Rolinski B, Wintergerst U, Matuschke A, Füessl H, Goebel F D, Roscher A A, Belohradsky B H
Department of Clinical Chemistry, Children's Hospital, Ludwig-Maximilians University, Munich, Germany.
AIDS. 1991 Jul;5(7):885-8. doi: 10.1097/00002030-199107000-00015.
To facilitate studies of the pharmacokinetic properties of zidovudine, the relationship between plasma and salivary concentrations of the drug was studied, after oral dosage, in 10 HIV-infected patients. Zidovudine concentrations were determined in plasma, unstimulated mixed saliva and citric-acid-stimulated mixed saliva over a period of 3 1/2 hours by high-performance liquid chromatography. Correlation coefficients were r = 0.97 (P less than 0.0001) for stimulated saliva compared with plasma and r = 0.89 (P less than 0.0001) for unstimulated saliva, with average values in unstimulated saliva being 113.8 +/- 44.6% in plasma and 67.8 +/- 25.4% in stimulated saliva. Stimulated saliva values found to be 70% of the total reflected the concentration of the unbound drug in plasma. Except for a shorter half-life time (t1/2) in saliva, pharmacokinetic parameters showed a good correlation in the three types of specimen. These findings and the convenience of sample collection suggest that citric-acid-stimulated saliva might be an appropriate specimen for monitoring zidovudine therapy.
为便于研究齐多夫定的药代动力学特性，对10例HIV感染患者口服该药后血浆和唾液浓度之间的关系进行了研究。通过高效液相色谱法在3.5小时内测定血浆、非刺激性混合唾液和柠檬酸刺激的混合唾液中的齐多夫定浓度。刺激唾液与血浆的相关系数r = 0.97（P < 0.0001），非刺激唾液与血浆的相关系数r = 0.89（P < 0.0001），非刺激唾液中的平均值在血浆中为113.8±44.6%，在刺激唾液中为67.8±25.4%。发现刺激唾液值占总量的70%，反映了血浆中游离药物的浓度。除唾液中的半衰期（t1/2）较短外，三种样本的药代动力学参数显示出良好的相关性。这些发现以及样本采集的便利性表明，柠檬酸刺激的唾液可能是监测齐多夫定治疗的合适样本。
