipients and incorporating specific antioxidants, thereby achieving reliability comparable to liquid forms while maintaining the advantages of solid dosage forms.
3Reliability
If phenylephrine is used as an active agent, then therapeutic effectiveness is improved for cold, cough, flu, and allergy symptoms, but susceptibility to degradation leading to isoquinoline formation increases
Solution Approach 1:
The patent converts the potential harm of phenylephrine degradation into a benefit by using antioxidants that prevent degradation. The same excipient environment that could cause degradation is modified to become protective, turning a harmful process into a beneficial one.
Solution Approach 2:
The patent introduces antioxidant intermediaries (vitamin C, vitamin E, BHT) that prevent the harmful interaction between phenylephrine and excipients, thereby eliminating isoquinoline degradant formation while preserving therapeutic effectiveness.
4Ease of manufacture
If conventional excipient compositions are used with phenylephrine, then manufacturing simplicity is maintained, but phenylephrine degradation is facilitated
Solution Approach 1:
The patent modifies the compositional parameters of the excipient formulation by eliminating aldehydes and incorporating specific antioxidants, achieving improved stability without significantly complicating the manufacturing process.
Data Source
AI summary
A chewable pharmaceutical composition comprising phenylephrine, artificial sweetener, and a substantially aldehyde-free matrix is provided. The composition has phenylephrine stability suitable for a typical commercial product with a two year shelf life. A method of manufacture of the composition and a method of use are also provided.