PHARMACOKINETICS OF AMPICILLIN-SULBACTAM IN HEALTHY ELDERLY AND YOUNG VOLUNTEERS
PHARMACOKINETICS OF AMPICILLIN-SULBACTAM IN HEALTHY ELDERLY AND YOUNG VOLUNTEERS
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DOI：
10.1128/aac.35.10.2098
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发表时间：
1991-10-01
影响因子：
4.9
通讯作者：
HIRSCHMAN, SZ
中科院分区：
文献类型：
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作者：
MEYERS, BR;WILKINSON, P;HIRSCHMAN, SZ
研究了氨苄西林-舒巴坦在老年受试者（65 - 85岁;第3组，n = 8）中的药代动力学，并与中年（41 - 64岁;第2组，n = 8）和年轻（20 - 40岁;第1组，n = 8）受试者进行了比较。 每例受试者在30分钟内接受单次2 g氨苄西林联合1 g舒巴坦60 ml静脉注射液给药。 在基线时采集血液和尿液样本，并在输注后8.5小时内连续采集。 氨苄西林和舒巴坦的浓度通过反相C-8柱上的高效液相色谱法测定。 第3组样本中氨苄西林和舒巴坦的血清平均水平均显著较高：氨苄西林从1至8.5 h，舒巴坦在除5.5 h外的相同时间间隔（P小于或等于0.05）。 组3中氨苄西林和舒巴坦的平均尿排泄量最低，尿浓度最高。 对于氨苄西林和舒巴坦，第3组的血清药物浓度-时间曲线下面积、半衰期和血清中的最大浓度最大，而总清除率最低。 这些结果与氨苄西林-舒巴坦在老年受试者中的抗菌活性较年轻受试者延长一致。
The pharmacokinetics of ampicillin-sulbactam in elderly subjects (65 to 85 years; group 3, n = 8), compared with those in middle-aged (41 to 64 years; group 2, n = 8) and younger (20 to 40 years; group 1, n = 8) subjects, were investigated. A single 2-g dose of ampicillin combined with 1 g of sulbactam in 60 ml of intravenous solution was administered to each subject over a 30-min period. Blood and urine samples were taken at baseline and serially over an 8.5-h period following the infusion. Ampicillin and sulbactam concentrations were assayed by high-performance liquid chromatography on a reversed-phase C-8 column. The mean levels in serum of both ampicillin and sulbactam were significantly higher for samples from group 3: for ampicillin from 1 through 8.5 h, and for sulbactam for the same time interval except at 5.5 h (P less-than-or-equal-to 0.05). The mean urinary excretion of both ampicillin and sulbactam was lowest, and urinary concentrations were highest in group 3. The areas under the serum drug concentration-time curve, the half-lives, and the maximum concentrations in serum were greatest, while the total clearance was lowest, for group 3 for both ampicillin and sulbactam. These results are consistent with a prolongation of antimicrobial activity of ampicillin-sulbactam in the elderly compared with that in younger subjects.