Facchini V, Jones M, Smith G E
Biopharmaceutical Research, Rhone-Poulenc Ltd., Dagenham Essex, U.K.
Drug Metabol Drug Interact. 1989;7(1):17-28.
The disposition and metabolism of the [35S]-labelled growth promotor bis[N1-methyl- N2-methylsulphonyl) guanidinylethyl] disulphide was studied in the rat following oral administration. There was rapid and significant absorption of drug-derived products evidenced by maximum concentrations for plasma and the majority of sampled tissues at 1 h post dose, and extensive renal clearance, with greater than 62% of dose voided in urine in 12 h. Analysis of urine revealed that the administered compound had been completely metabolised to five metabolites of which the two major products have been characterised. A metabolic pathway involving reductive cleavage of the disulphide bond, followed by S-methylation and sulphoxidation would appear to be involved in the biotransformation of the compound.
在大鼠口服给药后，研究了[35S]标记的生长促进剂双[N1-甲基-N2-甲基磺酰基）胍基乙基]二硫化物的处置和代谢。给药后1小时血浆和大多数采样组织中的药物衍生产物出现快速且显著的吸收，表现为达到最大浓度，并且存在广泛的肾清除，12小时内超过62%的剂量经尿液排出。尿液分析表明，给药的化合物已完全代谢为五种代谢物，其中两种主要产物已得到鉴定。该化合物的生物转化似乎涉及一个代谢途径，即二硫键的还原裂解，随后是S-甲基化和硫氧化。
