Starýchová Lenka, Žabka Marián, Špaglová Miroslava, Čuchorová Mária, Vitková Mária, Čierna Martina, Bartoníková Kamila, Gardavská Klára
Department of Galenic PharmacyFaculty of PharmacyComenius University in BratislavaBratislava832 32Slovakia.
Department of Galenic PharmacyFaculty of PharmacyComenius University in BratislavaBratislava832 32Slovakia.
J Pharm Sci. 2014 Dec;103(12):3977-3984. doi: 10.1002/jps.24213. Epub 2014 Oct 15.
The objective of this research is to outline the liberation of indomethacin from different chitosan gels containing O/W microemulsion. The influence of surfactant, sodium lauryl sulfate, in two concentrations (0.5% and 0.75%, w/w) was determined in dissolution medium on the release of indomethacin, which was used as poor water-soluble model drug. Chitosan gels were prepared in four different concentrations of chitosan-1%, 1.5%, 2%, and 3% (w/w). Microemulsion enhanced the liberation of the indomethacin from chitosan gels into all dissolution mediums. Adding the surfactant into phosphate-buffered saline decreased the amount of liberated indomethacin from microemulsion, gel mixture, but increased the drug liberation from pure chitosan gels. It was detected that with the increased concentration of chitosan in the samples, the amount of indomethacin liberated (p < 0.05) also increased. A conclusion was drawn that the liberation of indomethacin from chitosan gels was influenced by increased pH of the samples. The high viscosity induced a higher release of indomethacin from 3% (w/w) chitosan hydrogel at pH 5.8 as compared with 3% (w/w) chitosan hydrogel at pH 3.8. The highest percentage of released indomethacin was determined when a mixture of microemulsion gel with higher chitosan content was used.
本研究的目的是概述吲哚美辛从含有水包油微乳的不同壳聚糖凝胶中的释放情况。在溶出介质中测定了两种浓度（0.5%和0.75%，w/w）的表面活性剂十二烷基硫酸钠对吲哚美辛释放的影响，吲哚美辛用作难溶性模型药物。制备了四种不同浓度（1%、1.5%、2%和3%，w/w）的壳聚糖凝胶。微乳增强了吲哚美辛从壳聚糖凝胶向所有溶出介质中的释放。向磷酸盐缓冲盐溶液中添加表面活性剂会减少微乳凝胶混合物中吲哚美辛的释放量，但会增加纯壳聚糖凝胶中药物的释放量。检测到随着样品中壳聚糖浓度的增加，吲哚美辛的释放量（p<0.05）也增加。得出的结论是，壳聚糖凝胶中吲哚美辛的释放受样品pH值升高的影响。与pH值为3.8的3%（w/w）壳聚糖水凝胶相比，在pH值为5.8时，高粘度导致3%（w/w）壳聚糖水凝胶中吲哚美辛的释放量更高。当使用壳聚糖含量较高的微乳凝胶混合物时，吲哚美辛的释放百分比最高。
