Shrivastava R, Jain S R, Frank S G
J Pharm Sci. 1985 Feb;74(2):214-6. doi: 10.1002/jps.2600740224.
In the context of the potential usefulness of clays in retarding the rate of release of adsorbed drugs, dissolution dialysis studies of the release of metronidazole from montmorillonite adsorbates have been conducted. The goal was to develop a means for improving local gastrointestinal therapy of amebiasis while concurrently maintaining efficacy in treating hepatic amebiasis. At acidic pH, the clay was in a flocculated state and the rate of drug release was inhibited. This effect was apparently due to slow diffusion of the drug throughout the clay flocculate. A physical admixture of montmorillonite and metronidazole was also effective in inhibiting the rate of release of metronidazole. Upon increasing the pH to 7, the clay particles progressively deflocculated and the rate of release increased significantly.
鉴于黏土在延缓吸附药物释放速率方面可能具有的用途,已开展了甲硝唑从蒙脱石吸附物中释放的溶出度透析研究。目标是开发一种方法,以改善阿米巴病的局部胃肠道治疗,同时保持治疗肝阿米巴病的疗效。在酸性pH值下,黏土处于絮凝状态,药物释放速率受到抑制。这种效应显然是由于药物在整个黏土絮凝物中的缓慢扩散所致。蒙脱石与甲硝唑的物理混合物在抑制甲硝唑释放速率方面也有效。将pH值提高到7时,黏土颗粒逐渐解絮凝,释放速率显著增加。