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恒河猴对二甲基亚砜的吸收、代谢及排泄

The absorption, metabolism and excretion of dimethyl sulfoxide by rhesus monkeys.

作者信息

Layman D L, Jacob S W

出版信息

Life Sci. 1985 Dec 23;37(25):2431-7. doi: 10.1016/0024-3205(85)90111-0.

Abstract

The absorption and excretion of dimethyl sulfoxide (DMSO) were studied in Rhesus monkeys (Macaca mulatta) given daily oral doses of 3 gms DMSO/kg B.W. for 14 days. DMSO and its major metabolite, dimethyl sulfone (DMSO2), were measured in serum, urine and feces by gas-liquid chromatography. DMSO was absorbed rapidly, reached a steady state blood level after 1 day and then was cleared from blood within 72 hrs after ending treatment. Serum DMSO declined in a linear fashion on semilogarithmic coordinates as described by second order kinetics. It had a half-life of 16 hrs. DMSO2 appeared in blood within 2 hrs and reached a steady state concentration after 4 days of treatment. DMSO2 was cleared from blood about 120 hrs after DMSO administration was stopped. Its half-life in blood was calculated to be 38 hrs. Urinary excretion of unmetabolized DMSO and DMSO2 accounted for about 60% and 16%, respectively, of the total ingested dose. Neither DMSO nor DMSO2 was detected in fecal samples. However, when added to fecal samples, DMSO was degraded rapidly. Although dimethyl sulfide (DMS) was not measured, some DMSO was metabolized to this compound because of the particular sweetness of breath of the monkeys. We conclude that the absorption of DMSO by monkeys is similar to that for humans, but that its conversion to DMSO2 and urinary elimination are more rapid in monkeys.

摘要

对恒河猴(猕猴)进行了研究,这些猴子每天口服3克二甲基亚砜(DMSO)/千克体重,持续14天,以观察DMSO的吸收和排泄情况。通过气液色谱法测定血清、尿液和粪便中的DMSO及其主要代谢产物二甲基砜(DMSO2)。DMSO吸收迅速,1天后达到稳态血药浓度,停止治疗后72小时内从血液中清除。血清DMSO在半对数坐标上呈线性下降,符合二级动力学描述。其半衰期为16小时。DMSO2在2小时内出现在血液中,治疗4天后达到稳态浓度。停止给予DMSO后约120小时,DMSO2从血液中清除。其在血液中的半衰期经计算为38小时。未代谢的DMSO和DMSO2的尿排泄量分别约占总摄入量的60%和16%。在粪便样本中未检测到DMSO和DMSO2。然而,当添加到粪便样本中时,DMSO迅速降解。尽管未测定二甲基硫醚(DMS),但由于猴子呼出的气味有特殊甜味,推测部分DMSO代谢生成了该化合物。我们得出结论,猴子对DMSO的吸收与人类相似,但猴子体内DMSO转化为DMSO2以及经尿液消除的速度更快。

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