Faculty of Pharmacy, Department of Pharmaceutical Technology, Ege University, 35100, Bornova, Izmir, Turkey.
AAPS PharmSciTech. 2013 Mar;14(1):391-7. doi: 10.1208/s12249-013-9922-8. Epub 2013 Jan 24.
The aim of this work was to prepare organogels of Carbopol 974P NF (C974) in PEG 400 by using a novel technique, high-speed homogenization followed by microwave heating. Triclosan (TCS) was used as a model drug. C974, at concentrations ranging between 2% and 4%, was dispersed in 25 ml of PEG 400, and the dispersion was homogenised for 5 min at 24,000 rpm. The dispersion was either heated at 80°C in water bath under mechanic stirring at 200 rpm or exposed to micro-irradiation (1,200 W/1 h) for 2 min. The formulations prepared with both methods performed a well-structured gel matrix characteristic at 3% and 4% of C974 concentrations. As the concentrations of the polymer increased, the elastic properties also increased. The viscosity profiles indicated a shear-thinning system. DSC data revealed that TCS was dissolved in gel. Skin accumulation ability of TCS had been improved by these novel organogels regardless of the preparation method. TCS was still microbiologically effective after the microwave process was applied. It was determined that microwave heating is a suitable method to obtain C974 organogels. This novel production technique developed might be promising especially in industrial scale when the dramatic reduction in the preparation time and energy were considered.
本工作旨在通过高速匀化后微波加热的新方法制备 Carbopol 974P NF(C974)的 PEG 400 型有机凝胶。三氯生(TCS)用作模型药物。C974 以 2%至 4%的浓度分散在 25ml 的 PEG 400 中,分散体在 24,000rpm 下匀化 5 分钟。分散体在 80°C 的水浴中通过 200rpm 的机械搅拌加热,或者暴露于微辐射(1,200W/1h)2 分钟。用这两种方法制备的制剂在 3%和 4%的 C974 浓度下均表现出良好的结构化凝胶基质特征。随着聚合物浓度的增加,弹性特性也增加。粘度曲线表明存在剪切稀化体系。DSC 数据表明 TCS 溶解在凝胶中。无论采用哪种制备方法,这些新型有机凝胶都能提高 TCS 的皮肤蓄积能力。TCS 在微波处理后仍具有微生物学功效。确定微波加热是获得 C974 有机凝胶的合适方法。当考虑到制备时间和能源的大幅减少时,这种新开发的生产技术可能具有广阔的前景,特别是在工业规模上。