磷酸川芎嗪透皮贴含量均匀度及释放度测定

目的: 测定磷酸川芎嗪透皮贴中川芎嗪(2,3,5,6-tetramethylpyrazine,TMP)含量均匀度及释放度. 方法: 建立HPLC法测定贴剂中川芎嗪含量均匀度;按照中国药典附录ⅩD释放度测定法第三法测定贴剂的释放度. 结果: HPLC法测定川芎嗪含量的准确度和精密度良好.3批中试样品的含量均匀度均符合药典规定.贴剂释药曲线符合Higuchi方程;通过测定6批中试样品的释放度,确定本品在2、12和24 h的释放限度应分别为标示量的8%~30%、40%~75%和60%以上.贴剂体外释放度与体内吸收分数具有良好的相关性. 结论: 磷酸川芎嗪透皮贴制备工艺重演性好;建立的含量均匀度和释放度测定方法可用于贴剂的质量控制.

Objective: To determine the content uniformity and in vitro release of tetramethylpyrazine phosphate transdermal patch. Methods: HPLC method was established to determine the content uniformity of 2,3,5,6-tetramethylpyrazine(TMP) in transdermal patch.The release method apparatus (Chinese Pharmacopeia 2010,appendix ⅩD,method 3) was employed to assess the release of TMP from transdermal patch. Results: The established HPLC method was accurate,precise and stable.The content uniformity of 3 batches of pilot samples met the requirements of Chinese pharmacopoeia.The release rate profiles followed the Higuchi equation.Based on the release test of six batches,the 2-hour,12-hour and 24-hour cumulative release of TMP accounted for 8%-30%,40%-75% and more than 60% of the labelled amount,respectively.A good correlation of in vitro release and in vivo absorption could be obtained by means of the Loo-Riegelman method. Conclusion: Tetramethylpyrazine phosphate transdermal patches were prepared with good process repeatability.The methods established for content uniformity and release test could be used for quality control.