Nandi V, Soine W H
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond 23298-0540, USA.
J Pharm Biomed Anal. 1997 May;15(8):1187-95. doi: 10.1016/s0731-7085(96)01936-x.
A study was undertaken to determine if humans excrete both amobarbital N-glucuronides and N-glucosides in urine after an oral dose of amobarbital. Amobarbital N-glucuronides were synthesized and characterized. A reverse phase LC method using post-column pH adjustment and UV detection at 240 nm was developed and used for the quantification of the amobarbital N-glucosides and N-glucuronides in human urine. Amobarbital was administered orally to seven male subjects and the total urine was collected for a period of 48-53 h after dosing. After filtration, the urine was injected directly onto the HPLC column to analyze for the presence of metabolites. The previously identified (5S)-amobarbital N-glucoside was detected in all seven subjects. The (5R)-amobarbital N-glucoside was detected at lower concentrations in only four of the subjects. At the levels at which amobarbital N-glucosides were detected, there was no evidence for the formation and excretion of the amobarbital N-glucuronides. Amobarbital N-glucuronidation is not a quantitatively significant pathway for the biodisposition of amobarbital in humans.
开展了一项研究，以确定人类口服异戊巴比妥后尿液中是否会排泄异戊巴比妥N - 葡萄糖醛酸苷和N - 葡萄糖苷。合成并表征了异戊巴比妥N - 葡萄糖醛酸苷。开发了一种采用柱后pH调节和240 nm紫外检测的反相液相色谱法，并用于定量测定人尿中的异戊巴比妥N - 葡萄糖苷和N - 葡萄糖醛酸苷。对7名男性受试者口服异戊巴比妥，并在给药后48 - 53小时收集全部尿液。过滤后，将尿液直接注入高效液相色谱柱以分析代谢物的存在情况。在所有7名受试者中均检测到了先前鉴定出的(5S)-异戊巴比妥N - 葡萄糖苷。仅在4名受试者中检测到浓度较低的(5R)-异戊巴比妥N - 葡萄糖苷。在所检测到异戊巴比妥N - 葡萄糖苷的水平下，没有证据表明存在异戊巴比妥N - 葡萄糖醛酸苷的形成和排泄。异戊巴比妥N - 葡萄糖醛酸化不是异戊巴比妥在人体内生物转化的主要定量途径。
