Suryawati S, Santoso B
Department of Clinical Pharmacology, Faculty of Medicine, Gadjah Mada University, Jogyakarta, Indonesia.
Int J Clin Pharmacol Ther Toxicol. 1991 Dec;29(12):474-8.
Measurement of metronidazole concentration and its pharmacokinetics from saliva and serum samples have been conducted in 8 healthy volunteers. The pharmacokinetic study was carried out after an oral ingestion of 500 mg tablet of the drug, simultaneously from saliva and serum samples. The study showed a significant positive correlation between saliva and serum metronidazole concentrations. However, a better correlation was obtained during the elimination phase (r = 0.90, n = 51, p less than 0.001) compared to that during the absorption phase (r = 0.76, n = 26, p less than 0.001). The overall ratio of saliva to serum concentration was 0.93 +/- (SEM 0.05). Not surprisingly, the half-life of metronidazole obtained from saliva samples (8.03 +/- SEM 0.59 hours) was similar to that from serum (7.97 +/- SEM 0.39 hours). The mean area under the drug concentration (AUC0-infinity) in saliva was 153.56 +/- (SEM 16.42 micrograms/ml hour) and that in serum was 179.76 +/- (SEM 11.70 micrograms/ml hour), yielding a saliva to serum ratio of 0.87 (+/- SEM 0.10). It could be concluded, therefore, that the measurement of metronidazole concentration from saliva can be used for the estimation of its pharmacokinetics and may also be used as reliable and convenient method for bioequivalence studies.
在8名健康志愿者中进行了唾液和血清样本中甲硝唑浓度及其药代动力学的测定。在口服500毫克该药物片剂后，同时采集唾液和血清样本进行药代动力学研究。研究表明，唾液和血清中甲硝唑浓度之间存在显著正相关。然而，与吸收阶段相比，消除阶段的相关性更好（r = 0.90，n = 51，p < 0.001），吸收阶段的相关性为（r = 0.76，n = 26，p < 0.001）。唾液与血清浓度的总体比值为0.93±（标准误0.05）。不出所料，从唾液样本中测得的甲硝唑半衰期（8.03±标准误0.59小时）与血清中的半衰期（7.97±标准误0.39小时）相似。唾液中药物浓度的平均药时曲线下面积（AUC0-∞）为153.56±（标准误16.42微克/毫升·小时），血清中的为179.76±（标准误11.70微克/毫升·小时），唾液与血清的比值为0.87（±标准误0.10）。因此，可以得出结论，测定唾液中甲硝唑浓度可用于估算其药代动力学，也可作为生物等效性研究的可靠且便捷的方法。
