Sakamoto H, Hirose T, Nakamoto S, Mine Y
J Antibiot (Tokyo). 1985 Aug;38(8):1088-95. doi: 10.7164/antibiotics.38.1088.
The mechanism of renal excretion of FK027, a new oral cephalosporin, was investigated in dogs and rabbits. In dogs, FK027 was mainly cleared by glomerular filtration, and approximately 50% of the filtered drug was reabsorbed through the proximal tubules. This tubular reabsorption and a high binding ratio to serum protein lead to the exceptionally long serum half-life of the drug. The facts that the clearance ratio of FK027 declined slightly from 58.0 to 49.2% by the addition of probenecid, and that the effect of probenecid was less marked in the stop-flow study, along with no significant change in serum half-life, may account for the scarcely detectable secretion from the renal tubules. In rabbits, the addition of probenecid caused a decrease of the clearance ratio of FK027, disappearance of FK027 peak in the stop-flow study, and extended the serum half-life. These facts are evidence that FK027 is excreted by both tubular secretion and glomerular filtration in rabbits.
对一种新型口服头孢菌素FK027在犬和兔体内的肾脏排泄机制进行了研究。在犬体内，FK027主要通过肾小球滤过清除，约50%的滤过药物通过近端小管重吸收。这种肾小管重吸收以及与血清蛋白的高结合率导致该药物具有异常长的血清半衰期。FK027的清除率因加入丙磺舒而从58.0%略有下降至49.2%，且在停流研究中丙磺舒的作用不太明显，同时血清半衰期无显著变化，这些事实可能说明肾小管几乎没有分泌。在兔体内，加入丙磺舒导致FK027清除率降低、停流研究中FK027峰消失，并延长了血清半衰期。这些事实证明FK027在兔体内通过肾小管分泌和肾小球滤过两种方式排泄。
