Czejka M J, Zwoelfer N, Podesser B
Institute for Pharmaceutical Chemistry, University of Vienna, Austria.
Farmaco. 1992 Mar;47(3):387-91.
In-vitro binding of calcium-antagonists gallopamil and verapamil (and its main metabolite norverapamil) to human red blood cells (RBCs) was investigated. The drugs are bound reversibly and dose dependent to RBCs in the same order of magnitude, with partition-coefficients of kRBC = 0.12-0.34 for gallopamil, kRBC = 0.10-0.30 for verapamil and kRBC = 0.10-0.27 for norverapamil. The data indicate that, although RBCs may act as subcompartments of the blood for this class of compounds, they may have no influence on therapeutic plasma concentrations, due to their low kRBC.
研究了钙拮抗剂加洛帕米和维拉帕米（及其主要代谢产物去甲维拉帕米）与人红细胞（RBC）的体外结合情况。这些药物与红细胞可逆性结合且呈剂量依赖性，结合程度在同一数量级，加洛帕米的红细胞分配系数kRBC = 0.12 - 0.34，维拉帕米的kRBC = 0.10 - 0.30，去甲维拉帕米的kRBC = 0.10 - 0.27。数据表明，尽管红细胞可能作为这类化合物在血液中的亚区室，但由于其较低的红细胞分配系数，它们可能对治疗性血浆浓度没有影响。
