Kanaujia Parijat, Ng Wai Kiong, Tan Reginald B H
Institute of Chemical and Engineering Sciences , Jurong Island , Singapore .
J Microencapsul. 2014;31(3):293-8. doi: 10.3109/02652048.2013.843601. Epub 2013 Oct 24.
The aim of this work was to develop and characterise S-SEDDS containing fenofibrate (FF) for dissolution enhancement.
The self-emulsifying pre-concentrate was prepared by using different proportion of Labrafac WL1349 as oily phase, Cremophor EL as surfactants and Gelucire 44/14 as co-surfactant. The prepared pre-concentrate was solidified with PEG 6000. For comparison, formulations containing TPGS as surfactant and solidifier were prepared and studied.
The cremophor/PEG and TPGS based S-SEDDS formulations containing 10 and 15% w/w FF when dispersed in water, formed nanoemulsion with a size range of 150-200 nm. FF was present in the crystalline state in the formulations. The formulations containing 10% w/w FF showed 90-100% dissolution in 60 min whereas the untreated FF showed only 2-4% dissolution.
A novel S-SEDDS was developed for FF using cremophor/PEG and TPGS. The dissolution of FF was enhanced by approximately 20-fold in SGF pH 1.2.
本研究旨在开发并表征含非诺贝特（FF）的自乳化药物递送系统（S-SEDDS）以提高其溶出度。
以不同比例的Labrafac WL1349为油相、聚氧乙烯蓖麻油（Cremophor EL）为表面活性剂、Gelucire 44/14为助表面活性剂制备自乳化预浓缩物。将制备的预浓缩物用聚乙二醇6000固化。为作比较，制备并研究了含生育酚聚乙二醇1000琥珀酸酯（TPGS）作为表面活性剂和固化剂的制剂。
含10%和15% w/w FF的基于聚氧乙烯蓖麻油/聚乙二醇和TPGS的S-SEDDS制剂分散于水中时形成粒径范围为150 - 200 nm的纳米乳。制剂中FF以结晶状态存在。含10% w/w FF的制剂在60分钟内溶出度达90 - 100%，而未处理的FF溶出度仅为2 - 4%。
使用聚氧乙烯蓖麻油/聚乙二醇和TPGS为FF开发了一种新型S-SEDDS。在模拟胃液pH 1.2条件下，FF的溶出度提高了约20倍。
