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首页> 外文期刊>American Journal of Drug Discovery and Development >Development of a New Carvedilol Tablet with Rapid Onset of Action
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Development of a New Carvedilol Tablet with Rapid Onset of Action

机译:快速起效的新型卡维地洛片的研制

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The purpose of this study was to develop Freeze-dried Tablets (FDTs) for rapid absorption of carvedilol, an antihypertensive drug with poor solubility and poor bioavailability. Binary and ternary systems were first made of drug and different ratios of HPMC and Inutec and then were formulated into FDTs. Formulation of FDTs was based on 23 factorial design to study the influence of formulation variables namely, concentration of polymer matrix-former, concentration of collapse protectant and type of polymer used in formation of drug binary and ternary systems on tablet characteristics such as friability, in vitro disintegration time, in vivo disintegration time and initial dissolution. An optimized FDT formulation (RO) containing 2% gelatin, 1% glycine and binary system made of Drug: Inutec in the ratio 1:0.5 showed excellent mechanical strength, in vitro and in vivo disintegration times of less than 10 sec and more than 30% drug dissolved during the first 3 min compared to only 11% for the drug powder and 8% drug from an immediate release commercially available tablet (Carvepress). When the optimized FDT (RO) was administered to hypertensive rats it resulted in a significant decrease (p = 0.0015) in systolic blood pressure within the first 15 min compared to the immediate release conventional tablet as a reference which indicate the rapid dissolutionand absorption of carvedilol from the FDT.
机译:这项研究的目的是开发可快速吸收卡维地洛的冷冻干燥片剂(FDT),卡维地洛是一种溶解性和生物利用度较差的降压药。二元和三元系统首先由药物和不同比例的HPMC和Inutec组成,然后配制成FDT。 FDT的配方基于23阶乘设计,研究了配方变量(即聚合物基质前体的浓度,崩塌保护剂的浓度以及用于形成药物二元和三元体系的聚合物类型)对片剂特性(如易碎性)的影响。体外崩解时间,体内崩解时间和初始溶解。一种优化的FDT配方(RO),其中含有2%的明胶,1%的甘氨酸和以1:0.5的比例由Drug:Inutec制成的二元体系显示出优异的机械强度,体外和体内崩解时间少于10秒且超过30秒在前3分钟内溶解的药物百分比为5%,而粉末药和即时释放的市售片剂(Carvepress)的药物仅为8%。当将优化的FDT(RO)给予高血压大鼠时,与作为参考的速释常规片剂相比,前15分钟内收缩压显着降低(p = 0.0015),这表明卡维地洛迅速溶解和吸收来自FDT。

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