Diltiazem Hydrochloride Floating Matrix Tablet: Formulation and in vitro-in vivo Evaluation.

Krishna D Koradia, Bhavin K Jotaniya, Hiral D Koradia
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Abstract

Background: Diltiazem hydrochloride is a calcium channel-blocker with a plasma elimination half-life of 4.4 ± 1.3 h and has a narrow absorption window. So, this work aimed to prepare a gastro-retentive floating matrix tablet.

Methods: The direct compression method was used to manufacture tablets. 32 factorial design was applied for optimization, taking Hydroxypropyl Methylcellulose K100M (HPMC K 100M) and the amount of sodium bicarbonate as independent factors and cumulative percentage release at 1 h, at 6 h, and at 12 h and floating lag time as dependent variables.

Results: The high amount of HPMC K100M and sodium bicarbonate shows good results. The optimized preparation was evaluated for differential scanning calorimetry, in-vivo gastric retention in male albino rabbits, kinetic modeling, and stability study. An in vivo study revealed gastric retention of tablets up to 6 h in healthy male Albino rabbits. The stability study indicated no significant change in the buoyancy and release profiles of the drug.

Conclusion: From this study, it can be concluded that the gastro-retentive diltiazem hydrochloride floating matrix tablet was successfully prepared and retained inside the rabbit stomach for up to 6 h and was stable under accelerated stability study.

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盐酸地尔硫卓浮动基质片:制剂和体内外评价。
背景:盐酸地尔硫卓是一种钙通道阻滞剂,其血浆消除半衰期为 4.4 ± 1.3 h,且吸收窗口较窄。因此,本研究旨在制备一种胃复安浮动基质片剂:方法:采用直接压片法制备片剂。以羟丙基甲基纤维素 K100M(HPMC K 100M)和碳酸氢钠的用量为自变量,1 小时、6 小时、12 小时的累积释放百分比和浮滞时间为因变量,采用 32 因子设计进行优化:结果:HPMC K100M 和碳酸氢钠的用量越高,效果越好。对优化后的制剂进行了差示扫描量热法、雄性白化兔体内胃保留率、动力学模型和稳定性研究评估。体内研究表明,片剂在健康雄性白化兔体内的胃保留时间长达 6 小时。稳定性研究表明,药物的浮力和释放曲线没有明显变化:从这项研究中可以得出结论:成功制备了胃保留型盐酸地尔硫卓浮动基质片剂,并在兔子胃内保留了长达 6 小时,而且在加速稳定性研究中表现稳定。
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