Dyer Ann Margaret, Smith Alan
PharmaSci Consulting Limited, Nottingham, UK.
Drug Des Devel Ther. 2016 Dec 22;11:59-64. doi: 10.2147/DDDT.S123776. eCollection 2017.
The aim of the present work is to extensively evaluate the pharmaceutical attributes of currently available riluzole presentations. The article describes the limitations and risks associated with the administration of crushed tablets, including the potential for inaccurate dosing and reduced rate of absorption when riluzole is administered with high-fat foods, and the advantages that a recently approved innovative oral liquid form of riluzole confers on amyotrophic lateral sclerosis (ALS) patients. The article further evaluates the patented and innovative controlled flocculation technology used in the pseudoplastic suspension formulation to reduce the oral anesthesia seen with crushed tablets, resulting in optimized drug delivery for riluzole. Riluzole is the only drug licensed for treating ALS, which is the most common form of motor neurone disease and a highly devastating neurodegenerative condition. The licensed indication is to extend life or the time to mechanical ventilation. Until recently, riluzole was only available as an oral tablet dosage form in the UK; however, an innovative oral liquid form, Teglutik 5 mg/mL oral suspension, is now available. An oral liquid formulation provides an important therapeutic option for patients with ALS, >80% of who may become unable to swallow solid oral dosage forms due to disease-related dysphagia. Prior to the launch of riluzole oral suspension, the only way for many patients to continue to take riluzole as their disease progressed was through crushed tablets. A novel suspension formulation enables more accurate dosing and consistent ongoing administration of riluzole. There are clear and important advantages such as enhanced patient compliance compared with crushed tablets administered with food or via an enteral feeding tube and the potential for an improved therapeutic outcome and enhanced quality of life for ALS patients.
本研究的目的是广泛评估目前可用的利鲁唑制剂的药学属性。本文描述了服用碾碎片剂的局限性和风险,包括给药剂量不准确的可能性以及利鲁唑与高脂食物一起服用时吸收速率降低的情况,还阐述了最近获批的创新型利鲁唑口服液体制剂赋予肌萎缩侧索硬化症(ALS)患者的优势。本文进一步评估了用于假塑性混悬液制剂的专利创新型控制絮凝技术,该技术可减少碾碎片剂时出现的口腔麻醉现象,从而实现利鲁唑的优化给药。利鲁唑是唯一被批准用于治疗ALS的药物,ALS是运动神经元病最常见的形式,是一种极具破坏性的神经退行性疾病。其获批的适应证是延长生命或延长至需要机械通气的时间。直到最近,在英国利鲁唑仅有口服片剂剂型;然而,现在有一种创新型口服液体制剂,即5mg/mL的Teglutik口服混悬液可供使用。口服液体制剂为ALS患者提供了一种重要的治疗选择,超过80%的ALS患者可能因疾病相关的吞咽困难而无法吞咽固体口服剂型。在利鲁唑口服混悬液推出之前,许多患者在疾病进展时继续服用利鲁唑的唯一方法是服用碾碎的片剂。一种新型混悬液制剂能够实现更准确的给药以及利鲁唑的持续稳定给药。与与食物一起服用或通过肠内喂养管服用碾碎片剂相比,新型混悬液制剂具有明显且重要的优势,例如提高患者依从性,还有可能改善治疗效果并提高ALS患者的生活质量。