Uden D L, Strand L M, Miller K W, Zaske D E
Pharmacotherapy. 1983 Jul-Aug;3(4):235-8. doi: 10.1002/j.1875-9114.1983.tb03263.x.
Substantial error occurs when individual saliva theophylline concentrations are used to predict serum theophylline concentrations. However, the use of saliva theophylline concentrations to determine product bioavailability has never been evaluated. Subjects in this study were 18 stable patients (20-51 yr) with a history of chronic obstructive pulmonary disease. Three preparations--a capsule (Elixophyllin 400 mg), elixir (Elixophyllin 373 mg), and tablet (Theolair 375 mg)--were administered in a randomized crossover design. Serum and saliva samples were obtained pre-dose and 0.25, 0.5, 1, 2, 4, 6, and 8 hours after theophylline administration. The saliva AUC0-infinity and serum AUC0-infinity were highly associated for the elixir (r = 0.84) tablet (r = 0.89), and capsule (r = 0.89). The bioavailability of the tablet and capsule calculated from elixir saliva and elixir serum AUC0-infinity were not significantly different (p = 0.2). The bioavailability of the tablet calculated from saliva and serum was 93% and 102%, respectively. The bioavailability of the capsule calculated from saliva and serum was 113% and 102% respectively. Our data suggests that theophylline bioavailability can be reliably estimated from saliva theophylline concentrations. However, study designs that include larger sample sizes and more frequent sampling may be necessary when determining bioavailability from saliva.
当使用个体唾液中的茶碱浓度来预测血清茶碱浓度时，会出现显著误差。然而，使用唾液茶碱浓度来确定产品生物利用度的情况从未被评估过。本研究的受试者为18名稳定的慢性阻塞性肺疾病患者（年龄20 - 51岁）。采用随机交叉设计给予三种制剂——一种胶囊（埃利克索非林400毫克）、酏剂（埃利克索非林373毫克）和片剂（茶乐平375毫克）。在给药前以及茶碱给药后0.25、0.5、1、2、4、6和8小时采集血清和唾液样本。酏剂的唾液AUC0 - ∞与血清AUC0 - ∞高度相关（r = 0.84），片剂（r = 0.89）和胶囊（r = 0.89）亦是如此。根据酏剂唾液和酏剂血清AUC0 - ∞计算得出的片剂和胶囊的生物利用度无显著差异（p = 0.2）。由唾液和血清计算得出的片剂生物利用度分别为93%和102%。由唾液和血清计算得出的胶囊生物利用度分别为113%和102%。我们的数据表明，可从唾液茶碱浓度可靠地估算茶碱的生物利用度。然而，在通过唾液确定生物利用度时，可能需要设计包含更大样本量和更频繁采样的研究。
