Krishnamoorthy Venkateskumar, Nagalingam Arunkumar, Priya Ranjan Prasad Verma, Parameshwaran Siva, George Neema, Kaliyan Punitha
Iran J Pharm Res. 2011 Winter;10(1):13-24.
To enhance the aqueous solubility of olanzapine by using the Solid dispersion technique. Solid dispersions of olanzapine were prepared by the dispersion method using using PGS and SSG as carriers. Drug-carrier ratios such as 1 : 1, 1 : 2, 1 : 4, 1 : 6, 1: 8 and 1 : 10 were tried for optimization. Characterization was done by phase solubility, in-vitro release, saturation solubility, permeation, wettability, XRD and FTIR analysis. Solid dispersions showed higher solubility and an improved drug release profile than the pure drug. Solid dispersion and physical mixture with a drug-polymer ratio of 1 : 10 showed the best release profile in comparison with the other samples. Phase solubility results verified the solubilization effect of the carrier. XRD and NIR analysis confirmed the reduction of crystallinity in the samples. The release study findings were well supported by the results of wettability, saturation solubility and permeability studies. IR analysis substantiated the inertness of the carrier. It was concluded that pregelatinised starch (PGS) and sodium starch glycollate (SSG) could be utilized as effective carriers to improve the aqueous solubility of poorly soluble drugs.
通过固体分散技术提高奥氮平的水溶性。以聚乙二醇(PGS)和羟丙甲纤维素(SSG)为载体,采用分散法制备奥氮平固体分散体。尝试了1:1、1:2、1:4、1:6、1:8和1:10等药物-载体比例以进行优化。通过相溶解度、体外释放、饱和溶解度、渗透性、润湿性、X射线衍射(XRD)和傅里叶变换红外光谱(FTIR)分析进行表征。固体分散体比纯药物表现出更高的溶解度和改善的药物释放曲线。与其他样品相比,药物-聚合物比例为1:10的固体分散体和物理混合物表现出最佳的释放曲线。相溶解度结果证实了载体的增溶作用。XRD和近红外光谱(NIR)分析证实了样品中结晶度的降低。润湿性、饱和溶解度和渗透性研究的结果很好地支持了释放研究的发现。红外光谱分析证实了载体的惰性。得出的结论是,预胶化淀粉(PGS)和羟丙甲纤维素钠(SSG)可作为有效的载体来提高难溶性药物的水溶性。