Stability of tacrolimus ophthalmic solution
Stability of tacrolimus ophthalmic solution
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DOI：
10.2146/ajhp160169
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发表时间：
2017-07-01
影响因子：
2.7
通讯作者：
Alos-Alminana, Manuel
中科院分区：
文献类型：
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作者：
Ezquer-Garin, Carlos;Ferriols-Lisart, Rafael;Alos-Alminana, Manuel
目的。研究了0.3mg/mL他克莫司滴眼液在不同储存温度下的稳定性。方法。通过在滴眼剂中稀释他克莫司，在无菌条件下制备一式三份的 0.3 mg/mL 他克莫司的无菌眼用溶液。将三份该溶液转移到聚丙烯瓶中，并在 25、2-8 或 -15 至 -25 摄氏度下保存。制备后立即在选定的时间点收集样品，并使用高效液相色谱 (HPLC) 一式三份进行测定。还目视检查样品的宏观变化。 0.3 mg/mL 他克莫司溶液也经过酸处理和加热，以强制其降解并评估分析方法的选择性。如果通过 HPLC 分析时仍保留至少 90% 的平均初始浓度，则认为他克莫司眼用溶液是稳定的。结果。当储存在 2-8 摄氏度和 -15 至 -25 摄氏度之间时，在整个 85 天的研究期间至少保留了初始他克莫司浓度的 90%。起点和终点之间他克莫司浓度没有显着差异 (p > 0.05)。然而，当他克莫司溶液在25℃保存时，第28天时他克莫司初始浓度剩余百分比已降至90％以下。结论。在滴眼液中稀释至 0.3 mg/mL 的他克莫司在 25°C 下保存时可稳定 20 天，在 2-8°C 或 15 至 -25°C 的聚丙烯瓶中避光保存时可稳定至少 85 天。
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 degrees 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 degrees C and between -15 and -25 degrees 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 degrees 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 degrees C and for at least 85 days when stored at 2-8 degrees C or between- 15 and -25 degrees C in polypropylene bottles and protected from light.