Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Division of Pharmaceutical Sciences, Brooklyn, NY 11201, USA.
Drug Dev Ind Pharm. 2012 Aug;38(8):930-9. doi: 10.3109/03639045.2011.633264. Epub 2011 Nov 15.
Formation of solid dispersion also known as high energy solids is one of the most successful concepts to improve dissolution profile of poorly water-soluble drugs. Use of surfactants in formulation is one of the methods to increase solubility profile. In this research, we have used model drug, a weak acid (indomethacin) together with polymer (PVP) and anionic surfactant (sodium lauryl sulfate (SLS)) in different concentrations to study the effect of incorporation of SLS in solid dispersion. Three ratios and control were prepared. Physical characterization was performed using modulated differential scanning calorimetry (MDSC), X-ray diffraction (XRD) and Fourier transform infrared (FTIR) spectroscopy. Critical micelle concentration (CMC) measurements were conducted to see the effect of SLS on dissolution media. Dissolution studies were performed in hydrochloric acid buffer (pH 1.2 buffer), purified water and phosphate buffer (pH 7.4), respectively. Interestingly, depending upon addition of SLS into the system, release profiles were changed. SLS incorporated internally in a solid dispersion gave the highest release.
固体分散体的形成也称为高能固体,是提高难溶性药物溶解特性最成功的概念之一。在制剂中使用表面活性剂是增加溶解度特性的方法之一。在这项研究中,我们使用模型药物(一种弱酸(吲哚美辛))与聚合物(PVP)和阴离子表面活性剂(十二烷基硫酸钠(SLS))以不同浓度一起研究了 SLS 掺入固体分散体中的效果。制备了三个比例和对照。使用调制差示扫描量热法(MDSC)、X 射线衍射(XRD)和傅里叶变换红外(FTIR)光谱法进行物理特性表征。进行临界胶束浓度(CMC)测量以观察 SLS 对溶解介质的影响。分别在盐酸缓冲液(pH1.2 缓冲液)、纯化水和磷酸盐缓冲液(pH7.4)中进行溶出度研究。有趣的是,根据 SLS 添加到系统中的情况,释放曲线发生了变化。在固体分散体中内部掺入 SLS 可获得最高的释放。