Gumaste Suhas G, Dalrymple Damon M, Serajuddin Abu T M
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, 8000 Utopia Parkway, Queens, NY, 11439, USA.
Pharm Res. 2013 Jun 25;30(12):3186-99. doi: 10.1007/s11095-013-1106-4.
To develop tablet formulations by adsorbing liquid self-emulsifying drug delivery systems (SEDDS) onto Neusilin®US2, a porous silicate.
Nine SEDDS were prepared by combining a medium chain monoglyceride, Capmul MCM EP, a medium chain triglyceride, Captex 355 EP/NF, or their mixtures with a surfactant Cremophor EL, and a model drug, probucol, was then dissolved. The solutions were directly adsorbed onto Neusilin®US2 at 1:1 w/w ratio. Content uniformity, bulk and tap density, compressibility index, Hausner ratio and angle of repose of the powders formed were determined. The powders were then compressed into tablets. The dispersion of SEDDS from tablets was studied in 250 mL of 0.01NHCl (USP dissolution apparatus; 50 RPM; 37°C) and compared with that of liquid SEDDS.
After adsorption of liquid SEDDS onto Neusilin®US2, all powders demonstrated acceptable flow properties and content uniformity for development into tablet. Tablets with good tensile strength (>1 MPa) at the compression pressure of 45 to 135 MPa were obtained. Complete drug release from tablets was observed if the SEDDS did not form gels in contact with water; the gel formation clogged pores of the silicate and trapped the liquid inside pores.
Liquid SEDDS were successfully developed into tablets by adsorbing them onto Neusilin®US2. Complete drug release from tablets could be obtained.
通过将液体自乳化药物递送系统（SEDDS）吸附到多孔硅酸盐Neusilin®US2上开发片剂制剂。
通过将中链甘油单酯Capmul MCM EP、中链甘油三酯Captex 355 EP/NF或它们的混合物与表面活性剂聚氧乙烯蓖麻油Cremophor EL混合制备9种SEDDS，然后溶解一种模型药物普罗布考。将溶液以1:1重量比直接吸附到Neusilin®US2上。测定形成的粉末的含量均匀度、堆密度和振实密度、压缩指数、豪斯纳比和休止角。然后将粉末压制成片剂。在250 mL 0.01N HCl中（美国药典溶出度装置；50转/分钟；37°C）研究片剂中SEDDS的分散情况，并与液体SEDDS进行比较。
将液体SEDDS吸附到Neusilin®US2上后，所有粉末均表现出可接受的流动性质和含量均匀度，可用于开发片剂。在45至135 MPa的压缩压力下获得了具有良好抗张强度（>1 MPa）的片剂。如果SEDDS在与水接触时不形成凝胶，则可观察到片剂中的药物完全释放；凝胶的形成堵塞了硅酸盐的孔隙并将液体困在孔隙内。
通过将液体SEDDS吸附到Neusilin®US2上，成功地将其开发成片剂。片剂可实现药物完全释放。
