Onoyama K, Hirakata H, Iseki K, Fujimi S, Omae T, Kobayashi M, Kawahara Y
Hypertension. 1981 Jul-Aug;3(4):456-9. doi: 10.1161/01.hyp.3.4.456.
Blood concentration and urinary excretion of captopril following 50 mg oral administration were determined by high-performance liquid chromatography in normal subjects and patients with chronic renal failure. In normal subjects, the maximum blood concentration of the free form of captopril was obtained within 1 hour and was not detectable after 6 hours; 41% of administered captopril was excreted into the urine as free form and metabolites within 2 hours, and 58% within 6 hours. In chronic renal failure patients with an average serum creatinine of 5.1 mg/dl, the absorption constant (Ka), maximum concentration (Cmax), and area under the blood concentration curve (AUC) were not significantly different from those in the normal subjects, but the elimination constant (Ke) and biological half-life (T1/2) showed a significant delay in the disappearance of captopril from the blood (p less than 0.01 respectively). The cumulative amount of urinary excretion of either free-form captopril or its' metabolites was significantly decreased at 2, 4, and 6 hours in chronic renal failure patients (p less than 0.01 or less, respectively). Impairment of kidney function is suggested to be an important factor in the promotion of blood retention of captopril.
采用高效液相色谱法测定了50mg口服剂量卡托普利在正常受试者和慢性肾功能衰竭患者体内的血药浓度及尿排泄情况。在正常受试者中，卡托普利游离形式的最大血药浓度在1小时内达到，6小时后检测不到；给药后2小时内，41%的卡托普利以游离形式和代谢产物排泄到尿液中，6小时内为58%。在平均血清肌酐为5.1mg/dl的慢性肾功能衰竭患者中，吸收常数（Ka）、最大浓度（Cmax）和血药浓度曲线下面积（AUC）与正常受试者相比无显著差异，但消除常数（Ke）和生物半衰期（T1/2）显示卡托普利从血液中消失的时间显著延迟（分别p<0.01）。慢性肾功能衰竭患者在2、4和6小时时，游离形式卡托普利或其代谢产物的尿排泄累积量显著降低（分别p<0.01或更低）。肾功能损害被认为是促进卡托普利血液潴留的一个重要因素。
