Onyeji C O, Ogunbona F A
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Nigeria.
Pharm World Sci. 1996 Dec;18(6):211-6. doi: 10.1007/BF00735962.
Chloroquine has been reported to be secreted into human saliva. This is a report of a study designed to underscore the importance of the finding. It involved the administration of 600 mg chloroquine per oral to seven volunteers and 150 mg by intramuscular route to six others. Blood and simultaneous saliva samples were collected and analyzed for the drug by an HPLC method. The results showed that chloroquine reaches peak concentration at the same time in both plasma and saliva after oral administration of the drug. A good correlation was obtained between the AUC values derived from saliva and plasma level data. Saliva to plasma concentration ratios obtained after administration of the drug by both routes were high (mean > 11) and exhibited a time-dependent variability. These results suggest that an active process, among other mechanisms, may be involved in the transfer of chloroquine into human saliva. Caution should be exercised in the use of saliva for therapeutic monitoring of chloroquine.
据报道，氯喹可分泌至人唾液中。本文是一项旨在强调该发现重要性的研究报告。该研究让7名志愿者口服600mg氯喹，另外6人肌肉注射150mg氯喹。采集血液及同步的唾液样本，采用高效液相色谱法对样本中的药物进行分析。结果显示，口服该药后，氯喹在血浆和唾液中同时达到峰值浓度。唾液和血浆水平数据得出的AUC值之间具有良好的相关性。两种给药途径后获得的唾液与血浆浓度比值均较高（均值>11），且呈现出时间依赖性变化。这些结果表明，除其他机制外，一个活跃过程可能参与了氯喹向人唾液中的转运。在使用唾液进行氯喹治疗监测时应谨慎。
