摘要
目的 为了提高法莫替丁在水中的溶解度及其渗透性,采用药物共结晶技术,以对甲苯磺酸(PTS)和法莫替丁(FMT)为原料合成了药物共晶。方法 利用结合超声的溶剂挥发法制备共晶,通过扫描电镜、差示扫描量热法、热重分析、红外光谱和粉末x射线衍射对共晶进行了表征。应用X射线单晶衍成功获得了FMT-PTS-H_(2)O(1∶1∶1)的单晶结构,对新合成的共晶的溶解度和渗透性进行了研究。结果 形成共晶后,FMT的水溶性和渗透性分别提高了1.54和2.29倍。结论 与FMT原料药相比,形成共晶后的FMT溶解度和渗透性都有所提高。本研究为提高生物药剂学分类系统(BCS)Ⅲ类药物的渗透性提供了一种方法,将有助于低渗透性药物的开发。
OBJECTIVE To synthesize p-toluenesulfonic acid(PTS)and famotidine(FMT)cocrystal in order to improve thesolubility of famotidine in water and the permeability.METHODS The cocrystal was prepared by solvent evaporation method combined with ultrasound.The cocrystal was characterized by scanning electron microscopy,differential scanning calorimetry,thermogravimetric analysis,infrared spectroscopy and powder X-ray diffraction.The single crystal structure of FMT-PTS-H_(2)O(1∶1∶1)was successfully obtained,and the solubility and permeability of the newly synthesized cocrystal were studied.RESULTS After the formation of cocrystal,the water solubility and permeability of FMT increased by 1.54 and 2.29 times,respectively.CONCLUSION Compared with FMT,the solubility and permeability of FMT after the formation of cocrystal were improved.This study provides a method for improving the permeability of biopharmaceutics classification system(BCS)Ⅲdrugs,which will contribute to the development of low permeability drugs.
作者
赵永凤
范莹
张燕
徐红
李敏
杨钊
ZHAO Yongfeng;FAN Ying;ZHANG Yan;XU Hong;LI Min;YANG Zhao(College of Pharmacy,Qingdao University,Qingdao 266071,China;Pharmacy Department,Qingdao Special Servicemen Recuperation Center of CPLA Navy,Qingdao 266071,China;Qingdao Institute for Food and Drug Control,Qingdao 266071,China;Shandong University of Science and Technology,Qingdao 266590,China;Anqiu People′s Hospital,Weifang,262199,China)
出处
《中国药学杂志》
CAS
CSCD
北大核心
2024年第3期263-269,共7页
Chinese Pharmaceutical Journal
关键词
法莫替丁
对甲苯磺酸
晶体结构
水溶性
渗透性
famotidine
p-toluenesulfonic
crystal structure
aqueous solubility
permeability
