磷酸川芎嗪透皮贴含量均匀度及释放度测定  

Determination of content uniformity and in vitro release of tetramethylpyrazine phosphate transdermal patch

作　　者：安佃云 贺亚静[1,2] 张建芳[1] 翁伟宇[1] 李伟[2] 沈腾[1] 徐惠南[1] 

机构地区：[1]复旦大学药学院药剂学教研室,智能化递药教育部重点实验室,上海201203 [2]山东中医药大学药学院,济南250355

出　　处：《药物分析杂志》2014年第11期2087-2090,共4页Chinese Journal of Pharmaceutical Analysis

摘　　要：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,appendixⅩ D,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.

关 键 词：磷酸川芎嗪 含量均匀度 高效液相色谱法 透皮贴剂 体外释放度 体内吸收分数 体内体外相关性 

分 类 号：R917[医药卫生—药物分析学]