Department of Pharmaceutics, King Khalid University, Guraiger, Abha, 62529, Saudi Arabia.
Department of Pharmaceutics, N.R. Vekaria Institute of Pharmacy, Junegad, 362001, India.
AAPS PharmSciTech. 2019 Jan 2;20(1):35. doi: 10.1208/s12249-018-1265-z.
The main purpose of the study was to develop valsartan floating tablets (VFT) via non-effervescent technique using low density polypropylene foam powder, carbopol, and xanthan gum by direct compression. Before compression, the particulate powdered mixture was evaluated for pre-compression parameters. The prepared valsartan tablets were evaluated for post-compression parameters, swelling index, floating lag time, in vitro buoyancy studies, and in vitro and in vivo X-ray imaging studies in albino rabbits. The result of all formulations for pre- and post-compression parameters were within the limits of USP. FTIR and DSC studies revealed no interaction between the drug and polymers used. The prepared floating tablets had good swelling and floating capabilities for more than 12 h with zero floating lag time. The release of valsartan from optimized formulation NF-2 showed sustained release up to 12 h; which was found to be non-Fickian release. Moreover, the X-ray imaging of optimized formulation (NF-2) revealed that tablet was constantly floating in the stomach region of the rabbit, thereby indicating improved gastric retention time for more than 12 h. Consequently, all the findings and outcomes have showed that developed valsartan matrix tablets could be effectively used for floating drug delivery system.
本研究的主要目的是通过非发酵技术,使用低密度聚丙烯泡沫粉末、卡波姆和黄原胶,通过直接压缩,开发缬沙坦漂浮片(VFT)。在压缩之前,对颗粒状粉末混合物进行了压缩前参数评估。对制备的缬沙坦片进行了压缩后参数、溶胀指数、漂浮滞后时间、体外漂浮研究以及在白化兔体内和体内的 X 射线成像研究的评估。所有配方的预压缩和后压缩参数的结果均在 USP 范围内。FTIR 和 DSC 研究表明,药物与所用聚合物之间没有相互作用。所制备的漂浮片具有良好的溶胀和漂浮能力,超过 12 小时,无漂浮滞后时间。从优化配方 NF-2 中释放缬沙坦呈持续释放达 12 小时;被发现是非菲克释放。此外,优化配方(NF-2)的 X 射线成像显示,片剂在兔子的胃部区域持续漂浮,这表明胃滞留时间延长了 12 小时以上。因此,所有的发现和结果都表明,开发的缬沙坦基质片可有效用于漂浮药物传递系统。