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Intestinal absorption and excretion of troglitazone sulphate, a major biliary metabolite of troglitazone

2000; Taylor & Francis; Volume: 30; Issue: 7 Linguagem: Inglês

10.1080/00498250050078011

1366-5928

Kenji Kawai, Tsuyoshi Yamaguchi, Sumie Muramatsu, Fujiko Tsuruta, T. Ikeda, Kyoichi Kobashi, K Nakamura,

HIV/AIDS drug development and treatment

1. Deconjugation by sulphate transfer and intestinal absorption of troglitazone sulphate (M1), the major metabolite of a thiazolidinedione antidiabetic drug, troglitazone, were studied in the male F344 rat using 14C-troglitazone, 4C-M1 and 35S-M1. 2. Some part of M1, produced in the liver and excreted mostly in the bile, was deconjugated in the intestine to the parent compound, troglitazone, by arylsulphate sulphotransferase originated from intestinal flora. However, deconjugation of M1 was not catalyzed by arylsulphatases. Caecal injection of M1 led to the appearance of troglitazone and M1 in plasma. 3. Biliary excretion mostly as M1, and, following absorption, as M1 and troglitazone after deconjugation, were indicated as the basis for the enterohepatic circulation of troglitazone. 4. Enterohepatic circulation may prolong the pharmacological effects of troglitazone.