Patil S S, Patil A L
Ashokrao Mane College of Pharmacy, Karad Maharashtra, India.
Pharmazie. 2011 Jun;66(6):416-20.
The solid state properties and dissolution behaviour of binary systems of mefloquine hydrochloride (MH) with betaCD were investigated. MH-betaCD interaction in the solution state was studied by phase solubility analysis and demonstrates the ability of 3CD to complex with MH giving AL type profile with 120.34 M-1 stability constant. The kneading method was adopted to prepare binary sytems of MH with betaCD in 1:1 molar ratio. The solid inclusion was characterized by differential scanning calorimetry, fourier transformation infrared spectroscopy and X-ray powder diffractometry. Experimental results confirmed the existence of 1:1 inclusion complex of MH with ICD. Aqueous solubility of MH was found to be enhanced by 118% for inclusion complex. The dissolution properties of binary systems were studied in simulated gastric fluid without enzyme and compared with MH alone. The inclusion complex of MH prepared with 3CD showed a dissolution rate several times faster than that of physical mixture and pure drug.
研究了盐酸甲氟喹（MH）与β-环糊精（βCD）二元体系的固态性质和溶解行为。通过相溶解度分析研究了溶液状态下MH与βCD的相互作用，结果表明βCD能够与MH形成络合物，给出AL型曲线，稳定常数为120.34 M-1。采用捏合方法制备了MH与βCD摩尔比为1:1的二元体系。通过差示扫描量热法、傅里叶变换红外光谱法和X射线粉末衍射法对固体包合物进行了表征。实验结果证实了MH与βCD存在1:1包合物。发现包合物使MH的水溶性提高了118%。在无酶模拟胃液中研究了二元体系药物的溶出性能，并与单独的MH进行了比较。用βCD制备的MH包合物的溶出速率比物理混合物和纯药物快几倍。
