Hughes G S, Heald D L, Patel R, Spillers C R, Batts D H, Euler A R
Upjohn Research Clinic, Upjohn Company, Kalamazoo, Michigan.
Methods Find Exp Clin Pharmacol. 1990 Apr;12(3):197-204.
The effects of gastric motility on the pharmacokinetics of cefpodoxime proxetil, an oral, broad spectrum, third-generation cephalosporin antibiotic were evaluated in 12 healthy subjects. In this open-label, crossover trial, each subject took a 200 mg dose (two 100 mg film-coated tablets) in each study period. There was an initial fasting period followed by a control period and then either a propantheline or metoclopramide period. Gastric motility was measured using [99mTc]-labeled sulfur colloid in oatmeal in the control, propantheline and metoclopramide periods. Treatment with propantheline or metoclopramide was given 30 min before dosing with the antibiotic and the radioisotope. Serial images with a gamma counter were made every 15 min for 2 h. Gastric emptying time was faster than control with metoclopramide, but generally slower with propantheline than control. The mean peak plasma concentration, mean area under plasma concentration time curve and mean half-life of cefpodoxime proxetil were similar in all groups as compared to control. The mean time to peak plasma concentration was delayed in the propantheline period and peak plasma concentrations were greater at all sampling times at six hours after dosing. This study utilized the gastric nuclear scan with modification of gastric motility by metoclopramide and propantheline and with simultaneous determination of the disposition of cefpodoxime proxetil to understand the absorption of the drug.
在12名健康受试者中评估了胃动力对头孢泊肟酯（一种口服、广谱、第三代头孢菌素抗生素）药代动力学的影响。在这项开放标签的交叉试验中，每位受试者在每个研究阶段服用200 mg剂量（两片100 mg薄膜包衣片）。最初有一个禁食期，随后是一个对照期，然后是丙胺太林期或甲氧氯普胺期。在对照期、丙胺太林期和甲氧氯普胺期，使用[99mTc]标记的硫胶体燕麦片测量胃动力。在给予抗生素和放射性同位素前30分钟给予丙胺太林或甲氧氯普胺治疗。用γ计数器每15分钟进行一次连续图像采集，共采集2小时。甲氧氯普胺组的胃排空时间比对照组快，但丙胺太林组通常比对照组慢。与对照组相比，所有组中头孢泊肟酯的平均血浆峰浓度、血浆浓度-时间曲线下平均面积和平均半衰期相似。丙胺太林期血浆峰浓度的平均达峰时间延迟，给药后6小时所有采样时间的血浆峰浓度均更高。本研究采用胃核素扫描，通过甲氧氯普胺和丙胺太林改变胃动力，并同时测定头孢泊肟酯的处置情况，以了解药物的吸收情况。
