Horai Y, Zhou H H, Zhang L M, Ishizaki T
Division of Clinical Pharmacology, National Medical Center, Tokyo, Japan.
Br J Clin Pharmacol. 1988 Jan;25(1):81-7. doi: 10.1111/j.1365-2125.1988.tb03285.x.
1 The N-acetylation of dapsone (DDS) was studied in 108 unrelated Chinese subjects residing in the mainland of China. 2 The frequency of slow acetylators determined using the plasma monoacetyldapsone to DDS ratio (MADDS/DDS, slow acetylators less than 0.30 and rapid acetylators greater than 0.35) at 3 h after an oral dose of DDS (100 mg) was 13.0% (14 of the 108 subjects) with a 95% confidence interval of 7.9 to 20.6%. 3 The mean plasma concentration of MADDS was about three times lower in the slow than in the rapid acetylators and there was a highly significant correlation (rs = 0.886, P less than 0.001) between plasma MADDS concentration and acetylation ratio. 4 Urinary acetylation ratios (MADDS/DDS) and cumulative urinary excretion of MADDS were significantly (P less than 0.001) lower in slow acetylators compared with rapid acetylators. In addition, there was a significant relationship (rs = 0.510 to 0.718, P less than 0.001) between plasma and urinary acetylation ratios. However, the distribution of the urinary acetylation ratio was not bimodal. 5 The urinary acetylation ratio after an oral dose of DDS is not a discriminative index for determining acetylation phenotype.
对居住在中国内地的108名无亲缘关系的中国受试者进行了氨苯砜(DDS)的N - 乙酰化研究。
口服DDS(100mg)后3小时,使用血浆单乙酰氨苯砜与DDS的比值(MADDS/DDS,慢乙酰化者小于0.30,快乙酰化者大于0.35)确定慢乙酰化者的频率为13.0%(108名受试者中的14名),95%置信区间为7.9%至20.6%。
慢乙酰化者的MADDS平均血浆浓度比快乙酰化者低约三倍,血浆MADDS浓度与乙酰化比值之间存在高度显著相关性(rs = 0.886,P小于0.001)。
与快乙酰化者相比,慢乙酰化者的尿乙酰化比值(MADDS/DDS)和MADDS的累积尿排泄量显著更低(P小于0.001)。此外,血浆和尿乙酰化比值之间存在显著关系(rs = 0.510至0.718,P小于0.001)。然而,尿乙酰化比值的分布并非双峰分布。
口服DDS后的尿乙酰化比值不是确定乙酰化表型的鉴别指标。