Physical and chemical stability of esomeprazole sodium solutions.
BACKGROUND
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.


OBJECTIVE
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.


METHODS
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.


RESULTS
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.


CONCLUSIONS
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.
Kupiec
Thomas C
TC
Analytical Research Laboratories, Oklahoma City, OK, USA.
Aloumanis
Vasileios
V
Ben
Michel
M
Trissel
Lawrence A
LA
Chan
Pak
P
Patterson
Joe
J
D000897:Anti-Ulcer Agents / Q000737:chemistry*; D004355:Drug Stability; D004356:Drug Storage; D064098:Esomeprazole / Q000737:chemistry*; D005947:Glucose / Q000737:chemistry; D006801:Humans; D007552:Isotonic Solutions / Q000737:chemistry; D009853:Omeprazole / Q000737:chemistry; D011143:Polyvinyl Chloride / Q000737:chemistry; D000077325:Ringer's Lactate; D012965:Sodium Chloride / Q000737:chemistry; D012996:Solutions / Q000737:chemistry; D013997:Time Factors
D000897:Anti-Ulcer Agents; D007552:Isotonic Solutions; D000077325:Ringer's Lactate; D012996:Solutions; D012965:Sodium Chloride; D011143:Polyvinyl Chloride; D005947:Glucose; D009853:Omeprazole; D064098:Esomeprazole