Borin M T, Forbes K K, Hughes G S
Upjohn Company, Kalamazoo, MI 49001-0199, USA.
Biopharm Drug Dispos. 1995 May;16(4):295-302. doi: 10.1002/bdd.2510160405.
The bioavailability of cefpodoxime proxetil tablets relative to an oral solution of cefpodoxime proxetil in a sucrose/alcohol/citric acid vehicle was studied in 11 healthy volunteers in a randomized, crossover study. Fasted subjects took one cefpodoxime proxetil 100 mg tablet or 50 mL of a 2 mg mL-1 cefpodoxime proxetil oral solution on two separate occasions. In a third study period, all subjects took a 100 mg dose of the oral solution with a high-fat meal to investigate the effect of food on cefpodoxime proxetil absorption from the oral solution. Serial blood samples were obtained over a 24 h period, and urine was collected for 48 h after dosing. Cefpodoxime concentrations in plasma and in urine were determined using HPLC methods. The bioavailability of cefpodoxime proxetil tablets relative to the oral solution was 82%, as determined from AUC ratios. There was no difference in the rate of cefpodoxime absorption between dosage forms. Food had no effect on the extent of drug absorption from the oral solution but did result in delayed absorption. These results suggest that complete dissolution of cefpodoxime proxetil is critical for optimal bioavailability.
在一项随机交叉研究中，对11名健康志愿者进行了头孢泊肟酯片相对于以蔗糖/酒精/柠檬酸为溶媒的头孢泊肟酯口服溶液的生物利用度研究。空腹受试者在两个不同的时间分别服用一片100 mg头孢泊肟酯片或50 mL浓度为2 mg/mL的头孢泊肟酯口服溶液。在第三个研究阶段，所有受试者均在高脂餐后服用100 mg剂量的口服溶液，以研究食物对头孢泊肟酯从口服溶液中吸收的影响。在24小时内采集系列血样，并在给药后48小时收集尿液。使用高效液相色谱法测定血浆和尿液中的头孢泊肟浓度。根据AUC比值测定，头孢泊肟酯片相对于口服溶液的生物利用度为82%。两种剂型的头孢泊肟吸收速率没有差异。食物对药物从口服溶液中的吸收程度没有影响，但确实导致吸收延迟。这些结果表明，头孢泊肟酯的完全溶解对于最佳生物利用度至关重要。
