کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10127912 | 1645111 | 2018 | 30 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Establishment of a quantitative bioanalytical method for an acetylcholinesterase inhibitor Ethyl 3-(2-(4-fluorophenyl) amino)-4-phenylthiazol-5-yl)-3-oxopropanoate including its physicochemical characterization and in vitro metabolite profiling using Liqu
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آنالیزی یا شیمی تجزیه
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Ethyl 3-(2-(4-fluorophenyl)amino)-4-phenylthiazo)-5-yl)-3-oxopropanoate is a novel molecule with potent acetylcholinesterase inhibition property. In this research, we have developed a rapid and selective RP-HPLC bioanalytical method for quantitative measurement of the molecule. The method has been validated following the USFDA bioanalytical method validation guideline. In addition, as a part of drug development, in vitro metabolite identification has also been performed. A Kromasil C18 column was used in eluting the molecule chromatographically. The optimized mobile phase was composed of a mixture of acetonitrile and 10â¯mM ammonium formate buffer (pHâ¯4.6) in 70:30 ratio (v/v). The response of the molecule was found to be linear over a calibration range of 0.2â¯Î¼g/mL to 12â¯Î¼g/mL. The inter-day and intra-day accuracy of the method ranged from 89.95% to 101.90% and 99.84% to 104.08%, respectively. On the other hand, the precision (%CV) value for inter-day was in between 3.50% to 6.91% and for intra-day, it was 2.11% to 8.03%. The mean recovery of the molecule at three different quality control levels was more than 85%. The analyte was stable under different stability conditions including 12â¯h autosampler, 8â¯h bench top, 15â¯days long term at â20â¯Â°C and three freeze-thaw cycles. The method was applied to determine stability of the molecule in human plasma. The molecule was found to be stable with more than 90% remaining even after 120â¯min of incubation in plasma. Two metabolites each in rat liver microsome and human liver microsome has been identified.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Chromatography B - Volume 1096, 1 October 2018, Pages 214-222
Journal: Journal of Chromatography B - Volume 1096, 1 October 2018, Pages 214-222
نویسندگان
Kavya Sri Nemani, Amit Shard, Pinaki Sengupta,