METABOLISM OF [C-14]-DEBRISOQUINE IN MAN

被引:76
作者
IDLE, JR
MAHGOUB, A
ANGELO, MM
DRING, LG
LANCASTER, R
SMITH, RL
机构
关键词
D O I
10.1111/j.1365-2125.1979.tb00930.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
1 The synthesis of [14C]‐debrisoquine hydrochloride and 4‐hydroxy‐ debrisoquine sulphate is described. 2 The metabolic fate and excretion profile in both urine and faeces of 14C‐labelled debrisoquine was studied in five healthy human subjects. 3 Investigations showed that the drug is well‐absorbed after a single oral dose of 32 mg and quantitatively eliminated from the body within three days. 4 4‐Hydroxy‐ debrisoquine is the major metabolite of debrisoquine, although significant amounts of 5‐,6‐, 7‐ and 8‐hydroxy‐debrisoquine are also formed. 5 Electron‐capture gas chromatography is a useful method for measuring debrisoquine and its five hydroxylated metabolites in urine at the pg level. 1979 The British Pharmacological Society
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页码:257 / 266
页数:10
相关论文
共 30 条
[1]   METABOLISM OF DEBRISOQUINE SULFATE IN RAT, DOG AND MAN [J].
ALLEN, JG ;
BROWN, AN ;
MARTEN, TR .
XENOBIOTICA, 1976, 6 (07) :405-409
[2]  
ALLEN JG, 1975, DRUG METAB DISPOS, V3, P332
[3]  
ANGELO M, 1975, BRIT J PHARMACOL, V55, pP264
[4]  
ANGELO MM, 1977, BRIT J CLIN PHARMACO, V4, pP725
[5]  
ATHANASSIADIS D, 1966, BRIT MED J, V2, P733
[6]  
ATLAS SA, 1977, DRUG METABOLISM MICR, P393
[7]   CYCLIZATIONS OF DIALDEHYDES WITH NITROMETHANE .12. O-PHTHALALDEHYDE [J].
BAER, HH ;
ACHMATOWICZ, B .
JOURNAL OF ORGANIC CHEMISTRY, 1964, 29 (11) :3180-&
[8]  
BAMBERGER E, 1893, BER, V26, P1205
[9]   FATE OF BIGUANIDES IN MAN [J].
BECKMANN, R .
ANNALS OF THE NEW YORK ACADEMY OF SCIENCES, 1968, 148 (A3) :820-&
[10]   OXIDATION OF INDAN TO INDANOL AND INDANONE BY HEPATIC MICROSOMAL SYSTEM [J].
BILLINGS, RE ;
SULLIVAN, HR ;
MCMAHON, RE .
BIOCHEMISTRY, 1970, 9 (05) :1256-&