生物利用度
泊洛沙姆
胶束
莫沙比利
首过效应
溶解度
化学
肺表面活性物质
色谱法
材料科学
鼻腔给药
药理学
医学
水溶液
有机化学
生物化学
聚合物
共聚物
作者
Reham Waheed Hammad,Rania Abdel-Basset Sanad,Nevine Shawky Abdelmalak,Faisal A. Torad,Randa Latif
标识
DOI:10.1016/j.jare.2020.01.013
摘要
Mosapride belongs to class IV in Biopharmaceutics Classification System and is used in the treatment of reflux esophagitis. It exhibits poor bioavailability due to limited permeability, solubility and extensive first-pass metabolism. In this study, intranasal mosapride-loaded cross-linked xyloglucan Pluronic micelles (MOS-XPMs) was formulated and optimized to improve the low solubility & bioavailability of MOS. The solid dispersion technique using 23 full factorial design was applied. (MOS-XPMs) (F4) had the highest desirability value (0.952) and, therefore, it was selected as an optimal system. Xyloglucan cross-linked in the shell of Pluronic micelles offered improved stability and mucoadhesiveness to MOS-XPMs. 1H NMR spectra ensured the cross-linking of xyloglucan with Pluronic micelle shell and micelle stabilization. A Pharmacodynamic study revealed that MOS-XPMs showed 1.5-fold increase in duodenal and cecal motility compared to MOS suspension and 1.7-fold increase compared to the oral marketed product. The new MOS-XPMs were shown to be successful at improving the therapeutic efficacy of mosapride.
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