Katagiri Y, Nagasako S, Hayashibara M, Iwamoto K
Department of Pharmacy, Shimane Medical University Hospital, Izumo, Japan.
J Pharm Pharmacol. 1991 Jul;43(7):513-5. doi: 10.1111/j.2042-7158.1991.tb03525.x.
To investigate the kinetics and correlation between serum and saliva levels of mexiletine, serum (total and unbound) and saliva drug concentration-time courses have been analysed in five normal healthy volunteers after administration of a single oral dose (200 mg) of the drug. Mexiletine levels in saliva were always higher than those in serum. The drug concentration-time curve in each sample was analysed according to the non-linear least squares regression program MULTI, for a two-compartment model with first-order absorption. The saliva drug concentration in the post-absorption phase was found to be well correlated with either corresponding serum total or serum unbound drug level in four of the subjects. Although there was a large inter-individual variation in the ratio of saliva to serum drug concentrations as well as in the pharmacokinetic parameters, an almost consistent ratio was obtained in each individual.
为研究美西律血清和唾液水平之间的动力学及相关性，对5名正常健康志愿者单次口服一剂（200mg）该药物后的血清（总药物和游离药物）及唾液药物浓度-时间过程进行了分析。唾液中美西律水平始终高于血清中的水平。根据非线性最小二乘回归程序MULTI，对具有一级吸收的二室模型分析每个样本中的药物浓度-时间曲线。在4名受试者中，发现吸收后阶段的唾液药物浓度与相应的血清总药物水平或血清游离药物水平具有良好的相关性。尽管唾液与血清药物浓度之比以及药代动力学参数存在较大的个体间差异，但每个个体的比值几乎一致。
