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Formulation and evaluation of floating pulsatile drug delivery system of Metoprolol tartrate

机译:酒石酸美托洛尔的浮动脉动给药系统的设计与评价

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The objective of present investigation was to prepare and evaluate a floating pulsatile drug delivery system of metoprolol tartrate. The prepared floating pulsatile delivery system consisted of three different parts: a core tablet, containing the active ingredient, an erodible outer shell and a top cover buoyant layer. The rapid release core tablet (RRCT) was prepared by using superdisintegrants along with active ingredient. Dry coating of optimized RRCT was done by using different grades of hydroxy propyl methyl cellulose (HPMC) E5, E15, and E50 and upper most buoyant layer was prepared with HPMC K15M and sodium bicarbonate. Developed formulations were evaluated for their physical characteristics, drug content, in vitro disintegration time, in vitro drug release profile (lag time), floating lag time, floating time and in vivo X-ray study. On the basis of these evaluation parameters it was found that optimized floating pulsatile release formulation (FPRT) F9 showed floating lag time of 4 min, floating time of 12 hrs and release lag time of 6 hrs. The F9 formulation showed compliance with chronotherapeutic objective of hypertension.
机译:本研究的目的是制备和评估酒石酸美托洛尔的浮动脉动药物递送系统。所准备的浮动脉动递送系统由三个不同部分组成:包含活性成分的核心片剂,易蚀的外壳和顶盖浮力层。通过使用超崩解剂和活性成分来制备快速释放核心片剂(RRCT)。通过使用不同等级的羟丙基甲基纤维素(HPMC)E5,E15和E50进行优化RRCT的干涂,并用HPMC K15M和碳酸氢钠制备最上浮力层。评价开发的制剂的物理特性,药物含量,体外崩解时间,体外药物释放曲线(滞后时间),浮动滞后时间,浮动时间和体内X射线研究。根据这些评估参数,发现优化的浮式脉动释放制剂(FPRT)F9的浮潜时间为4分钟,浮潜时间为12小时,释放滞后时间为6小时。 F9配方显示符合高血压的计时治疗目标。

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