Hasan M M, el-Sayed Y M, Abdelaziz A A
Department of Pharmacology, Faculty of Medicine, Jordan University of Science and Technology, Irbid.
J Pharm Pharmacol. 1990 Feb;42(2):85-8. doi: 10.1111/j.2042-7158.1990.tb05359.x.
The effect of oral administration of activated charcoal on total body clearance of gentamicin administered intravenously (2 mg kg-1) has been studied in normal rabbits and rabbits with induced renal failure. Gastric intubation of a single dose (10 g) of activated charcoal to normal rabbits produced a significant reduction in gentamicin serum concentrations compared to control. Significant differences between treated and control groups, compatible with enhancement of gentamicin elimination, were observed in the calculated pharmacokinetic parameters (Kel, t 1/2, CL and AUC). To examine whether renal failure could augment the effect of activated charcoal in enhancing the systemic clearance of gentamicin, uranyl nitrate was used (0.75 mg kg-1, i.v.) to induce acute renal failure in rabbits. The derived pharmacokinetic parameters of gentamicin during the control phase in these animals were consistent with severe renal failure. The administration of activated charcoal, 2.5 h following gentamicin injection, produced a steeper decline in gentamicin concentration-time profiles and significant changes in Kel, t 1/2 and CL. The Kel and CL values increased to about 200%, while the t 1/2 value decreased to about 50%. The apparent changes in the pharmacokinetic parameters induced by charcoal administration were more marked in rabbits with renal failure than in normal rabbits; however, induction of renal failure did not augment the charcoal-induced clearance of gentamicin quantitatively.
已在正常兔和诱导肾衰竭的兔中研究了口服活性炭对静脉注射庆大霉素（2 mg kg-1）的全身清除率的影响。与对照组相比，给正常兔胃内插管单剂量（10 g）活性炭可使庆大霉素血清浓度显著降低。在计算的药代动力学参数（Kel、t 1/2、CL和AUC）中，观察到治疗组和对照组之间存在显著差异，这与庆大霉素消除增强一致。为了研究肾衰竭是否会增强活性炭对提高庆大霉素全身清除率的作用，使用硝酸铀酰（0.75 mg kg-1，静脉注射）诱导兔急性肾衰竭。这些动物在对照期庆大霉素的推导药代动力学参数与严重肾衰竭一致。在注射庆大霉素2.5小时后给予活性炭，庆大霉素浓度-时间曲线下降更陡，Kel、t 1/2和CL发生显著变化。Kel和CL值增加至约200%，而t 1/2值降至约50%。肾衰竭兔中活性炭给药引起的药代动力学参数的明显变化比正常兔更显著；然而，诱导肾衰竭并没有在数量上增强活性炭诱导的庆大霉素清除率。
