公开(公告)号：EP0533149A1

公开(公告)日：1993-03-24

申请号：EP92115869.7

申请日：1992-09-17

申请人： TAKEDA CHEMICAL INDUSTRIES, LTD. ,  LEDERLE (JAPAN), Ltd.

发明人： Kaneko, Masayoshi ,  Yabuno, Shigeo

IPC分类号： C07D477/00 ,  A61K31/40

CPC分类号： C07D477/20

摘要： A method of crystallizing (1R,5S,6S)-2-[(6,7-dihydro-5H-pyrazolo[1,2-a][1,2,4]triazolium-6-yl)]thio-6-[(R)-1-hydroxyethyl]-1-methyl-carbapenem-3-carboxylate (hereinafter simply referred to as L-627), which is characterized by maintaining an aqueous solution of L-627 at temperatures ranging from the eutectic temperature of the solution to temperatures lower than 0° C.
The method provides some advantages that loss of L-627 accompanied by crystallization is less, number of steps in the preparation of vial formulations is less and maintenance of these steps under sterile and dust-free conditions can be performed easily, dispensation of the drug can be conducted with quantitative accuracy, and the crystals dissolve in a solvent promptly at the time of use.

摘要翻译： （1R，5S，6S）-2 - [（6,7-二氢-5H-吡唑并[1,2-a] [1,2,4]三唑鎓-6-基）] - - [（R）-1-羟乙基] -1-甲基 - 碳青霉烯-3-羧酸酯（以下简称为L-627），其特征在于将L-627的水溶液保持在共晶温度 的溶液温度低于0℃。该方法提供了一些优点，即伴随结晶的L-627的损失较少，制备小瓶配方的步骤数量较少，并且在无菌和无粉尘下维持这些步骤 条件可以容易地进行，可以定量精确地进行药物的分配，并且晶体在使用时迅速溶解在溶剂中。