Targeted Drug Delivery Research Center, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran ; Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Student Research Committee, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Iran J Basic Med Sci. 2014 May;17(5):337-43.
In this research, zeolite X and zeolite Y were used as vehicle to prepare intestine targeted oral delivery systems of indomethacin and ibuprofen.
A soaking procedure was implemented to encapsulate indomethacin or ibuprofen within synthetic zeolites. Gravimetric methods and IR spectra of prepared formulations were used to assess drug loading efficiencies into zeolite structures. Scanning Electron Microscopy (SEM) was also utilized to determine morphologies changes in synthetic zeolites after drug loading. At the next stage, dissolution studies were used to predict the in vivo performance of prepared formulations at HCl 0.1 N and PBS pH 6.5 as simulated gastric fluid (SGF) and simulated intestine fluid (SIF), respectively.
Drug loadings of prepared formulations was determined between 24-26 % w/w. Dissolution tests at SGF were shown that zeolites could retain acidic model drugs in their porous structures and can be able to limit their release into the stomach. On the other hand, all prepared formulations completely released model drugs during 3 hr in simulated intestine fluid.
Obtained results indicated zeolites could potentially be able to release indomethacin and ibuprofen in a sustained and controlled manner and reduced adverse effects commonly accompanying oral administrations of NSAIDs.
本研究以沸石 X 和沸石 Y 为载体,制备吲哚美辛和布洛芬的肠靶向口服给药系统。
采用浸泡法将吲哚美辛或布洛芬包封于合成沸石中。采用重量法和红外光谱对制备的制剂进行评估,以确定药物在沸石结构中的负载效率。扫描电子显微镜(SEM)也用于确定药物负载后合成沸石的形貌变化。在下一步,通过溶出度研究分别在 0.1N HCl 和 PBS pH 6.5 作为模拟胃液(SGF)和模拟肠液(SIF)来预测制备制剂的体内性能。
制备制剂的药物载量为 24-26%w/w。在 SGF 中的溶出度试验表明,沸石可以在其多孔结构中保留酸性模型药物,并能够限制它们在胃中的释放。另一方面,所有制备的制剂在模拟肠液中 3 小时内完全释放了模型药物。
研究结果表明,沸石可能能够以持续和控制的方式释放吲哚美辛和布洛芬,并减少 NSAIDs 口服给药常见的不良反应。