Abstract
An automated direct assay system using high performance liquid chromatography was developed for the measurement of Danazol; DA and its two metabolites, Δ1-2-hydroxymethylethisterone (Δ1-2-HME), and 2-hydroxymethylethisterone (2-HME), in biological fluid (human serum and ascites). Serum concentrations of these compounds were measured up to 24h following a single oral administration of 200mg of DA to 6 females with endometriosis. The maximum serum concentration of DA, Δ1-2-HME and 2-HME was 208, 44 and 58ng/ml, respectively. The serum half-life of DA, Δ1-2-HME and 2-HME was 7.9, 4.3 and 4.4h, respectively. The mean serum concentration of DA and its two metabolites at the the sampling time (2h after oral administration of 200mg of DA every 4 weeks) hardly changed in the patients administered 400mg/day of DA over a period of 16 weeks. DA and Δ1-2-HME were detectable in ascites 2, 4 and 8h after oral administration of 200mg of DA, and 2-HME was detectable in ascites at 4 and 8h. This system could quantify DA and its metabolites easily and simultaneously, and was considered to be valuable in the studies on the relationship between the pharmaco-kinetics and the clinical effects of DA.
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全自動分析装置によるDanazolとその代謝産物の測定
1992 年 104 巻 1-2 号 p. 145-150
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抄録
An automated direct assay system using high performance liquid chromatography was developed for the measurement of Danazol; DA and its two metabolites, Δ1-2-hydroxymethylethisterone (Δ1-2-HME), and 2-hydroxymethylethisterone (2-HME), in biological fluid (human serum and ascites). Serum concentrations of these compounds were measured up to 24h following a single oral administration of 200mg of DA to 6 females with endometriosis. The maximum serum concentration of DA, Δ1-2-HME and 2-HME was 208, 44 and 58ng/ml, respectively. The serum half-life of DA, Δ1-2-HME and 2-HME was 7.9, 4.3 and 4.4h, respectively. The mean serum concentration of DA and its two metabolites at the the sampling time (2h after oral administration of 200mg of DA every 4 weeks) hardly changed in the patients administered 400mg/day of DA over a period of 16 weeks. DA and Δ1-2-HME were detectable in ascites 2, 4 and 8h after oral administration of 200mg of DA, and 2-HME was detectable in ascites at 4 and 8h. This system could quantify DA and its metabolites easily and simultaneously, and was considered to be valuable in the studies on the relationship between the pharmaco-kinetics and the clinical effects of DA.
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