Spencer John A, Gao Zongming, Moore Terry, Buhse Lucinda F, Taday Philip F, Newnham David A, Shen Yaochun, Portieri Alessia, Husain Ajaz
U.S. Food & Drug Administration, Division of Pharmaceutical Analysis, 1114 Market Street, St. Louis, Missouri 63101, USA.
J Pharm Sci. 2008 Apr;97(4):1543-50. doi: 10.1002/jps.21051.
Delayed release dosage forms such as Asacol employ coatings that are engineered to breakdown and release the drug topically at the nominal pH of the lower intestinal tract. Asacol tablets were found to dissolve in an erratic fashion when they are dissolved in buffers below pH 7 which can occur naturally. In this study Terahertz pulsed imaging (TPI) was used to accurately map the coating thickness of a group of Asacol tablets that were subsequently dissolved using the USP method at pH 6.8. The mean dissolution times were found to correlate with the average coating thickness measured over all surfaces. Thickness values for a single randomly selected face did not correlate well with the dissolution results. The speed and ease of TPI mapping may make it an attractive replacement for wet dissolution testing both in product development and eventually for process analysis.
诸如艾克沙尔（Asacol）之类的缓释剂型采用的包衣经过设计，可在肠道下段的标称pH值下局部分解并释放药物。当艾克沙尔片剂溶解在pH值低于7的缓冲液中时，发现其溶解方式不稳定，而pH值低于7的情况在自然条件下可能会出现。在本研究中，使用太赫兹脉冲成像（TPI）精确绘制了一组艾克沙尔片剂的包衣厚度，随后按照美国药典方法在pH 6.8条件下溶解这些片剂。发现平均溶解时间与在所有表面上测量的平均包衣厚度相关。单个随机选择面的厚度值与溶解结果的相关性不佳。TPI测绘的速度和便捷性可能使其在产品开发以及最终的过程分析中成为湿溶出度测试的有吸引力的替代方法。
