首页|氢氯噻嗪-氟胞嘧啶共晶的制备、表征及溶解性考察

氢氯噻嗪-氟胞嘧啶共晶的制备、表征及溶解性考察

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为提高氢氯噻嗪(1)的水溶性和改善氟胞嘧啶(2)的引湿性,该文制备了 1-2共晶.应用单晶X射线衍射、粉末X射线衍射、傅里叶变换红外光谱、热重和差示扫描量热等方法对其进行了表征,并研究了 1-2共晶的溶解性和引湿性.结果表明,与1相比,1-2共晶中的1在盐酸(pH 1.2)、磷酸盐缓冲液(pH 6.8)和纯水(pH 7.0)中的平衡溶解度和特性溶出速率均得到提高.并且,1-2共晶在25 ℃和相对湿度95%的条件下未发生增重.研究结果表明所制备的1-2共晶增加了1的溶解性,并减轻了2的引湿性,为提高难溶性药物溶解性的研究提供了参考.
Preparation,Characterization and Solubility Investigation of Hydrochlorothiazide-flucytosine Cocrystal
A cocrystal of hydrochlorothiazide(1)and flucytosine(2)was prepared to improve the solubility of 1 and the hygroscopicity of 2.The 1-2 cocrystal was characterized by single-crystal X-ray diffraction,powder X-ray diffraction,Fourier transform infrared spectroscopy,thermogravimetry,and differential scanning calorimetry.The solubility and hygroscopicity of the 1-2 cocrystal were also examined.Compared with 1,the equilibrium solubility and intrinsic dissolution rate of 1 in the 1-2 cocrystal in hydrochloric acid(pH 1.2),phosphate buffer(pH 6.8),and pure water(pH 7.0)were increased.Meanwhile,the weight of 1-2 cocrystal did not increase under the conditions of 25 ℃ and relative humidity of 95%.These results indicated that the solubility of 1 was increased and the hygroscopicity of 2 was weakened by forming a cocrystal of 1 and 2,which provided a reference for the research on improving the solubility of poorly water-soluble drugs.

hydrochlorothiazideflucytosinecocrystalsolubilityhygroscopicity

邓雪珍、陈乐乐、谭雨梦、钱坤、杨婕

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江西中医药大学药学院,江西南昌 330004

氢氯噻嗪 氟胞嘧啶 共晶 溶解性 引湿性

国家自然科学基金江西省研究生创新专项(2022)中药炮制技术的传承与创新项目

22165014YC2022-s856CXTD22003

2024

中国医药工业杂志
上海医药工业研究院,中国化学制药工业协会

中国医药工业杂志

CSTPCD
影响因子:0.487
ISSN:1001-8255
年,卷(期):2024.55(1)
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