Abstract:
:A sensitive (10 ng/mL) and specific high-performance liquid chromatographic (HPLC) assay, with electrochemical (EC) detection, for the geometric isomers of 3-hydroxy-N-(2-phenyl-2-(2-thienyl)ethenyl-5-(trifluoromethyl)benzo(b) thiophene-2-carboxamide in dog and human plasma has been developed. Both isomers strongly absorb light, leading to an efficient E in equilibrium Z photoisomerization. After iv administration of a single isomer (Z) to a dog, only the Zisomer was detected in plasma; no in vivo conversion to the E isomer was observed. However, when a mixture of the E and Z isomers (58.6:41.4) was administered in the same manner to the same dog, the E:Z ratio decreased significantly to 47.5:52.5 six hours after drug administration, indicating stereoselective disposition of the isomers. The elimination of the E isomer was found to be faster than that of the Z isomer.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Matuszewski BK,Kanovsky SM,Constanzer ML,Yeh KC,Bayne WFdoi
10.1002/jps.2600771014subject
Has Abstractpub_date
1988-10-01 00:00:00pages
880-4issue
10eissn
0022-3549issn
1520-6017pii
S0022-3549(15)47823-2journal_volume
77pub_type
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