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1.
Acta Pharmaceutica Sinica ; (12): 1176-1182, 2007.
Artículo en Chino | WPRIM | ID: wpr-268209

RESUMEN

To investigate the principal metabolites of 1-(1-(6-methoxyl-2-naphthyl) ethyl)-2-(4-nitrobenzyl)-6,7-dimethoxyl-1,2,3,4-tetrahydroisoquinoline hydrobromide (code designation: P91024) in rats after ig administration by LC-MS/MS, the phase I metabolites were discovered by comparing the fullscan and SIM chromatograms of the test samples with the corresponding blanks. The structures of phase I metabolites were identified by ESI-MS spectra and the product spectra of the corresponding adduct ions. The phase II metabolites were identified in the test samples after the phase I metabolites were completely removed with solvent extraction and then treated with glucuronidase for enzymolysis of phase II glucuronide conjugates and the hydrolysates. Two phase I metabolites of P91024 were identified in rat feces, one phase I and five phase II in bile, one phase I and three phase II in urine, and four phase I and one phase II in plasma. Their structures were elucidated, separately. P91024 was extensively metabolized in rat. The metabolites can be easily screened and identified by LC-MS/MS method.


Asunto(s)
Animales , Femenino , Masculino , Ratas , Bilis , Metabolismo , Cromatografía Liquida , Fibrinolíticos , Sangre , Metabolismo , Farmacocinética , Orina , Ratas Sprague-Dawley , Espectrometría de Masa por Ionización de Electrospray , Tetrahidroisoquinolinas , Sangre , Metabolismo , Farmacocinética , Orina
2.
Acta Pharmaceutica Sinica ; (12): 789-792, 2006.
Artículo en Chino | WPRIM | ID: wpr-294938

RESUMEN

<p><b>AIM</b>To study the excretion of (-)-clausenamide in rats.</p><p><b>METHODS</b>The urine, feces and bile were collected at predetermined time points after (-)-clausenamide was orally administrated to 6 rats (30 mg x kg(-1)). The concentrations of (-)-clausenamide and its metabolite 6-OH-(-)-clausnamide were determined by HPLC-MS/MS method using glipzide as the internal reference, and the accumulative excretion amount of (-)-clausenamide and 6-OH-(-)-clausenamide was calculated in the urine, feces and bile, separately.</p><p><b>RESULTS</b>(-)-Clausenamide was recovered mostly (44%) from feces in 112 hours, 7.1% was found from urine in 120 hours and 0.013% was detected from bile in 24 hours. The accumulative excretions of 6-OH-(-)-clausenamide were 0.92% , 0.46% and 0.0003% of the administered dose from feces, urine and bile, respectively.</p><p><b>CONCLUSION</b>The major amount of (-)-clausenamide was recovered from feces after (-)-clausenamide was orally administrated to rats (30 mg kg(-1)).</p>


Asunto(s)
Animales , Femenino , Masculino , Ratas , Administración Oral , Bilis , Metabolismo , Cromatografía Líquida de Alta Presión , Clausena , Química , Heces , Química , Lactamas , Química , Farmacocinética , Orina , Lignanos , Química , Farmacocinética , Orina , Espectrometría de Masas , Fármacos Neuroprotectores , Farmacocinética , Orina , Hojas de la Planta , Química , Plantas Medicinales , Química , Ratas Sprague-Dawley , Estereoisomerismo
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