Shah S, Pandya S, Bhalekar Mr
Department of Pharmaceutical Technology, Pioneer Pharmacy Degree College, Vadodara, India.
J Young Pharm. 2010 Jul;2(3):247-51. doi: 10.4103/0975-1483.66799.
Ondansetron is a serotonin 5HT3 antagonist; anti-emetic drug. Bitter taste of the ondansetron is a major problem in ensuring patient compliance. The study was designed to formulate tasteless complexes of ondansetron with ion exchange resin and evaluate molecular properties of drug complex. The drug-loading process was carried out using various resins and was optimized using different drug:resin ratio and pH. Resinates were characterized by infrared spectroscopy, thermal analysis, and X-ray powder diffraction (XRPD). Indion 234 gave the best loading efficiency at drug resin ratio of 1:1.5. pH had no effect on drug loading. XRPD studies revealed that drug is in amorphous state in complex. The Infrared studies revealed complexation of secondary amine group of drug with carboxylic functional group of resin. Taste evaluation by using semiquantitative method found resonates as tasteless and agreeable. The release of drug from resinates in simulated gastric fluid was complete in 30 min. Thus, ion exchange resinates offer an effective tool for masking of bitterness and improve drug release.
昂丹司琼是一种5-羟色胺5HT3拮抗剂，即抗呕吐药物。昂丹司琼的苦味是确保患者依从性的一个主要问题。本研究旨在制备昂丹司琼与离子交换树脂的无味复合物，并评估药物复合物的分子特性。药物负载过程使用了各种树脂，并通过不同的药物与树脂比例和pH值进行优化。树脂酸盐通过红外光谱、热分析和X射线粉末衍射（XRPD）进行表征。在药物与树脂比例为1:1.5时，Indion 234具有最佳的负载效率。pH值对药物负载没有影响。XRPD研究表明，药物在复合物中呈无定形状态。红外研究表明，药物的仲胺基团与树脂的羧基官能团发生了络合。采用半定量方法进行的味觉评估发现，树脂酸盐无味且口感宜人。药物从树脂酸盐在模拟胃液中的释放30分钟内完成。因此，离子交换树脂酸盐为掩盖苦味和改善药物释放提供了一种有效的工具。
