重庆润泽医药有限公司;CHONGQING RUZER PHARMACEUTICAL COMPANY LIMITED.
发明人:
YE, Lei,叶雷
申请号：
CNCN2017/118180
公开号：
WO2018/130063A1
申请日:
2017.12.25
申请国别(地区):
CN
年份:
2018
代理人:
摘要：
The present invention provides an (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form, which has diffraction peaks when 2θ is 12.423±0.2°, 16.465±0.2°, 17.344±0.2°, 21.889±0.2°, and 25.054±0.2°. The present invention can promote synthesis of phosphorylcholine and phosphoethanolamine and promote cerebral metabolism, has a stimulating effect on the specific central nervous pathway through the blood-brain barrier, and has special biological activity in the fields of sedation, anti-epilepsy, etc. The (R)-4-hydroxy-2-oxo-1-pyrrolidineacetamide crystal form in the present invention has a melting point peak temperature of 133.1±2°C and a solubility in water of greater than or equal to 100 mg/mL, dissolves fast in water, provides high bioavailability, good stability, and good particle fluidity, is suitable for production of pharmaceutical preparations and storage and transportation. The crystal form is suitable for preparation into a variety of pharmaceutical compositions, and can be prepared into a variety of preparations, such as tablets, capsules, dripping pills, sustained-release controlled-release preparations, freeze-dried powder injections, etc. The preparation method of the present invention is simple and suitable for industrial production.La présente invention concerne une forme cristalline de (R)-4-hydroxy-2-oxo-1-pyrrolidineacétamide, présentant des pics de diffraction lorsque 2θ est 12,423±0,2°, 16,465±0,2°, 17,344±0,2°, 21,889±0,2° et 25,054±0,2°. La présente invention peut favoriser la synthèse de phosphorylcholine et de phosphoéthanolamine et peut développer le métabolisme cérébral, présente un effet stimulant sur le trajet nerveux central spécifique à travers la barrière hémato-encéphalique, et possède une activité biologique spéciale dans les domaines de la sédation, de l'épilepsie, etc. La forme cristalline de (R)-4-hydroxy-2-oxo-1-pyrrolidineacétamide de la présente invention a une température de pic de point de fusion de 133,1 ± 2 °C et une solubilit
