Akram Aasma, Irfan Muhammad, Abualsunun Walaa A, Bukhary Deena M, Alissa Mohammed
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad 38000, Pakistan.
Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Pharmaceutics. 2022 Oct 23;14(11):2264. doi: 10.3390/pharmaceutics14112264.
The purpose of this study is to improve the solubility and dissolution of a poorly soluble drug, Irbesartan, using solid dispersion techniques. For that purpose, different polymers such as Soluplus Kollidon VA 64, Kolliphor P 407, and Polyinylpyrrolidone (PVP-K30) were used as carriers at different concentrations to prepare solid dispersion formulations through the solvent evaporation method. In order to prepare binary dispersion formulations, Soluplus and Kollidon VA 64 were used at drug: polymer ratios of 1:1, 1:2, 1:3, and 1:4 (). Saturation solubility of the drug in the presence of used carriers was performed to investigate the quantitative increase in solubility. Dissolution studies were performed to explore the drug release behavior from the prepared dispersions. Additionally, the characterization of the prepared formulations was carried out by performing DSC, SEM, XRD, and FTIR studies. The results revealed that among binary systems, K formulation (Drug: Kollidon VA 64 at ratio of 1:4 exhibited optimal performance in terms of increased solubility, drug release, and other investigated parameters. Furthermore, ternary dispersion formulations of the optimized binary formulation were prepared with two more polymers, Kolliphor P 407 and Polyvinylpyrrolidone (PVP-K30), at (Drug: Kollidon VA 64:ternary polymer) ratios of 1:4:1, 1:4:2, and 1:4:3 (). The results showed that KPVP (TD) exhibited the highest increase in solubility, as well as dissolution rate, among ternary solid dispersion formulations. Results of solubility enhancement by ternary solid dispersion formulations were also supported by FTIR, DSC, XRD, and SEM analysis. Conclusively, it was found that the ternary solid dispersion-based systems were more effective compared to the binary combinations in improving solubility as well as dissolution of a poorly soluble drug (Irbesartan).
本研究的目的是使用固体分散技术提高难溶性药物厄贝沙坦的溶解度和溶出度。为此,采用不同浓度的不同聚合物,如固体分散体聚乙烯己内酰胺、共聚维酮VA 64、聚氧乙烯蓖麻油ELP 407和聚乙烯吡咯烷酮(PVP-K30)作为载体,通过溶剂蒸发法制备固体分散体剂型。为了制备二元分散体剂型,固体分散体聚乙烯己内酰胺和共聚维酮VA 64以药物:聚合物比例1:1、1:2、1:3和1:4()使用。在使用的载体存在下进行药物的饱和溶解度研究,以研究溶解度的定量增加。进行溶出度研究以探索所制备分散体的药物释放行为。此外,通过进行差示扫描量热法(DSC)、扫描电子显微镜(SEM)、X射线衍射(XRD)和傅里叶变换红外光谱(FTIR)研究对所制备的剂型进行表征。结果表明,在二元体系中,K剂型(药物:共聚维酮VA 64比例为1:4)在溶解度增加、药物释放和其他研究参数方面表现出最佳性能。此外,用另外两种聚合物聚氧乙烯蓖麻油ELP 407和聚乙烯吡咯烷酮(PVP-K30)以(药物:共聚维酮VA 64:三元聚合物)比例1:4:1、1:4:2和1:4:3()制备优化二元剂型的三元分散体剂型。结果表明,KPVP(TD)在三元固体分散体剂型中溶解度增加以及溶出速率最高。三元固体分散体剂型提高溶解度的结果也得到了FTIR、DSC、XRD和SEM分析的支持。总之,发现基于三元固体分散体的体系在改善难溶性药物(厄贝沙坦)的溶解度和溶出度方面比二元组合更有效。