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本研究应用气相色谱法,测定了我国124位蒙族健康志愿者一次口服异喹胍(DB)后尿中DB和4羟异喹胍(4-OH-DB)的含量。结果表明,我国蒙族志愿者的DB羟化代谢具有双态性。求得DB和4-OH-DB代谢比值的对数值(Log MR)的分布范围为-0.57～1.49(MR为0.27～31)。124位志愿者中发现一位弱代谢者,其缺陷频发率为0.81％。吸烟和性别对DB羟化代谢的MR值无明显影响(P>0.25)。服药后6小时尿中DB和4-OH-DB的回收率分别为18.08±8.64％和11.79±5.27％。药代动力学研究表明,DB和4-OH-DB的t 1/2分别为2.60±0.21和2.69±0.86小时;K分别为0.2684±0.0207和0.2973±0.1603小时~(-1)。
In this study, the contents of DB and 4-OH-DB in urine of 124 Mongolian healthy volunteers after oral administration of oral gingivalidin (DB) were determined by gas chromatography. The results showed that DB hydroxylation metabolism of Mongolian volunteers in our country is bimodal. The Log MR distribution of DB and 4-OH-DB was found to range from -0.57 to 1.49 (MR 0.27 to 31). A weak metabolizer was found in 124 volunteers, with a frequency of 0.81%. Smoking and sex had no significant effect on MR values of DB hydroxylation (P> 0.25). The urinary DB and 4-OH-DB recoveries at 6 h after treatment were 18.08 ± 8.64% and 11.79 ± 5.27%, respectively. Pharmacokinetic studies showed that the t1 / 2 of DB and 4-OH-DB were 2.60 ± 0.21 and 2.69 ± 0.86 hours respectively; K were 0.2684 ± 0.0207 and 0.2973 ± 0.1603 h -1, respectively.