Kommavarapu Pavan, Maruthapillai Arthanareeswari, Palanisamy Kamaraj, Koya Ravi Teja
Department of Chemistry, SRM University, Kattankulathur, India.
Department of Pharmaceutical analysis, Acharya Nagarjuna University, Guntur, India.
Pak J Pharm Sci. 2016 Nov;29(6):2023-2031.
The aim of the current exertion was to prepare Solid Dispersion of Etravirine by Spray drying technique to enhance aqueous solubility and dissolution rate. Solid dispersions (SD) of Etravirine were prepared using Copovidone and Povidone-Copovidone in dichloromethane and physical properties were characterized by Scanning electron microscopy (SEM), X-Ray diffractometry (PXRD), Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC). SD's were evaluated for equilibrium solubility and in vitro drug release profile by dissolution testing. The diffraction and thermal patterns of solid dispersions indicated the conversion of crystalline Etravirine to amorphous form. The solubility of drug in SD's was appreciably more when evaluated against physical mixtures and intact Etravirine. Drug release characteristics were evaluated in three different media at different pH and found that drug release kinetic was best described by weibull mathematical model. Mean dissolution time (MDT) and Dissolution efficiency (DE %) in different media were evaluated for SDs. Statistical evaluation of dissolution data using Analysis Of Variance (ANOVA) single factor and t-Test: Paired Two Sample for Means was applied for better understanding and evaluation.
当前研究的目的是通过喷雾干燥技术制备依曲韦林固体分散体,以提高其水溶性和溶解速率。采用共聚维酮和聚维酮 - 共聚维酮在二氯甲烷中制备依曲韦林固体分散体,并通过扫描电子显微镜(SEM)、X射线衍射仪(PXRD)、傅里叶变换红外光谱仪(FTIR)、差示扫描量热法(DSC)对其物理性质进行表征。通过溶出度测试评估固体分散体的平衡溶解度和体外药物释放曲线。固体分散体的衍射和热图谱表明结晶态依曲韦林转变为无定形形式。与物理混合物和完整的依曲韦林相比,药物在固体分散体中的溶解度明显更高。在三种不同pH值的不同介质中评估药物释放特性,发现药物释放动力学最适合用威布尔数学模型描述。对固体分散体在不同介质中的平均溶出时间(MDT)和溶出效率(DE%)进行了评估。使用方差分析(ANOVA)单因素和t检验:均值的成对双样本对溶出数据进行统计评估,以更好地理解和评估。