首页|法莫替丁-对甲苯磺酸共晶的制备表征及性质研究

法莫替丁-对甲苯磺酸共晶的制备表征及性质研究

Synthesis,Characterization and Physicochemical Properties of an Famotidine and P-toluenesulfonic Acid Cocrystal

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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-H2O(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,将有助干低渗透性药物的开发.
OBJECTIVE To synthesize p-toluenesulfonic acid(PTS)and famotidine(FMT)cocrystal in order to improve thesolu-bility 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-H2 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)Ⅲ drugs,which will contribute to the development of low permeability drugs.

famotidinep-toluenesulfoniccrystal structureaqueous solubilitypermeability

赵永凤、范莹、张燕、徐红、李敏、杨钊

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青岛大学药学院,山东青岛 266071

海军青岛特勤疗养中心药剂科,山东青岛 266071

青岛食品药品检验研究院,山东青岛 266071

山东科技大学,山东青岛 266590

安丘市人民医院,山东潍坊 262199

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法莫替丁 对甲苯磺酸 晶体结构 水溶性 渗透性

2024

中国药学杂志
中国药学会

中国药学杂志

CSTPCD北大核心
影响因子:0.957
ISSN:1001-2494
年,卷(期):2024.59(3)
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