Design, development, and characterization of amorphous rosuvastatin calcium tablets

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Rosuvastatin calcium is a BCS class II drug with poor solubility, necessitating formulation strategies to improve bioavailability.
• Amorphous forms often exhibit enhanced dissolution compared to crystalline counterparts.

Purpose of the Study:

• To design, develop, optimize, and evaluate amorphous rosuvastatin calcium tablets.
• To achieve rapid disintegration and high dissolution rates for enhanced bioavailability.
• To utilize the SeDeM methodology for direct compression tablet manufacturing.

Main Methods:

• Formulation design with careful excipient selection and proportioning.
• Characterization using SEM, DSC, TGA, FT-IR, and PXRD.
• Application of the SeDeM methodology for galenic profiling and direct compression suitability assessment.

Main Results:

• Optimized amorphous rosuvastatin calcium tablets were successfully produced via direct compression.
• The formulation exhibited excellent pharmacotechnical properties, including rapid disintegration and dissolution.
• Manufactured tablets met all pharmacopoeial standards for quality attributes.

Conclusions:

• The developed methodology enables cost-effective production of amorphous rosuvastatin calcium tablets with superior dissolution profiles.
• Direct compression is a viable method for manufacturing these tablets with enhanced bioavailability.
• The study provides a robust approach for formulating poorly soluble drugs like rosuvastatin calcium.