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首页> 外文期刊>American Journal of Drug Discovery and Development >Preparation and Evaluation of Floating Matrix Tablet of Ranitidine
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Preparation and Evaluation of Floating Matrix Tablet of Ranitidine

机译:雷尼替丁漂浮基质片剂的制备与评价

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Ranitidine hydrochloride has a short biological half-life (2.1±0.2 h) and 50% absolute bioavailability. Development of sustained release formulation of ranitidine hydrochloride can be advantageous, that can provide prolong gastric retention and increase efficacy of the dosage form. Calculate theoretical release profile from floating matrix tablets of ranitidine and perform the drug excipient interaction study. In vitro dissolution studies, dissolution profiles, drug: polymer ratio, effect of low density copolymer PSDVB on the release profile of chitosan-carbopol 940 floating matrix tablets, geometry on release, effect of diluents were performed. Select the best batch and swelling index, kinetic modeling of drug release, accelerated stability and in vivo study were carried out. No chemical interaction between ranitidine hydrochloride and the polymers used. Result shows loss of integrity with the increase in concentration of carbopol 940. Significant changes in the floating lag time of the formulation with increased amount of co-polymer. With increasing initial tablet radius, the volume of the system and, thus, the amount of drug available for diffusion increases, resulting in increased absolute amounts of drug released. In contrast, the relative surface area of the device decreases and the amount of drug released in%/ time unit decreased. The x-ray and swelling index shows significant result in batch A12. The present investigation shows that the chitosan-carbopol 940 mixed matrices can be used to modify release rates in hydrophilic matrix tablets prepared by direct compression.
机译:盐酸雷尼替丁的生物半衰期短(2.1±0.2小时),绝对生物利用度为50%。开发盐酸雷尼替丁的持续释放制剂可能是有利的,其可以提供延长的胃滞留时间并增加剂型的功效。计算雷尼替丁漂浮基质片剂的理论释放曲线,并进行药物赋形剂相互作用研究。进行了体外溶出度研究,溶出度分布,药物:聚合物比率,低密度共聚物PSDVB对壳聚糖-carbopol 940漂浮基质片剂的释放分布的影响,释放的几何形状,稀释剂的影响。选择最佳批次和溶胀指数,进行药物释放动力学模型,加速稳定性和体内研究。盐酸雷尼替丁与所用聚合物之间没有化学相互作用。结果表明,随着carbopol 940浓度的增加,完整性下降。随着共聚物量的增加,配方的漂浮滞后时间发生了显着变化。随着初始片剂半径的增加,系统的体积以及因此可用于扩散的药物的量增加,导致释放的药物的绝对量增加。相反,装置的相对表面积减小,并且释放的药物量(单位为%/时间单位)减少。 X射线和溶胀指数在批次A12中显示出明显的结果。本研究表明,壳聚糖-carbopol 940混合基质可用于改变通过直接压制制备的亲水性基质片剂的释放速率。

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