Bupropion Hydrobromide Modified Release Tablets
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Solution Overview
Problem
Current bupropion hydrochloride formulations have stability issues, leading to rapid drug release and increased risk of seizures, and there is a need for a more stable once-daily formulation to improve patient compliance and reduce side effects.
Innovation Solution
Development of bupropion hydrobromide dosage forms that exhibit enhanced stability compared to bupropion hydrochloride, with a controlled release matrix tablet formulation and SMARTCOAT technology to prevent dose dumping, allowing for a once-daily administration without significant food effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If bupropion hydrochloride is used in immediate release formulation, then rapid drug release is achieved, but stability issues occur and seizure risk increases
Solution Approach 1:
The patent changes the salt form parameter from hydrochloride to hydrobromide, which fundamentally alters the stability profile. Bupropion hydrobromide demonstrates superior stability compared to hydrochloride, resolving the stability issues while maintaining rapid release characteristics when needed
Solution Approach 2:
The patent divides the release profile into controlled segments through matrix tablet formulation with specific polymers (hydroxypropyl methylcellulose, carboxymethyl cellulose, and polyvinyl alcohol). This segmentation allows controlled release rates while maintaining formulation stability, preventing the harmful effects of uncontrolled rapid release
2Reliability
If multiple dosing is required to manage side effects, then seizure risk is reduced, but patient compliance deteriorates
Solution Approach 1:
The patent implements continuous release action through sustained release matrix tablets that provide consistent bupropion delivery over extended periods. This continuous action maintains therapeutic levels without peaks that cause seizures, while the once-daily dosing frequency dramatically improves patient compliance through continuous rather than intermittent administration
Solution Approach 2:
The patent changes the release rate parameter through controlled release formulation technology. By adjusting polymer ratios and matrix composition, the release rate is optimized to provide steady plasma levels that prevent seizures while allowing once-daily dosing that improves compliance
3Loss of time
If sustained release formulation is used, then dosing frequency is reduced, but release control precision must be maintained
Solution Approach 1:
The patent uses composite matrix materials combining hydroxypropyl methylcellulose, carboxymethyl cellulose, and polyvinyl alcohol in specific ratios. This composite approach provides both sustained release capability and precise control over the release rate, achieving once-daily dosing while maintaining manufacturing precision through the synergistic properties of the polymer combination
Solution Approach 2:
The patent applies different polymer formulations to different regions of the matrix tablet to create zones with specific release characteristics. This local quality approach allows precise control over release rates while maintaining overall sustained release performance, enabling once-daily dosing without sacrificing precision
Data Source
AI summary
The present invention relates to pharmaceutical compositions, formulations and medicaments comprising a bupropion salt, in particular, modified-release tablets comprising an effective amount of bupropion hydrobromide, and the use of the bupropion salt to prepare a medicament to treat a condition.