水分对阿莫西林克拉维酸钾颗粒稳定性的影响

Influence of Moisture on Stability of Amoxicillin and Potassium Clavulanate Granules

目的根据颗粒剂的制剂特点,探讨水分(包括水分含量和水分活度)对阿莫西林克拉维酸钾颗粒稳定性的影响;并以稳定性为指针,揭示阿莫西林克拉维酸钾颗粒在制剂过程中的关键质量控制属性。方法通过高湿加速稳定性实验[实验温度(25±2)℃;相对湿度(75±5)%],考察阿莫西林克拉维酸钾颗粒的水分、含量、有关物质、晶型特征等。结果阿莫西林克拉维酸钾颗粒的稳定性与样品的水分活度呈正相关,与样品的水分含量关系不大,水分活度低的样品的稳定性高。结论阿莫西林克拉维酸钾颗粒的关键质控属性是水分,关键工艺参数是水分活度。

OBJECTIVE To investigate the influence of moisture including water content and water activity on the stability of amoxicillin and potassium clavulanate granules according to the characteristics of the granules, and reveal the key quality control prop- erty in the preparation process with stability as an indicator. METHODS Under the condition of （25 ± 2）℃ and （75± 5 ）% RH, the water content, active ingredient contents, related substances and characteristics of crystal form of amoxicillin and potassium clavu- lanate granules were studied. RESULTS The stability of amoxicillin and clavulante potassium granules was positively correlated with water activity in the samples, but was not related to water content closely. The sample with lower water activity was of higher stability. CONCLUSION The key quality control property of amoxicillin and potassium clavulanate granules is the moisture, and the key process parameter in the preparation is the water activity.