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顺序注射分析用于药物释放曲线的自动化和评估:克霉唑释放监测。

Sequential Injection Analysis for Automation and Evaluation of Drug Liberation Profiles: Clotrimazole Liberation Monitoring.

机构信息

Department of Analytical Chemistry, Faculty of Pharmacy in Hradec Králové, Charles University, 500 05 Hradec Králové, Czech Republic.

Contipro a.s., 561 02 Dolní Dobrouč, Czech Republic.

出版信息

Molecules. 2021 Sep 12;26(18):5538. doi: 10.3390/molecules26185538.

Abstract

A fully automated sequential injection system was tested in terms of its application in liberation testing, and capabilities and limitations were discussed for clotrimazole liberation from three semisolid formulations. An evaluation based on kinetic profiles obtained in short and longer sampling intervals and steady-state flux values were applied as traditional methods. The obtained clotrimazole liberation profile was faster in the case of Delcore and slower for Clotrimazol AL and Canesten cream commercial formulations. The steady-state flux values for the tested formulations were 52 µg cm h for Canesten, 35 µg cm h for Clotrimazol AL, and 7.2 µg cm h for Delcore measured in 4 min sampling intervals. A simplified approach for the evaluation of the initial rate based on the gradient between the second and third sampling points was used for the first time and was found to correspond well with the results of the conventional methods. A comparison based on the ratio of the steady-state flux and the initial rate values for Canesten and Clotrimazol AL proved the similarity of the obtained results. The proposed alternative was successfully implemented for the comparison of short-term kinetic profiles. Consequently, a faster and simpler approach for dissolution/liberation testing can be used.

摘要

本文测试了一种全自动顺序注射系统在释放测试方面的应用,并讨论了其在从三种半固体制剂中释放克霉唑方面的能力和局限性。基于在较短和较长采样间隔以及稳态通量值获得的动力学曲线进行评估,这些方法是传统方法。在 Delcore 的情况下,获得的克霉唑释放曲线更快,而在 Clotrimazol AL 和 Canesten 乳膏商业制剂的情况下则更慢。在 4 分钟采样间隔下,测试制剂的稳态通量值分别为 52 µg cm h 用于 Canesten、35 µg cm h 用于 Clotrimazol AL 和 7.2 µg cm h 用于 Delcore。首次使用基于第二和第三采样点之间梯度的初始速率简化评估方法,并且与传统方法的结果非常吻合。基于稳态通量与初始速率比值的 Canesten 和 Clotrimazol AL 的比较证明了所得结果的相似性。所提出的替代方法成功地用于比较短期动力学曲线。因此,可以使用更快、更简单的方法进行溶解/释放测试。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7ba3/8467677/43a49423f637/molecules-26-05538-g001.jpg

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