Bupropion-Cysteine Compositions with Controlled-Release Polymers
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Solution Overview
Problem
Bupropion is unstable in the presence of common excipients, leading to potential degradation and reduced efficacy in pharmaceutical compositions.
Innovation Solution
Formulating bupropion with cysteine in a molecular complex at specific molar ratios, which stabilizes bupropion and enhances its stability in the presence of excipients, and incorporating controlled release polymers and other additives to create stable pharmaceutical compositions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If bupropion is formulated with common excipients, then the pharmaceutical composition can be manufactured and administered, but bupropion degrades and loses efficacy
Solution Approach 1:
The patent introduces a stabilizing agent as an intermediary substance that mediates between bupropion and common excipients. This stabilizing agent prevents direct harmful interactions between bupropion and excipients, thereby maintaining bupropion stability while allowing the use of standard pharmaceutical excipients for manufacturability.
Solution Approach 2:
The patent creates a composite pharmaceutical composition that combines bupropion with stabilizing agents and specific excipients in controlled ratios. This composite formulation maintains the therapeutic benefits of bupropion while incorporating stabilizing components that prevent degradation, resolving the contradiction between manufacturability and stability.
2Device complexity
If bupropion is used alone in pharmaceutical compositions, then the formulation is simple, but bupropion stability is reduced leading to degradation
Solution Approach 1:
The patent merges bupropion with stabilizing agents in a single pharmaceutical composition. This combination approach integrates multiple functional components (active ingredient + stabilizer) into one formulation, maintaining relative simplicity while significantly improving bupropion stability compared to using bupropion alone.
3Reliability
If bupropion is stabilized using additional substances, then bupropion stability is enhanced, but the pharmaceutical composition becomes more complex
Solution Approach 1:
The patent optimizes the concentrations and ratios of stabilizing agents and excipients to achieve effective bupropion stability with minimal formulation complexity. By carefully controlling parameters such as the amount of stabilizing agent (e.g., 0.1-10% w/w) and using standard pharmaceutical excipients, the formulation achieves stability enhancement without excessive complexity.
Data Source
AI summary
This disclosure relates to pharmaceutical compositions comprising bupropion and cysteine, and pharmaceutical dosage forms comprising bupropion and cysteine. The disclosure also relates to molecular complexes of bupropion and cysteine. These compositions and dosage forms may have improved stability of bupropion.
