丁丙诺啡透皮贴剂在释放度测定中桨碟法与转筒法的差异

目的: 对透皮贴剂释放度测定中转筒法装置与中国药典桨碟法装置进行比较。 方法: 分别使用转筒法装置与中国药典桨碟法装置对丁丙诺啡透皮贴剂的释放曲线进行测定,释放介质为0.9%的氯化钠溶液900 mL;以TC-C₁₈ 为固定相的Agilent色谱柱(250 mm×4.6 mm,5 μm),0.05 mol·L^-1 的磷酸二氢钾溶液与乙腈的混合溶液(1.3∶ 1)为流动相,流速为1.0 mL·min^-1 ,柱温为30 ℃,检测波长为220 nm。 结果: 丁丙诺啡在0.4~24 μg·mL^-1 范围内线性关系良好(r=0.9999),回收率为102.1%。对于20 mg规格的透皮贴剂采用不同方法所得的丁丙诺啡释放曲线不存在差异,而对于5 mg规格和10 mg规格则存在差异。 结论: 中国药典桨碟法装置在测量透皮贴剂的释放度时不能完全替代美国药典转筒法装置。

Objective: To compare the difference between the methods of cylinder and paddle over disk used in the release test of transdermal drug deliver system. Method: The cylinder and paddle over disk method were used respectively to test buprenorphine transdermal patches with the release media of 900 mL of 0.9% sodium chloride solution.Agilent column which packed TC-C₁₈ as solid phase (250 mm×4.6 mm,5 μm) and the mixture of acetonitrile and 0.05 mol·L^-1 potassium dihydrogen phosphate solution(1∶ 1.3)as mobile phase were adoptd.The flow rate was 1.0 mL·min^-1.The column temperature was kept at 30 ℃ and the detective wave length was 220 nm. Result: The linear correlation of buprenorphine was observed from the concentrations of 0.4-24 μg·mL^-1 (r=0.9999).The recovery of buprenorphine was 102.1%.There were not difference between the methods of cylinder and paddle over disk used in the release test of transdermal drug deliver system in testing 20 mg of buprenorphine transdermal patches,while there existed difference in testing 5 mg and 10 mg of buprenorphine transdermal patches. Conclusion: There will be error when testing large area patch with paddle over disk method.