Preformulation studies on solid self-emulsifying systems in powder form containing magnesium aluminometasilicate as porous carrier.

Preformulation studies on solid self-emulsifying systems in powder form containing magnesium aluminometasilicate as porous carrier.
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DOI:
10.1208/s12249-014-0247-z
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发表时间:
2015-06
期刊:
影响因子:
3.3
通讯作者:
Jachowicz R
Jachowicz R
中科院分区:
医学3区
文献类型:
--
作者:
Krupa A;Szlęk J;Jany BR;Jachowicz R

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考察了碱性和中性偏硅酸镁铝作为多孔固体载体对布洛芬自乳化液处方的影响。将碘溶解在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获得的制剂的性质。三种含有Neusilin SG 2的固体自乳化(S-SE)制剂和六种由Neusilin US 2组成的固体自乳化(S-SE)制剂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不同。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。如果使用中性等级的偏硅酸铝镁,则低于10 nm的最小孔完全被液体制剂填充,但仍存在一定数量的40-100 nm的孔。在pH = 1.2下进行的液体SEDDS的溶出度研究表明,与纯药物相比,Labrasol改善了布洛芬的溶出度。在pH 7.2下检查的液体SE制剂中的药物溶出是立即的。液体吸附到硅酸盐颗粒上导致释放的药物量减少。最后,从由中性级偏硅酸铝镁组成的S-SE中溶解的布洛芬多于从含有碱性硅酸盐的制剂中溶解的布洛芬。
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.
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