润滑剂对不同生物制药分类系统抗高血压药物常规片剂性能的影响

Dindawar Kavita, B.M Supriya, Kolageri Shivanand
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引用次数: 0

摘要

背景:高血压是动脉血压升高的一种长期病症。高血压会导致冠状动脉疾病、中风、心力衰竭、肾脏疾病等。 目标:本研究旨在找出润滑剂对含有不同 BCS 类抗高血压药物的常规片剂性能的影响。我们选择了琥珀酸美托洛尔和阿替洛尔等分别代表 BCS I 级和 II 级的抗高血压药物。 方法:润滑剂是所有固体制剂的基本成分。亲水性润滑剂富马酸硬脂钠与传统的疏水性润滑剂硬脂酸镁进行了比较。使用富马酸硬脂钠或硬脂酸镁作为 1%或 2%的润滑剂,通过直接压缩或湿法制粒技术制备无包衣片剂,润滑剂的混合时间分别为 3 分钟和 6 分钟。 结果无论药物类别、浓度、混合时间和加工方法如何,作为片剂润滑剂,硬脂富马酸钠都比硬脂酸镁有效。当使用较低浓度和较短混合时间时,两种润滑剂都能产生较好的片剂特性。将硬脂富马酸钠和硬脂酸镁(1%,3 分钟)在 400±20C/75% 相对湿度下贮存 90 天,以检查老化和贮存的影响。 得出结论:根据贮藏期结束时对不同片剂特性的调查,没有观察到明显的变化。
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Effect of Lubricants on Properties of Conventional Tablets of Antihypertensive Drugs from Different Biopharmaceutical Classification System
Background: Hypertension is a long-term medical condition in which blood pressure in the arteries is elevated. Hypertension causes coronary artery disease, stroke, heartfailure; kidney diseases etc.to over come hypertension, antihypertensive drugs are used. Objectives: The aim of present work was to find out effectsof lubricants on properties of conventionaltablets containing antihypertensive drugs from different BCS class. Antihypertensive drugs suchas Metoprolol succinate, and Atenolol were selected which represented BCS class I, and II respectively. Methods: Lubricants are the essential components of all solid dosage forms. Sodium stearyl fumarate, a hydrophilic lubricant was compared with Magnesium stearate,a conventional hydrophobic lubricant. Uncoatedtabletswereprepared either by direct compression or wet granulation technique employing sodium stearyl fumarate or magnesium stearate as a lubricant at 1% or 2%, mixing time of lubricants was varied as 3 and 6mins. Results: Irrespective of class of drug, concentration, mixing time and processing method sodium stearyl fumarate turned out to be effective as tablet lubricant than Magnesium stearate. Both the Lubricants, when used at lower concentration and shorter mixing time resulted in superior tablets properties.Direc tcompression method gave better results than wet granulation technique. Both Sodium stearyl fumarate and Magnesium stearate (1%, 3min) were subjected to storage at400± 20C/ 75% RH for 90 days to check effect of aging and storage. Conclusion: According to at the end of storage period up on investigating for different tablet properties there were no significan tchanges observed.
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