Petró É, Paál T L, Erős I, Kenneth A S, Baki G, Csóka I
Institute of Drug Regulatory Affairs and.
Pharm Dev Technol. 2015 May;20(3):330-6. doi: 10.3109/10837450.2013.867446. Epub 2013 Dec 13.
The aim of the present work was to extend our previous in-vitro drug release studies using semisolid dermatological bases with non-impregnated cellulose acetate membranes. A comparison of the performances of two apparatuses, the more commonly used Franz cell and the new modified USP (mini paddle with ointment holding cell) systems were applied to this work. Five different semisolid as well as two marketed preparations containing 1% diclofenac sodium were used. Complex, slightly non-linear release curves indicating sink conditions were found. This was explained by the co-diffusion of excipients modifying the characteristics of the membrane and the receiving medium dynamically. Although our test model is, as a rule, not suitable to establish an in-vivo-in-vitro correlation, good qualitative as well as quantitative correlations were found within some types of dermatological bases. The correlation between the results of the two in-vitro methods also depends on the type of semisolids studied. The release curve characteristics and the amount of diclofenac sodium released at 6 h were measured. Their repeatability and reproducibility were calculated. The slopes and Q-values were correlated with in-vivo data. In general, the modified USP method provided more precise results than the Franz cell method.
本研究的目的是扩展我们之前使用含未浸渍醋酸纤维素膜的半固体皮肤病学基质进行的体外药物释放研究。将两种装置（更常用的Franz扩散池和新型改良的美国药典系统（带软膏容纳池的微型搅拌桨））的性能进行比较，并应用于本研究。使用了五种不同的半固体以及两种含有1%双氯芬酸钠的市售制剂。发现了表明漏槽条件的复杂、略呈非线性的释放曲线。这可以通过辅料的共同扩散来解释，辅料动态地改变了膜和接收介质的特性。虽然我们的测试模型通常不适合建立体内-体外相关性，但在某些类型的皮肤病学基质中发现了良好的定性和定量相关性。两种体外方法结果之间的相关性也取决于所研究的半固体类型。测量了释放曲线特征以及双氯芬酸钠在6小时时的释放量。计算了它们的重复性和再现性。将斜率和Q值与体内数据进行关联。总体而言，改良的美国药典方法比Franz扩散池法提供了更精确的结果。
