Rask H S, Angelo H R, Christensen H R
Department of Clinical Biochemistry, Bispebjerg Hospital, Copenhagen, Denmark.
Chirality. 1998;10(9):808-12. doi: 10.1002/(SICI)1520-636X(1998)10:9<808::AID-CHIR6>3.0.CO;2-H.
rac-Isradipine is a dihydropyridine type calcium antagonist. Its calcium entry blocking effect is due primarily to the (+)-(S)-enantiomer. This study describes a sensitive enantioselective method for the determination of isradipine in human serum. Following alkaline extraction into hexane, the enantiomers of isradipine are separated quantitatively by high-performance liquid chromatography on a Chiralcel OJ column at 39 degrees C. The collected fractions were evaporated and assayed using capillary gas chromatography on a HP 50+ column with nitrogen selective detection. Using 2.0 ml of serum, 0.7 nmol/1 (0.26 ng/ml) of each enantiomer could be determined with acceptable precision. The method has successfully been used to measure (+)-(S)- and (-)-(R)-isradipine concentrations in samples from volunteers after intravenous and oral administration of isradipine.
消旋尼群地平是一种二氢吡啶类钙拮抗剂。其钙通道阻滞作用主要归因于(+)-(S)-对映体。本研究描述了一种灵敏的对映体选择性方法，用于测定人血清中的尼群地平。将血清用碱萃取到己烷中后，尼群地平的对映体在39℃下于Chiralcel OJ柱上通过高效液相色谱法定量分离。收集的馏分经蒸发后，使用配备氮选择性检测的HP 50+柱通过毛细管气相色谱法进行测定。使用2.0 ml血清时，每种对映体的测定浓度可达0.7 nmol/1(0.26 ng/ml)，精密度良好。该方法已成功用于测定志愿者静脉注射和口服尼群地平后样本中(+)-(S)-和(-)-(R)-尼群地平的浓度。
