Gupta College of Technological Sciences, Ashram More, G.T Road, Asansol-713301, West Bengal, India.
Drug Deliv. 2010 Jul;17(5):288-300. doi: 10.3109/10717541003706265.
In this study, carboxymethyl derivative of locust bean gum was prepared, characterized, and its gelling ability with different concentrations (1-5% w/v) of aluminum chloride (AlCl(3)) was utilized for the development of glipizide-loaded beads in a completely aqueous environment. The beads were spherical when observed under a scanning electron microscope. Increase in gelling ion concentration decreased the drug entrapment efficiency from 97.68% to 95.14%. The beads swelled more slowly in pH 1.2 KCl-HCl buffer and exhibited a slower drug release pattern than that observed in pH 7.4 phosphate buffer. Irrespective of the dissolution media, the drug release became slower at higher AlCl(3) concentration. The drug release in alkaline medium was found to be controlled by a combination of diffusion as well as polymer relaxation phenomena. Comparing the release profiles, it was observed that the beads treated with 5% AlCl(3) provided slower drug release up to 10 h in alkaline medium without any sign of disintegration and, thus, this formulation was selected for further studies. Fourier transform infrared (FTIR) spectroscopy indicated the stable nature of the drug in the beads. Differential scanning calorimetry and X-ray diffraction analysis showed that most of the drug remained in amorphous state in the beads. Stability study indicated no statistical significant difference in drug entrapment efficiency of the beads. In vivo activity of the beads was tested and a prolonged hypoglycemic effect was achieved. Hence, carboxymethyl locust bean beads could be a potential carrier for controlled oral delivery of glipizide.
在这项研究中,制备了槐豆胶的羧甲基衍生物,对其进行了表征,并利用其与不同浓度(1-5%w/v)的氯化铝(AlCl(3))的凝胶能力,在完全水相环境中开发了格列吡嗪载药微球。扫描电子显微镜下观察到这些微球呈球形。随着凝胶化离子浓度的增加,药物包封效率从 97.68%降低到 95.14%。在 pH 1.2 的 KCl-HCl 缓冲液中,微球的溶胀速度较慢,且药物释放模式比在 pH 7.4 的磷酸盐缓冲液中观察到的要慢。无论溶解介质如何,AlCl(3)浓度越高,药物释放越慢。在碱性介质中,药物释放被认为是扩散和聚合物松弛现象的综合控制。比较释放曲线,观察到用 5%AlCl(3)处理的微球在碱性介质中提供了长达 10 小时的缓慢药物释放,没有任何崩解的迹象,因此,选择这种制剂进行进一步研究。傅里叶变换红外(FTIR)光谱表明药物在微球中性质稳定。差示扫描量热法和 X 射线衍射分析表明,大部分药物在微球中仍处于无定形状态。稳定性研究表明,微球的药物包封效率没有统计学上的显著差异。对微球的体内活性进行了测试,结果表明其具有延长的降血糖作用。因此,羧甲基槐豆胶微球可能是格列吡嗪控释口服给药的潜在载体。