The objective of this study was to prepare a 72 h-release formulation of silybin (72 h-SLB) using a combination of solid dispersion, gel matrix and porous silica nanoparticles (PSNs) and to investigate the in vitro/in vivo correlations (IVIVCs). The results of scanning electron microscopy and N(2) adsorption demonstrated that empty PSNs possessed a spherical shape, a highly porous structure, a large specific surface area (385.89 ± 1.12 m(2)/g) and a small pore size (2.74 nm on average). The in vitro dissolution profiles of both 72 h-SLB and silybin-loaded PSNs in different concentrations (0.01, 0.06 and 0.08M) of Na(2)CO(3) solutions revealed that 0.06 M Na(2)CO(3) solution was the optimal medium in which silybin could be released from 72 h-SLB with first-order release kinetics and from PSNs with Higuchi kinetics. Furthermore, the IVIVCs of 72 h-SLB and silybin-loaded PSNs in beagle dogs were also established. Using 0.06 M Na(2)CO(3) solution as the in vitro dissolution medium, a good linear relationship could be achieved for both 72 h-SLB and silybin-loaded PSNs. The findings support the fact that the 72 h-SLB (consisting of solid dispersion, regular gel matrix and PSNs) together with Na(2)CO(3) solution as an in vitro dissolution medium can be developed into a promising formulation for poorly soluble drugs, which enjoys a good IVIVC.

译文

本研究的目的是使用固体分散体,凝胶基质和多孔二氧化硅纳米颗粒 (psn) 的组合制备水飞蓟宾 (72 h-SLB) 的72 h释放制剂,并研究体外/体内相关性 (IVIVCs)。扫描电子显微镜和N(2) 吸附结果表明,空psn具有球形,高度多孔结构,大的比表面积 (385.89 ± 1.12 m(2)/g) 和小的孔径 (平均2.74 nm)。72 h-SLB和水飞蓟宾负载的psn在不同浓度 (0.01,0.06和0.08M) 的Na(2)CO(3) 溶液表明,0.06 M Na(2)CO(3) 溶液是最佳介质,其中水飞蓟宾可以从72 h-SLB中释放,具有一级释放动力学和psn。具有Higuchi动力学。此外,还建立了beagle犬中72 h-SLB和水飞蓟宾psn的ivvc。使用0.06 M Na(2)CO(3) 溶液作为体外溶出介质,对于72 h-SLB和水飞蓟宾负载的psn都可以实现良好的线性关系。研究结果支持以下事实: 72 h-SLB (由固体分散体,规则凝胶基质和psn组成) 与Na(2)CO(3) 溶液一起作为体外溶出介质,可以开发为具有良好的IVIVC可溶性药物的有希望的制剂。

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