Huang J D
Department of Pharmacology, National Cheng Kung University, Medical College, Tainan, Taiwan, Republic of China.
J Pharm Sci. 1988 Nov;77(11):959-62. doi: 10.1002/jps.2600771113.
The ability of activated charcoal to enhance the drug elimination of two enantiomers, R- and S-disopyramide, was compared in rabbits. Orally administered activated charcoal significantly decreased the area under the serum concentration curve of R-disopyramide, whereas the same treatment had no effect on that of S-disopyramide. The difference could be explained by the difference in the hepatic extraction ratio of two enantiomers in rabbits. S-Disopyramide is a drug of high hepatic extraction ratio in rabbits and R-disopyramide is of intermediate hepatic extraction ratio. Equations were derived to illustrate the influence of the hepatic extraction ratio on the apparent gastrointestinal clearance. A higher hepatic extraction ratio decreases the apparent gastrointestinal clearance of a drug. This phenomenon may explain some unsuccessful experiments of gastrointestinal dialysis. When considering the use of activated charcoal to enhance systemic drug elimination, the hepatic extraction ratio of the drug should be included.
在兔体内比较了活性炭增强两种对映体（R-和S-双异丙吡胺）药物消除的能力。口服活性炭显著降低了R-双异丙吡胺的血清浓度曲线下面积，而相同处理对S-双异丙吡胺的血清浓度曲线下面积无影响。这种差异可以用兔体内两种对映体肝提取率的差异来解释。S-双异丙吡胺在兔体内是高肝提取率药物，R-双异丙吡胺是中等肝提取率药物。推导了一些方程来说明肝提取率对表观胃肠清除率的影响。较高的肝提取率会降低药物的表观胃肠清除率。这种现象可能解释了一些胃肠透析实验的失败。在考虑使用活性炭增强全身药物消除时，应考虑药物的肝提取率。
