title: Physicochemical and crystal structure analysis of pranlukast pseudo-polymorphs II: Solvate and cocrystal.
abstract: Pranlukast (PRS) is a leukotriene receptor antagonist for the treatment of bronchial asthma. In this study, six new solvates and one new cocrystal of PRS were characterized by PXRD, TG-DTA, DSC, vapor sorption analysis and the dissolution test. In addition, the crystal structures were determined by single crystal X-ray structure analysis. PRS was found to be a rare example of a promiscuous multicomponent crystal former. The crystal packing patterns of these crystals can be categorized into the sheet-like and channel-like patterns. The ethanol solvate (PRS/ethanol) and urea cocrystal (PRS/urea) were more stable than the others under humid conditions. PRS/ethanol showed an improved dissolution profile compared to PRS HH and PRS/urea.
authors: Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1, Miyama, Funabashi, Chiba 274-8510, Japan.
authors: Hideaki
authors: H
authors: Furuta
authors: 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: Shintaro
authors: S
authors: Mori
authors: Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1, Miyama, Funabashi, Chiba 274-8510, Japan.
authors: Yasuo
authors: Y
authors: Yoshihashi
authors: School of Pharmacy and Pharmaceutical Sciences, Hoshi University, 2-4-41, Ebara, Shinagawa, Tokyo 142-8501, Japan.
authors: Etsuo
authors: E
authors: Yonemochi
authors: 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: Hidehiro
authors: H
authors: Uekusa
authors: 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: Kiyohiko
authors: K
authors: Sugano
authors: Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Toho University, 2-2-1, Miyama, Funabashi, Chiba 274-8510, Japan.
authors: Katsuhide
authors: K
authors: Terada
mesh_terms: D002867:Chromones / Q000737:chemistry*; D003460:Crystallization / Q000379:methods; D000431:Ethanol / Q000737:chemistry; D020024:Leukotriene Antagonists / Q000737:chemistry*; D012995:Solubility; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D002867:Chromones; D020024:Leukotriene Antagonists; D000431:Ethanol; C047681:pranlukast
keywords: Crystal structure; Dissolution; Pranlukast; Pseudo-polymorph; Vapor sorption