Crystal form of cephradine

Area of Science:

• Pharmaceutical Sciences
• Solid-State Chemistry

Background:

• Cephradine is a widely used cephalosporin antibiotic.
• Understanding the solid-state properties of drug substances is crucial for formulation development and bioavailability.

Purpose of the Study:

• To isolate and characterize different crystalline forms of cephradine.
• To evaluate the dissolution profiles and solid-state stability of these cephradine crystal forms.

Main Methods:

• Recrystallization was employed to obtain four distinct crystal forms of cephradine.
• Characterization involved powder X-ray diffractometry, differential scanning calorimetry, and thermogravimetric analysis.
• Dissolution studies were conducted in water at 37°C, and stability was assessed under various relative humidity conditions.

Main Results:

• Four crystal forms of cephradine were successfully isolated and characterized.
• Dissolution rates varied significantly, with Form I dissolving completely (100%) within 120 minutes, followed by Form 3 (98.9%), Form 4 (77.83%), and Form 2 (75.55%).
• No polymorphic transformations were observed in any of the crystal forms after two months of storage under different humidity levels (0%, 52%, and 95% RH).

Conclusions:

• Cephradine exhibits polymorphism, with different crystal forms possessing distinct dissolution characteristics.
• Form I demonstrates superior dissolution properties compared to other identified forms.
• The crystal forms of cephradine are stable and do not undergo transformation under the tested storage conditions, suggesting good solid-state stability for pharmaceutical applications.