In vitro metabolism and stability of adefovir mixed phosphonate derivative Q3-I2 / 中国药科大学学报
Journal of China Pharmaceutical University
;
(6): 699-705, 2018.
Artigo
em Chinês
| WPRIM
| ID: wpr-811776
ABSTRACT
@#A, UPLC-QTOF-MS/MS and UPLC-MS/MS were used to investigate the derivative of adefovir mixed phosphonate Q3-I2. Stability and in vitro metabolites of Q3-I2, and the control drug adefovir dipivoxil were co-inculbated with artificial gastric juice, artificial intestinal juice, rat blank plasma and rat liver microsomes, using UPLC-MS/MS and UPLC-QTOF-MS/MS measure the residual concentration of the compounds in each incubation system and the metabolites in the liver microsomal system, respectively, and calculate the half-life and clearance rate by the substrate elimination method. The compounds designed and synthesized in this experiment are stable in the gastrointestinal tract, prolonging t1/2 of plasma and liver microsomes and rapidly degrading the active meta-bolites. In the liver microsomal system, a total of 8 metabolites were detected by positive and negative ion mode, including hydrolysis, oxidation, acetylation, and glucuronidation.
Texto completo:
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Índice:
WPRIM (Pacífico Ocidental)
Idioma:
Chinês
Revista:
Journal of China Pharmaceutical University
Ano de publicação:
2018
Tipo de documento:
Artigo
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