title: Physicochemical and crystal structure analysis of pranlukast pseudo-polymorphs I: anhydrates and hydrate.
abstract: Pranlukast (PRS) is a leukotriene receptor antagonist for the treatment of bronchial asthma. Pranlukast is formulated as a hemihydrate (HH) form in the drug product. Here, we report three new anhydrate forms of PRS (AH, form I-III). These polymorphs and PRS HH were characterized by PXRD, TG-DTA, simultaneous PXRD-DSC and vapor sorption analysis. In addition, the crystal structures of HH and AH-I were determined by single crystal X-ray structure analysis for the first time. HH transformed to AH-I, AH-II and AH-III as the temperature was increased from 25°C to 210°C. At 25°C, AH-I transformed to HH at above 5%RH. HH and AH-I possessed similar crystal packing patterns and molecular structures.
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1, Miyama, Funabashi, Chiba 274-8510, Japan.
authors.forename: Hideaki
authors.initials: H
authors.lastname: Furuta
authors.affiliation: Graduate School of Science and Engineering, Department of Chemistry and Materials Science, Tokyo Institute of Technology, 12-1-H62, Ookayama 2, Meguro-ku, Tokyo 152-8551, Japan.
authors.forename: Shintaro
authors.initials: S
authors.lastname: Mori
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1, Miyama, Funabashi, Chiba 274-8510, Japan.
authors.forename: Yasuo
authors.initials: Y
authors.lastname: Yoshihashi
authors.affiliation: School of Pharmacy and Pharmaceutical Sciences, Hoshi University, 2-4-41, Ebara, Shinagawa, Tokyo 142-8501, Japan.
authors.forename: Etsuo
authors.initials: E
authors.lastname: Yonemochi
authors.affiliation: Graduate School of Science and Engineering, Department of Chemistry and Materials Science, Tokyo Institute of Technology, 12-1-H62, Ookayama 2, Meguro-ku, Tokyo 152-8551, Japan.
authors.forename: Hidehiro
authors.initials: H
authors.lastname: Uekusa
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1, Miyama, Funabashi, Chiba 274-8510, Japan. Electronic address: kiyohiko.sugano@phar.toho-u.ac.jp.
authors.forename: Kiyohiko
authors.initials: K
authors.lastname: Sugano
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1, Miyama, Funabashi, Chiba 274-8510, Japan.
authors.forename: Katsuhide
authors.initials: K
authors.lastname: Terada
mesh_terms: D002152:Calorimetry, Differential Scanning; D002867:Chromones / Q000737:chemistry*; D003460:Crystallization / Q000379:methods; D020024:Leukotriene Antagonists / Q000737:chemistry*; D015394:Molecular Structure; D013696:Temperature; D013818:Thermogravimetry / Q000379:methods; D014867:Water / Q000737:chemistry; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D002867:Chromones; D020024:Leukotriene Antagonists; D014867:Water; C047681:pranlukast
keywords: Anhydrate; Crystal structure; Hydrate; Pranlukast; Pseudo-polymorph