在体外对品牌与通用rivaroxaban抗凝剂效果进行比较的研究
Karl Mangion1, Kevin Vella2, Alex Gatt3
1Department of Applied Biomedical Science, Faculty of Health Sciences, University of Malta, Msida, Malta.
Thrombosis research
|January 31, 2024
概括
品牌和通用里瓦罗克萨班在体外显示出相同的抗凝剂作用. 这项研究证实,在凝血试验中,里瓦洛克萨班配方的疗效相当.
科学领域:
- 药理学 药理学是指药理学的学科.
- 血液学 血液学 血液学
- 分析化学 分析化学
背景情况:
- 现在可以获得通用里瓦罗克萨班配方,旨在与品牌产品互换使用.
- 没有先前的研究直接比较了品牌与通用rivaroxaban的体外抗凝效应.
- 这项研究旨在评估品牌 (Xarelto®) 和两种通用 (Rivarolto®,Rivaroxaban Sandoz®) 里瓦洛克萨班配方的体外抗凝活性.
研究的目的:
- 为了比较品牌和通用rivaroxaban的体外抗凝作用.
- 评估利瓦洛克萨班度对各种凝血试验的影响.
- 为了确定仿制的里瓦罗克萨班配方是否与品牌版本具有可比的抗凝剂活性.
主要方法:
- 三种里瓦罗克萨班配方 (品牌和两种仿制药) 在聚合正常血中进行了测试.
- 里瓦罗克萨班度 (50-750 ng/ml) 用校准的抗Xa测定测量,并通过UHPLC-MS/MS.确认.
- 凝血试验包括PT,aPTT,dRVVT,TT,克劳斯纤维素,因子VII,VIII,IX试验,以及血栓形成显微镜.
主要成果:
- 所有三种里瓦洛克萨班配方的度增加都显示出与PT,aPTT和dRVVT有很强的正相关性.
- 在因子VII,VIII和IX试验中观察到强烈的负相关性.
- 在可比度的品牌和通用里瓦洛克萨班之间的凝血测定结果中没有发现显著差异.
结论:
- 品牌和仿制的里瓦罗克萨班配方在体外表现出相当于抗凝剂效果.
- 这项研究支持基于体外凝血概况的里瓦洛克萨班配方可互换使用.
- 在这种体外评估中,里瓦罗克萨班的抗凝剂活性在不同配方中是一致的.
相关概念视频
Anticoagulant Drugs: Vitamin K Antagonists and Direct Oral Anticoagulants
1.2K
Oral anticoagulants are vital tools in preventing and treating blood clotting disorders. This diverse class of medications can be categorized as vitamin K antagonists, exemplified by warfarin, and direct thrombin inhibitors (DTIs), such as dabigatran, as well as factor Xa inhibitors, including rivaroxaban.
Warfarin, a prominent vitamin K antagonist family member, exerts its effect by inhibiting the enzyme VKORC1 (vitamin K epoxide reductase complex 1). By hindering this enzyme, warfarin...
Warfarin, a prominent vitamin K antagonist family member, exerts its effect by inhibiting the enzyme VKORC1 (vitamin K epoxide reductase complex 1). By hindering this enzyme, warfarin...
1.2K
Anticoagulant Drugs: Low-Molecular-Weight Heparins
698
Hemostasis is a crucial process that prevents excessive blood loss from damaged blood vessels. It involves various mechanisms such as vasoconstriction, platelet adhesion and activation, and fibrin formation. The importance of each mechanism depends on the type of vessel injury. In contrast, thrombosis is the abnormal formation of a blood clot within the blood vessels, leading to potential complications if the clot obstructs blood flow. Thrombosis can be caused by increased coagulability of the...
698
Therapeutic Index
4.3K
The therapeutic index of a drug is a key parameter in pharmacology that quantifies the relative safety of a drug by calculating the ratio between the dose that causes toxicity in half the population (50%) to the dose that proves to be effective for half the population (50%). It provides a spectrum of doses for a particular drug ranging from effective to potentially toxic. To illustrate, consider an anticoagulant agent like warfarin. It possesses a narrow window within its therapeutic index to...
4.3K
Bioequivalence: Overview
1.0K
Pharmaceutical equivalents, by definition, are drug products with the same active ingredient in the same quantities, encapsulated in identical dosage forms, and intended for the same administration routes. These pharmaceutical equivalents are deemed bioequivalent if the bioavailability of the active entity in the drug preparations is similar. Moreover, pharmaceutical equivalents demonstrating bioequivalence are also regarded as therapeutically equivalent. This means that when used as directed,...
1.0K
Antiplatelet Drugs: Prostaglandin Synthesis, P2Y12 and Glycoprotein IIb/IIIa Inhibitors
525
Antiplatelet drugs emerge as frontline defenders against the insidious threat of thromboembolic diseases, where abnormal clots obstruct vital blood vessels. These drugs stand as bulwarks, inhibiting platelet aggregation and clot formation, thereby mitigating the risk of life-threatening conditions like myocardial infarction, coronary artery disease, and thrombotic strokes.
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
Prostaglandin synthesis inhibitors, exemplified by the widely known aspirin, wield their power by irreversibly acetylating...
525


