STUDIES ON THE METABOLISM OF DILTIAZEM IN MAN
スポンサーリンク
概要
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The human urinary metabolites of diltiazem were analyzed by thin-layer chroma tography (TLC) and gas chromatography-mass spectrometry. Diltiazem was metabolized by deacetylation, N-demethylation, O-demethylation and conjugation. Metabolite M_A, N-monodemethyl-diltiazem, was identified as a new major metabolite in human urine, and four metabolites were identified as deacetyl-diltiazem (M_1), deacetyl-N-monodemethyl-diltiazem (M_2), deacetyl-O-demethyl-diltiazem (M_4), deacetyl-N, O-demethyl-diltiazem (M_6) which were known as rat urinary metabolites. Metabolite M_2,M_4 and M_6 were converted in part to glucuronides and/or sulfates. Unchanged diltiazem and metabolite M_A were determined in human plasma and urine by TLC-densitometry. Diltiazem and metabolite M_A excreted in 24-h urine were 44.4 and 48.5% of the total unconjugated form, rcspectively. The mean plasma level of metabolite M_A was approximately one-third of diltiazem level. On the basis of these findings, a probable metabolic pathway of diltiazem in man is presented.
- 公益社団法人日本薬学会の論文
著者
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Ando Hidehiro
Biological Research Laboratory Tanabe Seiyaku Co. Ltd.
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HARIGAYA SHOICHI
Pharmacological Research Laboratory, Tanabe Seiyaku Co., Ltd.
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Harigaya S
Biological Research Laboratory : Organic Chemistry Research Laboratory : Tanabe Seiyaku Co. Ltd.
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SUGIHARA Juko
Pharmaceutical Development Research Laboratory, Tanabe Seiyaku Co., Ltd.,
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Sugawara Yoichi
Pharmacological Research Laboratory Tanabe Seiyaku Co.
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ANDO HIDEHIRO
Pharmacological Research Laboratory, Tanabe Seiyaku Co.
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ETOH AKIRA
Products Formulation Research Laboratory, Tanabe Seiyaku Co.
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KOHNO KEIICHI
Products Formulation Research Laboratory, Tanabe Seiyaku Co.
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Etoh Akira
Products Formulation Research Laboratory Tanabe Seiyaku Co.
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Kohno Keiichi
Products Formulation Research Laboratory Tanabe Seiyaku Co.
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HARIGAYA Shoichi
Pharmacological Research Laboratory, Tanabe Seiyaka Co., Ltd.
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SUGIHARA Juko
Pharmaceutical Development Research Laboratory, Tanabe Seiyaku Co. Ltd.
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Sugihara Juko
Pharmaceutical Development Research Laboratory Tanabe Seiyaku Co., Ltd.,
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