硫酸氨基葡萄糖的吸收、分布、代谢和排泄。复习一下。

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硫酸氨基葡萄糖的吸收、分布、代谢和排泄。复习一下。

Arzneimittelforschung。2001年9月,51 (9):699 - 725。doi: 10.1055 / s - 0031 - 1300105。

PubMed ID
11642003 (在PubMed
]
文摘

本文回顾了相关文献吸收、分布、代谢和排泄(ADME)氨基葡萄糖(Gl)在人类和动物管理结晶硫酸氨基葡萄糖(CGS)。静脉管理研究生院理事会在人,单丸静脉注射(注射)1005毫克CGS Gl(628毫克),父Gl消失从等离子体明显半衰期为1.11 h。调查与均匀14 c标记Gl和502毫克(14 c-gl)管理研究生院理事会表明Gl的消失是由于纳入的血浆球蛋白发生滞后时间为0.45 h - h和0.26的速度。放射性达到峰值后10 h和消除单一静脉输液后t1/2 95 h。502毫克剂量的CGS追踪与14 c-gl, 120 h尿排泄的占29%的服用剂量。得到了一致的结果在老鼠和狗,在放射性迅速出现在肝脏,肾脏和其它组织,包括关节软骨。在人,1005毫克CGS输液丸注入后,24小时的尿排泄Gl与离子交换色谱法确定服用剂量的38%,主要是在第一个8 h后管理。类似的结果跟踪CGS 14 c-gl。得到了一致的结果尿排泄的老鼠和狗追踪与14 c-gl cg。放射性物质的排泄粪便是很小的。消除放射性与呼气14 co2以老鼠达49%的服用剂量144 h后管理,其中16%发生在第一个6 h。肌内管理研究生院理事会的男人,一个单一的肌内注射的502毫克CGS追踪14 c-gl,静脉输液管理后给结果类似。口服CGS的男人,单一剂量的7.5 g CGS之后,Gl在等离子体是低于定量的限制(3微克/毫升)的离子交换色谱法。 After a single dose of 314 mg CGS traced with 14C-Gl, radioactivity appeared incorporated in plasma globulins with a lag time of 1.5 h and increasing with a rate of 0.24 h-1. The peak was reached at the 9th h after administration. The radioactivity then was eliminated with a t1/2 of 58 h. The absolute oral bioavailability evaluated on the AUCs of the globulin-incorporated radioactivity was 44%. The fecal excretion in 120 h was 11.3% of the administered dose showing that at least 88.7% of the administered dose was absorbed through the gastrointestinal tract. The difference of 45% is probably due to a hepatic first-pass effect. Investigated in the rat with doses from 126 to 3768 mg CGS traced with 14C-Gl, a linear relationship was found with the AUCs as well as between doses and the Cmax of radioactivity in total and in deproteinized plasma. The urinary elimination in man of the parent Gl in 24 h determined with ion exchange chromatography after a single dose of 7.5 g of CGS was 1.19% of the administered dose, occurring mostly in the first 8 h after administration. After administration of 1884 mg repeated for 7 days the daily urinary excretion of Gl increased from 1.60% of the daily dose during the first 24 h to 2.22% of the daily dose in the last 24 h. The steady state was reached after the second day. The urinary excretion at steady state during repeated administration allowed to conclude that daily 1884 CGS administered either t.i.d. in sugar coated tablets or once a day in oral solution were bioequivalent. The elimination of radioactivity with the expired as 14CO2 measured in rats was 82% of the administered dose in the 144 h following the administration, 61% of which occur in the first 6 h. Interaction of Gl with the ADME of glucose The ADME of glucose was investigated in the rat administering i.v. or orally 14C uniformly labeled glucose. The kinetic in plasma and the tissue distribution of glucose differed totally from those of Gl, pointing out that exogenous glucose provides the energy for biochemical processes, whereas exogenous Gl acts mainly as substrate for the biosynthesis of mucopolysaccharides and of biopolymers of the articulations and bones. There was no evidence of interaction by Gl orally administered with the ADME of glucose.

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