Design, evaluation and optimization of taste masked clarithromycin powder

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Clarithromycin (CLA), a macrolide antibiotic, possesses an extremely bitter taste, negatively impacting patient adherence and therapeutic outcomes.
• Taste masking is crucial for improving the palatability of bitter drugs like CLA, especially in pediatric populations.

Purpose of the Study:

• To develop and optimize a taste-masked clarithromycin resinate using a weak acidic cation exchange resin, Indion® 234.
• To characterize the formed CLA-resin complex and evaluate its taste-masking efficacy and drug release profile.

Main Methods:

• Utilized design of experiments to optimize CLA-resin complex formation, assessing variables like temperature, CLA-resin ratio, stirring time, and pH.
• Employed spectrophotometry for CLA loading efficiency and release studies (USP Apparatus II).
• Confirmed complex formation using DSC, SEM, FT-IR, and XRD; taste evaluation performed spectrophotometrically.

Main Results:

• Optimized conditions for CLA-resin complex formation were identified: 1:4 CLA-resin ratio, 80°C, 3 hours stirring time, at pH 8.
• Characterization confirmed CLA was crystalline, while the complex was amorphous; FT-IR indicated the absence of the bitter tertiary amine functional group.
• All developed resinate batches demonstrated complete taste masking, with CLA stable in simulated salivary fluid and released within 3 hours in gastric fluid.

Conclusions:

• The developed Indion® 234-based CLA resinate effectively masks the bitter taste of clarithromycin, enhancing its palatability.
• Optimized formulation and characterization confirmed the successful formation of an amorphous CLA-resin complex with improved taste-masking properties.
• This taste-masked formulation holds significant potential for improving patient compliance in clarithromycin therapy.