[A study on the metabolites of dl-3-n-butyphthalide in rats].
The metabolites of dl-3-n-butylphthalide(NBP), a novel drug with promising protective action against cerebral ischemia, was studied in rats. Two main in vitro metabolites of NBP, M I and M II, were isolated and purified from rat liver microsome incubating system by using HPLC. The structure elucidation was mainly accomplished by spectral studies(UV, 1H-NMR, MS). Within 24 h following i.g. 3H-NBP, the total radioactivity excreted in urine and feces was 73.7% of the dose. Comparing with previous study, within 72 h following i.g. NBP, the total prototype drug excreted in urine and feces was 2.53% of the dose. This result excludes the possibility that NBP accumulates in vivo. The urine and brain homogenate of the rats(i.g. 3H-NBP) were analyzed by TLC. M I and M II were found in urine and M I was found in brain only. Furthermore, the ratio of radioactive M I to proptype drug was 1:1 in rat brain within 1 h following i.g. 3H-NBP. So, M I and M II were supposed to be the two main in vivo metabolites of NBP and M I might be an active metabolite.
Wang
C H
CH
Institute of Materia Medica, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050.
Feng
Y P
YP
Wu
Y L
YL
D000818:Animals; D001572:Benzofurans / Q000378:metabolism* / Q000652:urine; D001921:Brain / Q000378:metabolism; D005243:Feces / Q000737:chemistry; D008297:Male; D018696:Neuroprotective Agents / Q000378:metabolism* / Q000652:urine; D051381:Rats; D017208:Rats, Wistar
D001572:Benzofurans; D018696:Neuroprotective Agents; C027125:3-n-butylphthalide