Krupa Anna, Szlęk Jakub, Jany Benedykt R, Jachowicz Renata
Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, Jagiellonian University, Medical College, 9 Medyczna Str, 30-688, Cracow, Poland,
AAPS PharmSciTech. 2015 Jun;16(3):623-35. doi: 10.1208/s12249-014-0247-z. Epub 2014 Dec 11.
The influence of alkaline and the neutral grade of magnesium aluminometasilicate as a porous solid carrier for the liquid self-emulsifying formulation with ibuprofen is investigated. Ibuprofen is dissolved in Labrasol, then this solution is adsorbed on the silicates. The drug to the silicate ratio is 1:2, 1:4, and 1:6, respectively. The properties of formulations obtained are analyzed, using morphological, porosity, crystallinity, and dissolution studies. Three solid self-emulsifying (S-SE) formulations containing Neusilin SG2 and six consisting of Neusilin US2 are in the form of powder without agglomerates. The nitrogen adsorption method shows that the solid carriers are mesoporous but they differ in a specific surface area, pore area, and the volume of pores. The adsorption of liquid SE formulation on solid silicate particles results in a decrease in their porosity. If the neutral grade of magnesium aluminometasilicate is used, the smallest pores, below 10 nm, are completely filled with liquid formulation, but there is still a certain number of pores of 40-100 nm. Dissolution studies of liquid SEDDS carried out in pH = 1.2 show that Labrasol improves the dissolution of ibuprofen as compared to the pure drug. Ibuprofen dissolution from liquid SE formulations examined in pH of 7.2 is immediate. The adsorption of the liquid onto the particles of the silicate causes a decrease in the amount of the drug released. Finally, more ibuprofen is dissolved from S-SE that consist of the neutral grade of magnesium aluminometasilicate than from the formulations containing the alkaline silicate.
研究了碱性和中性级别的镁铝硅酸盐作为布洛芬液体自乳化制剂的多孔固体载体的影响。布洛芬溶解在Labrasol中，然后将该溶液吸附在硅酸盐上。药物与硅酸盐的比例分别为1:2、1:4和1:6。使用形态学、孔隙率、结晶度和溶出度研究来分析所得制剂的性质。三种含有Neusilin SG2的固体自乳化（S-SE）制剂和六种由Neusilin US2组成的制剂均为无团聚物的粉末形式。氮吸附法表明，固体载体是介孔的，但它们在比表面积、孔面积和孔体积方面存在差异。液体SE制剂在固体硅酸盐颗粒上的吸附导致其孔隙率降低。如果使用中性级别的镁铝硅酸盐，小于10 nm的最小孔隙会完全被液体制剂填充，但仍有一定数量的40-100 nm的孔隙。在pH = 1.2下进行的液体SEDDS溶出度研究表明，与纯药物相比，Labrasol提高了布洛芬的溶出度。在pH为7.2的条件下检测的液体SE制剂中布洛芬的溶出是即时的。液体在硅酸盐颗粒上的吸附导致药物释放量减少。最后，由中性级别的镁铝硅酸盐组成的S-SE制剂中溶解的布洛芬比含有碱性硅酸盐的制剂更多。
