Fixed combination of rivaroxaban and Aspirin: Tablet formulation and analytical method validation

IF 4.1 Q1 CHEMISTRY, ANALYTICAL Talanta Open Pub Date : 2024-02-26 DOI:10.1016/j.talo.2024.100298

Hani Naseef , Mosab Afaneh , Moammal Qurt , Abdullah Rabba , Abdallah Abukhalil , Numan Malkieh , Maher Kharouf , Ramzi Moqadi

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Abstract

Rivaroxaban and aspirin are commonly used antithrombotic agents in combination to prevent coronary artery disease (CAD) and atherothrombotic events in adult patients after acute coronary syndrome (ACS) with elevated cardiac biomarkers, or with coronary artery disease (CAD) or symptomatic peripheral artery disease (PAD) in high-risk patients. The recommended dosage is 2.5 mg rivaroxaban twice daily in combination with 75–100 mg aspirin once daily. This study aimed to develop a fixed-dose combination tablet of rivaroxaban (2.5 mg) and aspirin (50 mg) to enhance medication adherence and decrease pill burden.

Compatibility studies were conducted on the active ingredients to develop the product formula. The formula and the manufacturing procedure were chosen based on the risk assessment for each active substance, wet granulation with both actives intragranular was found to have faster dissolution than direct mix formulae. Furthermore, a validated reverse-phase HPLC stability indicator method was developed to detect APIs and their possible degradants.

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利伐沙班和阿司匹林的固定复方制剂：片剂配方和分析方法验证

利伐沙班和阿司匹林是常用的联合抗血栓药物，用于预防急性冠状动脉综合征（ACS）后心脏生物标志物升高的成年患者、冠状动脉疾病（CAD）或无症状外周动脉疾病（PAD）高危患者的冠状动脉疾病（CAD）和动脉粥样硬化血栓事件。推荐剂量为 2.5 毫克利伐沙班，每天两次，联合 75-100 毫克阿司匹林，每天一次。本研究旨在开发一种利伐沙班（2.5 毫克）和阿司匹林（50 毫克）的固定剂量复方片剂，以提高服药依从性并减少药片负担。根据对每种活性物质的风险评估结果，选择了配方和生产程序，发现将两种活性物质粒内湿法制粒比直接混合配方溶解更快。此外，还开发了一种经过验证的反相高效液相色谱稳定性指标法，用于检测原料药及其可能的降解剂。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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