不同超崩解剂对特兰多普利速释片的研制与表征

ARPNA INDURKHYA, MAHENDRA PATEL, MASHEER AHMED KHAN
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引用次数: 0

摘要

一种有效的非巯基前药,曲多乐普利在肝脏中转化为活性物质曲多乐普利。对于伴有轻中度原发性高血压的肥胖患者,曲多普利是安全有效的。trandolapril和trandolaprilat的消除时间分别约为6小时和16-24小时。本研究的目的是利用不同的超崩解剂制备特兰多普利速释片。以浓度分别为2%、4%和6%的交叉聚维酮、淀粉乙醇酸钠和交叉卡蜜糖钠作为超崩解剂进行优化。采用直接压缩技术制备了9个配方(IRTR 1 ~ IRTR 9),并对各批次的粉末共混物进行了不同参数的评价,以了解粉末的流动特性,发现该粉末共混物具有良好的流动特性和压缩特性。然后,根据IP测试压缩片剂的质量控制参数。制剂IRTR1-IRTR9的崩解时间为30.23 ~ 71.67秒,30 min内释药率超过70%。综合评价结果,认为特兰多乐普即刻释放片研制成功。崩解时间最短30.23 s, 30 min释药率为90.56%。关键词:曲度普利,速释型,交叉旋维酮,乙醇酸淀粉钠,豆胶糖钠
本文章由计算机程序翻译,如有差异,请以英文原文为准。
DEVELOPMENT AND CHARACTERIZATION OF TRANDOLAPRIL IMMEDIATE RELEASE TABLETS USING DIFFERENT SUPERDISINTEGRATING AGENTS
A potent non-sulfhydryl prodrug, trandolapril is transformed into the active substance, trandolaprilat, in the liver. For obese individuals with mild-to-moderate essential hypertension, Trandolapril is effective and safe. The elimination t1/2 of trandolapril and trandolaprilat are approximately 6 hours and 16–24 hours, respectively. The goal of present work is to develop the Trandolapril immediate release tablet using various superdisintegrants. Crospovidone, Sodium starch glycolate and Croscarmellose sodium in concentrations of 2%, 4%, and 6% were used as superdisintegrating agents for the optimization. Direct compression technique was used to make nine formulations (IRTR 1 to IRTR 9). The powder blends of all batches were evaluated for different parameters to know the powder flow characteristics and it was found that the powder blend had excellent flow and compressibility characteristics. Then, compressed tablets were tested for quality control parameters as per the IP. In formulation IRTR1-IRTR9, disintegration time was observed 30.23 to 71.67 Sec and more than 70% drug was released in 30 min. Thus, based on evaluation results, it is concluded that formulation of immediate release (IR) tablets of Trandolapril were successfully developed. Minimum disintegration time 30.23 seconds 90.56% drug release in 30 min was obtained with IRTR3. KEYWORDS: Trandolapril, Immediate release, Crospovidone, Sodium starch glycolate, crocarmellose sodium
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