Wagh Vijay D, Pawar Nilesh
Department of Pharmaceutics, R. C. Patel Institute of Pharmaceutical Education and Research, Near Karvand Naka, Maharashtra, Shirpur 425405, India.
ISRN Pharm. 2012;2012:438342. doi: 10.5402/2012/438342. Epub 2012 Jun 18.
An attempt was made to sustain the release of Betahistine hydrochloride by complexation technique using strong cation-exchange resin, Tulsion T344. The drug loading onto ion-exchange resin was optimized for mixing time, activation, effect of pH, swelling time, ratio of drug : resin, and temperature. The resinate was evaluated for micromeritic properties and characterized using XRPD and IR. For resinate sustained release tablets were formulated using hydoxypropyl methylcellulose K100M. The tablets were evaluated for hardness, thickness, friability, drug content, weight variation, and in vitro drug release. Tablets thus formulated (Batch T-3) provided sustained release of drug over a period of 12 h. The release of Betahistine HCl from resinate controls the diffusion of drug molecules through the polymeric material into aqueous medium. Results showed that Betahistine HCl was formulated into a sustained dosage form as an alternative to the conventional tablet.
尝试采用强阳离子交换树脂Tulsion T344通过络合技术来维持盐酸倍他司汀的释放。针对混合时间、活化、pH值影响、溶胀时间、药物与树脂比例以及温度等因素，对离子交换树脂上的药物负载量进行了优化。对树脂酸盐的微观性质进行了评估，并使用X射线粉末衍射（XRPD）和红外光谱（IR）进行了表征。对于树脂酸盐，使用羟丙基甲基纤维素K100M制备了缓释片。对片剂的硬度、厚度、脆碎度、药物含量、重量差异和体外药物释放进行了评估。如此制备的片剂（批次T-3）在12小时内实现了药物的缓释。盐酸倍他司汀从树脂酸盐中的释放控制了药物分子通过聚合物材料扩散到水性介质中的过程。结果表明，盐酸倍他司汀被制成了一种缓释剂型，作为传统片剂的替代剂型。
