Method for producing crystals of diazabicyclooctane derivative and stable lyophilized preparation

• Main Authors: OGAWA TAKAYA, ICHIKI MASATO, YOKOYAMA TAKUYA, FURUYAMA SHUSUKE, FUSHIHARA KENICHI
• Format: Patent
• Language: Chinese; English
• Published: 01.08.2017
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The purpose of the present invention is to provide a method with which it is possible to easily produce crystals of compound (I) on an industrial scale, and to provide a stable lyophilized composition of said compound (I). It was discovered that a lyophilized composition having exceptional storage stability and in which compound (I) is in crystalline form can be obtained by lyophilizing an aqueous solution that contains said compound (I) and an inorganic salt such as sodium chloride, and that crystals of said compound (I) can be obtained from said aqueous solution even without lyophilization. 本发明的目的是提供可以以工业规模简便地制备化合物(I)的结晶的方法，以及化合物(I)的稳定的冻干组合物。发现了通过将含有化合物(I)和氯化钠等的无机盐的水溶液冻干，得到化合物(I)为结晶的保存稳定性良好的冻干组合物，此外，即使不进行冻干，也可以从该水溶液中得到化合物(I)的结晶。