Enhancement of particle properties of cefuroxime sodium by simultaneous control of polymorph and uniform spherulites

Abstract

Cefuroxime Sodium (CS) is a low-toxicity and highly effective antibiotic drug with a wide application market. Its polymorph form β has the advantage of thermal stability and resistance to degradation. However, poor powder properties cause filtration difficulties, severe electrostatic phenomena and difficulties in automated dispensing, which limit its application. In order to improve the powder properties and stability of CS from the source, we used a one-step crystallization method to prepare CS (form β) with high sphericity and uniform particle size. The spherulites of form β of CS (β spherulites) have excellent powder properties, with high flowability (32.8°), good sphericity (90.2%), low C.V. (45.6%), and adjustable particle size distribution. Thanks to improved powder properties, the β spherulites exhibits 40% higher thermal stability and maximum 41% faster dissolution rate in the compatible solutions, compared to commercially available products, which implies the β spherulites is more competitive in powder formulations.