| 摘要 |
PROBLEM TO BE SOLVED: To provide 2-[N-(3-amidinophenyl)-N-(3carboxymethyloxybenzyl)amino]- N-[4-[1-(l-iminoethyl)piperidin-4-yl]phenyl]acetamide sulfate dihydrate polymorphic crystal (β-type crystal) which has a strong and selective activated blood coagulation factor X-inhibiting activity and is useful as an agent for preventing or treating thromboembolism. SOLUTION: This polymorphic crystal exhibits strong diffraction peaks at 17.7, 18.9, 19.3, 20.2, 20.7, 21.3 and 25.5 degree at a diffraction angle (2θ±0.1) in a powder X-ray diffraction figure. The polymorphic crystal is produced by adding 2-[N-(3-amidinophenyl)-N-(3-carboxymethyloxybenzyl)amino]-N-[4-[1-(1- iminoethyl)piperidin-4-yl]phenyl]acetamide sulfate dihydrate (α-form crystal) to tetrahydrofuran-water (weight ratio of 1:1 to 3:1, stirring the mixture in a suspension state at >=50 deg.C for >=3 hr, cooling the product and then filtering the cooled mixture to obtain the crystals.
|
