Calvo R, Sarabia S, Carlos R, Du Souich P
Biopharm Drug Dispos. 1987 Mar-Apr;8(2):115-24. doi: 10.1002/bdd.2510080203.
This study was designed to determine whether the surgical procedures for gastroduodenal ulcers influence sulfamethazine (SMZ) absorption and disposition. Prior to and on the average 79 days after surgery, eight patients received 10 mg kg-1 of sulfamethazine orally. Blood samples were obtained at regular intervals over 24 h and urine was collected for 48 h. Vagotomy with pyloroplasty or with gastrojejunostomy had no effect on SMZ kinetics. Vagotomy with partial gastrectomy decreased the SMZ plasma peak concentrations from 43.9 +/- 7.1 (mean +/- SEM) to 17.2 +/- 5.2 micrograms ml-1 (p less than 0.05) and increased the time required to reach this peak from 2.6 +/- 0.8 to 9.8 +/- 2.8 h (p less than 0.05). SMZ rate constant of absorption decreased only slightly (1.22 +/- 0.45 to 0.24 +/- 0.07 h-1) and SMZ bioavailability was not affected at all. In two (out of four) patients, SMZ volume of distribution and total body clearance increased, as reflected in the 41 per cent decrease in the mean area under the SMZ plasma concentration-time curve. No changes were detected in SMZ protein binding. Computer simulations indicated that in some subjects SMZ plasma concentrations at steady state could be 76 per cent lower following vagotomy with partial gastrectomy than before surgery. It was concluded that vagotomy and antrectomy with a gastroduodenostomy or Billroth I reconstruction decreased the rate of SMZ absorption and only in some subjects increased the SMZ volume of distribution and rate of elimination. The possible mechanisms involved in these reported kinetic changes are discussed.
本研究旨在确定胃十二指肠溃疡的手术操作是否会影响磺胺二甲嘧啶(SMZ)的吸收和代谢。在手术前及平均术后79天,8名患者口服10mg/kg的磺胺二甲嘧啶。在24小时内定期采集血样,并收集48小时的尿液。迷走神经切断术加幽门成形术或加胃空肠吻合术对SMZ的动力学没有影响。迷走神经切断术加部分胃切除术使SMZ血浆峰值浓度从43.9±7.1(平均值±标准误)降至17.2±5.2μg/ml(p<0.05),并使达到该峰值所需的时间从2.6±0.8小时增加到9.8±2.8小时(p<0.05)。SMZ的吸收速率常数仅略有下降(从1.22±0.45降至0.24±0.07h-1),而SMZ的生物利用度根本没有受到影响。在4名患者中的2名患者中,SMZ的分布容积和全身清除率增加,这反映在SMZ血浆浓度-时间曲线下平均面积减少41%。未检测到SMZ蛋白结合的变化。计算机模拟表明,在某些受试者中,迷走神经切断术加部分胃切除术后的SMZ稳态血浆浓度可能比手术前低76%。得出的结论是,迷走神经切断术和胃窦切除术加胃十二指肠吻合术或毕罗Ⅰ式重建降低了SMZ的吸收速率,仅在某些受试者中增加了SMZ的分布容积和消除速率。讨论了这些报道的动力学变化所涉及的可能机制。