Physical and chemical stability of esomeprazole sodium solutions

• Published in: The Annals of pharmacotherapy Vol. 42; no. 9; p. 1247
• Main Authors: Kupiec, Thomas C, Aloumanis, Vasileios, Ben, Michel, Trissel, Lawrence A, Chan, Pak, Patterson, Joe
• Format: Journal Article
• Language: English
• Published: United States 01.09.2008
• Subjects: Anti-Ulcer Agents - chemistry; Drug Stability; Drug Storage; Esomeprazole - chemistry; Glucose - chemistry; Humans; Isotonic Solutions - chemistry; Omeprazole - chemistry; Polyvinyl Chloride - chemistry; Sodium Chloride - chemistry; Solutions - chemistry; Time Factors
• ISSN: 1542-6270
• DOI: 10.1345/aph.1L079

Esomeprazole sodium (Nexium IV, AstraZeneca) is the S-isomer of omeprazole and acts as a proton pump inhibitor gastric antisecretory agent indicated for the short-term treatment of gastroesophageal reflux disease in patients with a history of erosive esophagitis. Currently, there is no information on the long-term stability of esomeprazole sodium in infusion solutions beyond 12 hours. To evaluate the stability of esomeprazole sodium in 5% dextrose, 0.9% sodium chloride, and lactated Ringer's injection, at 2 concentrations, at room temperature and when refrigerated. Triplicate samples of esomeprazole 0.4 and 0.8 mg/mL as the sodium salt were prepared in the solutions required. Stability evaluations were performed initially, over 2 days stored at 23 degrees C, and over 5 days stored at 4 degrees C. Physical stability was assessed using turbidimetric and particulate measurement, as well as visual observation. Chemical stability was evaluated by stability-indicating high-performance liquid chromatography. The samples in all 3 infusion solutions were physically stable throughout the study. None of the samples had evidence of visible haze or particulates. Most samples developed a slight yellow discoloration within 24 hours, but this discoloration was not accompanied by an excessive loss of drug content. The esomeprazole sodium samples in all 3 infusion solutions exhibited less than 7% loss over 2 days at 23 degrees C and over 5 days at 4 degrees C. Esomeprazole 0.4 and 0.8 mg/mL as the sodium salt in the infusion solutions tested is chemically and physically stable for at least 2 days at room temperature and 5 days under refrigeration.