缬沙坦与氢氯噻嗪药物-药物共晶的制备与表征  

Preparation and characterization of drug-drug cocrystal of Valsartan with Hydrochlorothiazide

作　　者：王青青 卢庆梅 张立国[1] 倪力军[1] 栾绍嵘[1] 钱俊红[1] WANG Qingqing;LU Qingmei;ZHANG Liguo;NI Lijun;LUAN Shaorong;QIAN Junhong(Chemistry&Molecular Engineering College,East China University of Science and Technology,Shanghai 200237,China)

机构地区：[1]华东理工大学化学与分子工程学院,上海200237

出　　处：《高校化学工程学报》2025年第1期112-118,共7页Journal of Chemical Engineering of Chinese Universities

摘　　要：为改进难溶性药物缬沙坦与氢氯噻嗪的溶出性能,采用液体辅助研磨法制备了缬沙坦-氢氯噻嗪共晶产物。通过粉末X-射线衍射法、拉曼光谱法、红外光谱法等对共晶产物、缬沙坦、氢氯噻嗪粉末及二者物理混合物进行了系列表征,并采用高效液相色谱方法分析了上述4个样品中药物活性成分(APIs)的体外溶出性能。结果表明,缬沙坦与氢氯噻嗪之间形成了共晶,共晶中APIs的溶出性能较原料药有显著改进,溶出曲线具有协同溶出的趋势。研究结果为缬沙坦与氢氯噻嗪联合用药提供了一种新的选择。Valsartan-hydrochlorothiazide co-crystals were prepared by a liquid-assisted milling method to improve the dissolution performance of the insoluble drugs.Samples of cocrystal,valsartan,hydrochlorothiazide powders and valsartan-hydrochlorothiazide mixtures were characterized by powder X-ray diffraction,Raman spectroscopy,infrared spectroscopy and other methods.The in vitro dissolution properties of Active Pharmaceutical Ingredient(API)in the above four samples were analyzed by high performance liquid chromatography.The results confirm the cocrystal formation of valsartan and hydrochlorothiazide,and show that the dissolution performance of the APIs in the cocrystal is significantly improved when compared with the bulk drugs.The two APIs had a tendency to dissolve synergistically in the cocrystal.The results provide a new option for the co-administration of valsartan and hydrochlorothiazide.

关 键 词：药物-药物共晶 心血管疾病 缬沙坦 氢氯噻嗪 体外累积溶出度 

分 类 号：TQ460.1[化学工程—制药化工]