Lyophilized composition of a diazabicyclooctane compound and process of producing the same
Inventors
Ogawa, Takaya • Yokoyama, Takuya • FURUYAMA, Shusuke • ICHIKI, Masato • Fushihara, Kenichi
Assignees
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Publication Number
US-10294224-B2
Publication Date
2019-05-21
Expiration Date
Abstract
A process for producing crystals of a compound represented by the following formula (I): by crystallizing the compound from an aqueous solution containing the compound and an inorganic salt, such as sodium chloride. Such crystals can be subjected to lyophilization to provide a lyophilized composition having a desirable storage stability.
Core Innovation
The invention is directed to producing a crystalline diazabicyclooctane compound represented by formula (I), especially crystalline form I, by crystallization from an aqueous solution. The aqueous solution contains the compound and a salt, and the resulting crystals are crystalline form I identified by powder X-ray diffraction characteristic peaks with specified lattice spacing (d) values. The process includes subjecting the aqueous solution to lyophilization to obtain a lyophilized composition containing crystals of crystalline form I.
A key aspect is that crystals of crystalline form I are obtained by crystallizing the compound from the salt-containing aqueous solution prior to lyophilization, including cases where the salt is sodium chloride. The document emphasizes improved storage stability for the lyophilized composition containing crystalline form I relative to amorphous lyophilized material. Powder X-ray diffraction characterization is used to distinguish crystalline form I from amorphous outcomes.
The document describes producing a lyophilized composition by lyophilizing the salt-containing aqueous solution, and it emphasizes that crystalline form I and improved storage stability are obtained without necessarily performing heat treatment/refreezing between freezing and drying. Comparative outcomes are described where omitting the salt leads to amorphous results, whereas including the salt enables formation of crystalline form I.
Claims Coverage
Two independent claims are identified, covering a process for producing a lyophilized composition with crystalline form I defined by powder X-ray diffraction peak lattice spacings and the resulting lyophilized composition comprising crystalline form I crystals and a selected salt. Across the independent claims, the main inventive features are salt-containing aqueous crystallization followed by lyophilization, and crystalline form I defined by characteristic powder X-ray diffraction peak lattice spacing (d) values.
Salt-containing aqueous crystallization followed by lyophilization
Crystallizing a compound of formula (I) by subjecting an aqueous solution containing the compound and a salt to lyophilization.
Crystalline form I defined by powder X-ray diffraction lattice spacings
Obtaining crystals of the compound of formula (I) as crystalline form I having characteristic peaks appearing at specified lattice spacing (d) values in a powder X-ray diffraction pattern.
Lyophilized composition with crystalline form I crystals and selected salt
A lyophilized composition comprising crystals of the compound of formula (I) and a salt selected from the specified group.
Crystalline form I definition in the lyophilized composition
The lyophilized composition is characterized in that the crystals are crystalline form I having characteristic peaks appearing at the specified lattice spacing (d) values in a powder X-ray diffraction pattern.
The independent claims collectively require a lyophilized composition containing crystalline form I crystals of compound (I), where crystalline form I is defined by specified powder X-ray diffraction lattice spacings, and where crystallization and formation are carried out using an aqueous solution containing the compound and a selected salt from the listed group.
Stated Advantages
Improved storage stability of the lyophilized composition containing crystalline form I versus amorphous lyophilized material.
Crystalline form I formation is achieved by using the salt-containing aqueous solution during crystallization and lyophilization.
Documented Applications
The salt is selected from inorganic salts amenable to be added to a parenteral injection, and the compositions and processes are presented in that context.
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