Patel Ashok R, Joshi Vishal Y
Department of Pharmaceutical Sciences, University Institute of Chemical Technology, Matunga, Mumbai 400019, India.
AAPS PharmSciTech. 2008;9(2):583-90. doi: 10.1208/s12249-008-9093-1. Epub 2008 May 6.
The present investigation aims at studying the effect of mixed surfactant system of sodium lauryl sulphate (SLS) and alkyl polyglucosides (C(10)APG, C(12)APG and C(12/14)APG) on dissolution rate enhancement of poorly water soluble drug. Aceclofenac--a non-steroidal anti-inflammatory agent was used as a model drug as it has limited water solubility. The influence of the surfactant concentration in various blends on dissolution rate of Solid Dispersion (SD), prepared using solution method with ethanol as the solvent was studied and the advantage of mixed surfactant systems over the individual surfactants was illustrated by differences in the in-vitro dissolution profiles of SD. Physico chemical evaluation (critical micellar concentration, zeta potential and beta-parameter calculations) was carried out to study the mixed surfactant systems. Solid mixtures were characterized by Infrared spectroscopy (FT-IR); X-ray diffraction studies (XRD) and scanning electron microscopy (SEM). It was seen that the dissolution rate of aceclofenac from SD increased with the increase in the APG proportion relative to SLS with the optimum ratio of 0.2 SLS:0.8 APG showing the best effect in all cases. Results obtained from physico-chemical evaluation (the decrease in the value of critical micelle concentration and higher negative value of beta-parameters) suggested the existence of synergism between surfactants blends. The observed results in the dissolution rate enhancement could be attributed to the drug--surfactant interactions as evident from FT-IR, SEM and XRD results.
本研究旨在探讨月桂醇硫酸酯钠(SLS)与烷基多苷(C(10)APG、C(12)APG和C(12/14)APG)混合表面活性剂体系对难溶性药物溶出速率提高的影响。双氯芬酸——一种非甾体抗炎药,因其水溶性有限,被用作模型药物。研究了各种混合体系中表面活性剂浓度对以乙醇为溶剂采用溶液法制备的固体分散体(SD)溶出速率的影响,并通过SD体外溶出曲线的差异说明了混合表面活性剂体系相对于单一表面活性剂的优势。对混合表面活性剂体系进行了物理化学评估(临界胶束浓度、ζ电位和β参数计算)。通过红外光谱(FT-IR)、X射线衍射研究(XRD)和扫描电子显微镜(SEM)对固体混合物进行了表征。结果表明,双氯芬酸从SD中的溶出速率随着APG相对于SLS比例的增加而增加,最佳比例为0.2 SLS:0.8 APG,在所有情况下均显示出最佳效果。物理化学评估结果(临界胶束浓度值降低和β参数更高的负值)表明表面活性剂混合物之间存在协同作用。从FT-IR、SEM和XRD结果可以明显看出,溶出速率提高的观察结果可归因于药物与表面活性剂的相互作用。