Isolation and identification of a major metabolite of SFZ-47 in the rabbit urine / 药学学报
Acta Pharmaceutica Sinica
;
(12): 141-143, 2002.
Artigo
em Chinês
| WPRIM
| ID: wpr-343381
ABSTRACT
<p><b>AIM</b>To isolate and identify a glucuronide metabolite of SFZ-47 [3H-1,2-dihydro-2-(4-methyl-phenylamino)methyl-1-pyrrolizinone], which is difficult to synthesize because it undergoes hydrolysis and intramolecular acyl migration at physiological pH, in rabbit urine.</p><p><b>METHODS</b>Two rabbits were ig 200 mg doses of SFZ-47. Urine was collected for 24 h, adjusted to pH 4.0 with acetic acid and lyophilized. The residues were reconstituted in 25 mL methanol and centrifuged at 5,000 r.min-1 for 10 min. The supernatant was filtered (0.45 micron) and then isolated with semi-preparative reversed phase HPLC. The eluent collected from individual peaks was evaporated by rotary evaporation and freeze-drying. Compounds were then identified with electrospray ion trap mass spectrometry and 1HNMR spectroscopy.</p><p><b>RESULTS</b>The 1HNMR and ESI-MSn results indicate that the metabolite is the 1-O-acyl beta-D-glucuronide conjugate of 4-(3H-1,2-dihydro-1-pyrrolizinone-2-methylamino) benzoic acid.</p><p><b>CONCLUSION</b>This method was shown to be rapid and simple and gave excellent resolution from endogenous constituents in urine, and it is suitable for preparation of the glucuronide metabolites of SFZ-47 and its analogues.</p>
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Pirróis
/
Urina
/
Estrutura Molecular
/
Química
/
Anti-Inflamatórios não Esteroides
/
Cromatografia Líquida de Alta Pressão
/
Espectrometria de Massas por Ionização por Electrospray
/
Metabolismo
Tipo de estudo:
Estudo diagnóstico
Limite:
Animais
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2002
Tipo de documento:
Artigo
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