Production of Spherical Agglomerates of Cephalosporin Antibiotic Crystals

JOURNAL OF CHEMICAL ENGINEERING OF JAPAN

Keiichi Koga¹  Koji Machiya³  Takashi Mukuta²  Hiroshi Ooshima³  Shigeru Moriki¹  Kooji Kagara¹ 

[1] Chemical Development Laboratories, Fujisawa Pharmaceutical Co., Ltd. (former);Process Chemistry Laboratories, Astellas Pharma Inc.;Department of Applied Chemistry and Bioengineering, Graduate School of Engineering, Osaka City University

关键词: Pharmaceuticals;    Agglomeration;    Spherical Agglomerates;    Crystallization;   

DOI  :  10.1252/jcej.08we178

来源: Maruzen Company Ltd

【 摘 要 】

References(8)A cephalosporin antibiotic, PATC (5-Amino-2-[((6R,7R)-7-{(2Z)-2-(5-amino-1,2,4- thiadiazol-3-yl)-2-[(1-carboxy-1-methylethoxy)imino]acetylamino}-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl)methyl]-1-(2-hydroxyethyl)-1H-pyrazol-2-iumchloride; MW 632.1 Da), was crystallized by neutralization method, and the spherical agglomeration of micro crystals was obtained to develop a drug for injection. The morphology of agglomerates depended on the initial super-saturation ratio and the presence or absence of seed crystals. Spherical agglomerates were obtained by adding seed crystals of 0.1 wt% under a high initial super-saturation ratio of 130. The compactly packed spherical agglomerates were composed of a number of rod-shape crystals with a uniform length of 60 μm, and had good filtration property. The specific volume of spherical agglomerates was 1.75 cm3/g.

【 授权许可】

Unknown