Enantiomerically Pure S-Bupropion Dosage Forms for Reduced Dosing
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Solution Overview
Problem
Current bupropion treatments often require higher doses of racemic bupropion to achieve desired pharmacokinetic and therapeutic effects, which can lead to increased adverse events and inefficiencies.
Innovation Solution
Development of dosage forms containing enantiomerically pure or enriched (S)-bupropion, allowing for reduced dosages while maintaining equivalent pharmacokinetic profiles and therapeutic effects by administering 95% or higher enantiomerically pure (S)-bupropion, either alone or in combination with other drugs, to achieve the same outcomes as racemic bupropion.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If racemic bupropion is administered to achieve desired pharmacokinetic effects, then therapeutic effect is achieved, but higher doses are required leading to increased adverse events
Solution Approach 1:
The patent extracts and isolates the therapeutically active (S)-enantiomer from the racemic mixture of bupropion. By administering only the active (S)-enantiomer instead of the racemic mixture containing both (R) and (S) enantiomers, the therapeutic effect is maintained while the inactive or potentially harmful (R)-enantiomer is eliminated, thereby reducing the required dose and associated adverse events
Solution Approach 2:
The patent applies local quality by providing enantiomerically enriched or pure (S)-bupropion dosage forms with specific optical purity (at least 95% enantiomeric excess). This localized purification at the molecular level ensures that only the therapeutically beneficial enantiomer is present in the dosage form, optimizing therapeutic effect while minimizing adverse events associated with the racemic mixture
2Reliability
If racemic bupropion is administered to achieve desired pharmacokinetic effects, then therapeutic effect is achieved, but higher doses are required
Solution Approach 1:
The patent extracts and isolates the therapeutically active (S)-enantiomer from the racemic mixture of bupropion. By administering only the active (S)-enantiomer instead of the racemic mixture containing both (R) and (S) enantiomers, the therapeutic effect is maintained while the inactive or potentially harmful (R)-enantiomer is eliminated, thereby reducing the required dose and associated adverse events
Solution Approach 2:
The patent changes the optical purity parameter of the bupropion dosage form from a racemic mixture (50:50 ratio of R and S enantiomers) to enantiomerically enriched or pure (S)-bupropion (at least 95% enantiomeric excess). This parameter change in optical purity directly impacts the dose requirement, allowing for lower doses to achieve the same pharmacokinetic and therapeutic effects
Data Source
AI summary
This disclosure relates to dosage forms containing an enantiomerically enriched or pure bupropion such as enantiomeric excess of (S)-bupropion, enantiomerically enriched (S)-bupropion, or enantiomerically pure (S)-bupropion and methods of using these dosage forms. These dosage forms may be administered to human beings in a reduced amount as compared to the amount of racemic bupropion that would be administered in the same situation.