新規抗生物質E1040の固体安定性と製剤化研究について

概要

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In designing the dosage form, one major factor controling their physicochemical properties is solid forms of the drug powder. The method for improving the physicochemical stability of unstable β-lactam antibiotics is very important. E1040 is a novel parenteral 3-betaine type cephalosporin which has a broad antibacterial spectrum and potent activities against Citrobacter, freundii, Enterobacter cloacase, and glucose-nonfermentative bacteria, including P. aeruginosa. The present study was intended to provide the solid-state chemical stability of perenteral steril dry dosage form of E1040. The chemical stability differences among the various solid forms, dry amorphous, additive freeze dried amorphous solid and crystalline powder, were evaluated as a function of temperature by thermo stress tests. Freeze dried anhydrous amorphous form was the first steril dry dosage form investigated during the preformulation study. However, this compound is chemically unstable, in the titer of them, reduction are observed in the freeze dried amorphous solid. In order to select the most suitable solid form of E1040,two methods were used. One was crystalline solid and the other was NaCl additive freezedried formulation. Through our experiments, the solid-state chemical stabilization can be achieved by these two methods (effect of crystal structure and effect of NaCl additive).
社団法人日本薬学会の論文
1990-03-25