Bupropion-Cysteine Molecular Complex for Excipient Stability
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Solution Overview
Problem
Bupropion is prone to instability in the presence of common excipients, leading to potential degradation and reduced efficacy in pharmaceutical formulations.
Innovation Solution
Formulating bupropion with cysteine in a molecular complex, with a molar ratio of about 0.9:1 to about 1.1:1, stabilizes the drug and enhances its stability in the presence of excipients such as calcium phosphate and methylcellulose.
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 the bupropion becomes unstable and degrades
Solution Approach 1:
Cysteine is introduced as an intermediary substance that mediates between bupropion and common excipients. The cysteine forms a molecular complex with bupropion, acting as a protective barrier that prevents direct interaction between bupropion and degrading excipients, thereby maintaining stability while allowing formulation with standard pharmaceutical excipients
Solution Approach 2:
The invention creates a composite molecular complex consisting of bupropion and cysteine. This composite structure combines the therapeutic properties of bupropion with the stabilizing properties of cysteine, resulting in a formulation that maintains both manufacturability and enhanced stability
2Stability of the object's composition
If bupropion is stabilized using cysteine in a molecular complex, then the stability and efficacy are enhanced, but the formulation complexity increases
Solution Approach 1:
The invention optimizes specific parameters including the molar ratio of bupropion to cysteine (approximately 1:1) and the molecular complex structure. By controlling these parameters, the formulation achieves enhanced stability without requiring complex manufacturing processes or additional excipients, maintaining relative formulation simplicity
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.