Stability of tacrolimus ophthalmic solution.
PURPOSE
The stability of 0.3-mg/mL tacrolimus ophthalmic solution at different storage temperatures was studied.


METHODS
A sterile ophthalmic solution of 0.3 mg/mL tacrolimus was prepared in triplicate under aseptic conditions by diluting tacrolimus in eye drops. Three aliquots of this solution were transferred into polypropylene bottles and stored at 25, 2-8, or -15 to -25 °C. Samples were collected immediately after preparation and at selected time points and assayed in triplicate using high-performance liquid chromatography (HPLC). Samples were also visually examined for macroscopic changes. The 0.3-mg/mL tacrolimus solution was also exposed to acidic treatment and heat to force its degradation and to evaluate the selectivity of the analytic method. The tacrolimus ophthalmic solution was considered stable if at least 90% of the mean initial concentration remained when analyzed by HPLC.


RESULTS
When stored at 2-8 °C and between -15 and -25 °C, at least 90% of the initial tacrolimus concentration remained throughout the 85-day study period. There were no significant differences in tacrolimus concentrations between the starting and ending points (p > 0.05). However, when tacrolimus solution was stored at 25 °C, the percentage of the initial tacrolimus concentration remaining had decreased to less than 90% on day 28.


CONCLUSION
Tacrolimus diluted to 0.3 mg/mL in eye drop solution was stable for 20 days when stored at 25 °C and for at least 85 days when stored at 2-8 °C or between -15 and -25 °C in polypropylene bottles and protected from light.
['Ezquer-Garin|Carlos|C|', 'Ferriols-Lisart|Rafael|R|', 'Alós-Almiñana|Manuel|M|']
D060433:Administration, Ophthalmic D002851:Chromatography, High Pressure Liquid D004355:Drug Stability D004356:Drug Storage D006801:Humans D007166:Immunosuppressive Agents D009883:Ophthalmic Solutions D019999:Pharmaceutical Solutions D016559:Tacrolimus D013696:Temperature
tacrolimus ophthalmic solutions drug stability