Bupropion Microparticle Formulation With 50–100 μm Size Control
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Solution Overview
Problem
The particle size of bupropion microparticles affects their dissolution profile and pharmacokinetics, which can impact their therapeutic efficacy.
Innovation Solution
Formulating bupropion microparticles with a controlled particle size distribution, specifically between 50 μm to 100 μm, and incorporating a stabilizer like cysteine, along with controlled release polymers such as Carbopol 971P, to enhance stability and release profile.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If bupropion microparticles are formulated with controlled particle size distribution (50 μm to 100 μm), then dissolution profile and pharmacokinetics are improved, but manufacturing precision requirements increase
Solution Approach 1:
The patent applies parameter changes by controlling the particle size of bupropion microparticles within a specific range (50 μm to 100 μm). This parameter optimization directly improves the dissolution profile and pharmacokinetics of bupropion, resolving the technical contradiction between reliability and manufacturing precision by establishing clear parameter specifications that guide manufacturing processes.
Solution Approach 2:
The patent employs preliminary action through the use of stabilizers (such as cysteine) and controlled release polymers (such as Carbopol 971P) that are incorporated into the microparticle formulation before administration. These additives pre-establish stability and controlled release characteristics, ensuring consistent dissolution profiles while reducing the burden on manufacturing precision during the formulation process.
2Stability of the object's composition
If stabilizers and controlled release polymers are incorporated into the formulation, then stability and release profile are enhanced, but device complexity increases
Solution Approach 1:
The patent applies composite materials by combining bupropion with stabilizers (e.g., cysteine) and controlled release polymers (e.g., Carbopol 971P) to create a composite microparticle formulation. This composite approach enhances formulation stability and achieves controlled release profiles while managing complexity through the synergistic interaction of selected components rather than multiple separate systems.
Solution Approach 2:
The patent employs universality by selecting polymers like Carbopol 971P that serve multiple functions: they act as stabilizers, provide controlled release characteristics, and maintain formulation integrity. This multi-functionality reduces the need for multiple separate additives, thereby enhancing stability while limiting the increase in formulation complexity.
Data Source
AI summary
This disclosure relates to microparticles containing bupropion, e.g., microparticles having a particle diameter of about 50 μm to about 100 μm. These microparticles may be included in pharmaceutical compositions and/or dosage forms for treatment of various disease, such as depression.