Roseman University of Health Sciences, College of Pharmacy, South Jordan, Utah.
Division of Clinical Pharmacology, School of Medicine, University of Utah.
Int J Pharm Compd. 2024 May-Jun;28(3):246-248.
Amiloride is a U.S. Food and Drug Administration-approved diuretic agent used to treat hypertension and congestive heart failure. Recent human and animal studies have suggested that amiloride may also have a role in treating anxiety through its acid-sensing ion channel antagonism. Intranasal administration of amiloride nasal spray via an extemporaneously compounded preparation has the potential for rapid delivery to the site of action to achieve therapeutic outcomes in individual patients with anxiety disorders. However, these patient-specific preparations do not have the pre-formulation characterization, including chemical stability, that conventional manufactured dosage forms have. The objective of this study was to assess the estimated chemical stability of compounded amiloride nasal spray over 6 months and 12 months utilizing accelerated degradation with high heat and the Arrhenius equation. A stability-indicating highperformance liquid chromatography analytical method was employed at appropriate intervals over a 12-month period to reveal that amiloride remained chemically stable over the period tested and by extrapolation. Physical stability and compatibility with the preservative benzyl alcohol were also confirmed via visual inspection, pH monitoring, and measurement of turbidity.
阿米洛利是一种获得美国食品和药物管理局批准的利尿剂，用于治疗高血压和充血性心力衰竭。最近的人体和动物研究表明，阿米洛利通过其酸感应离子通道拮抗作用，也可能在治疗焦虑方面发挥作用。通过临时配制的制剂经鼻内给予阿米洛利鼻喷雾剂，有可能迅速将药物递送至作用部位，从而在患有焦虑症的个体患者中实现治疗效果。然而，这些针对特定患者的制剂没有经过预配方特性（包括化学稳定性）的研究，而常规制造的剂型则具有这些特性。本研究的目的是利用高温加速降解和阿仑尼乌斯方程，评估在 6 个月和 12 个月期间临时配制的阿米洛利鼻喷雾剂的估计化学稳定性。在 12 个月的时间内，采用稳定性指示高效液相色谱分析方法在适当的时间间隔进行检测，结果表明阿米洛利在测试期间和推断期间保持化学稳定。通过目视检查、pH 值监测和浊度测量，还确认了物理稳定性以及与防腐剂苯甲醇的相容性。
