University of Greenwich, School of Science , Chatham Maritime, Kent , UK .
Pharm Dev Technol. 2014 Aug;19(5):531-8. doi: 10.3109/10837450.2013.805775. Epub 2013 Jun 13.
Sustained release diclofenac sodium (Df-Na) solid lipid matrices with Compritol® 888 ATO were developed in this study. The drug/lipid powders were processed via cold and hot melt extrusion at various drug loadings. The influence of the processing temperatures, drug loading and the addition of excipients on the obtained dissolution rates was investigated. The physicochemical characterization of the extruded batches showed the existence of crystalline drug in the extrudates with a small amount being solubilized in the lipid matrix. The drug content and uniformity on the tablet surface were also investigated by using energy dispersive X-ray microanalysis. The dissolution rates were found to depend on the actual Df-Na loading and the nature of the added excipients, while the effect of the processing temperatures was negligible. The dissolution mechanism of all extruded formulations followed Peppas-Korsemeyer law, based on the estimated determination coefficients and the dissolution constant rates, indicating drug diffusion from the lipid matrices.
本研究制备了载有双氯芬酸钠（Df-Na）的固体脂质基质，并使用 Compritol® 888 ATO 作为辅料。通过冷和热熔挤出的方法在不同的载药量下处理药物/脂质粉末。考察了加工温度、载药量和辅料的添加对获得的溶出率的影响。挤出物的理化特性表明，挤出物中存在结晶药物，且少量药物溶解在脂质基质中。还通过能量色散 X 射线微分析研究了片剂表面的药物含量和均匀性。发现溶出率取决于实际的 Df-Na 载药量和添加辅料的性质，而加工温度的影响可以忽略不计。根据估计的决定系数和溶解常数速率，所有挤出制剂的溶解机制均符合 Peppas-Korsemeyer 定律，表明药物从脂质基质中扩散。
