Williams P E, Alwazir Y A, Routledge P A, Campbell I A
Br J Clin Pharmacol. 1986 Oct;22(4):383-7. doi: 10.1111/j.1365-2125.1986.tb02906.x.
Plasma and saliva theophylline concentrations were measured in 21 asthmatic subjects receiving chronic oral therapy with a new sustained-release theophylline capsule (K1B Riker) given as a once daily dose, after titration to achieve a before-dose concentration of 8 mg l-1 or greater, or to the maximum dose of 1200 mg of theophylline daily. Plasma concentrations rose from a mean +/- s.d. minimum concentration (Cmin) of 7.9 +/- 2.3 mg l-1 to a mean maximum of 13.6 +/- 3.3 mg l-1 at a median time of 10 h after dosing. Saliva theophylline concentrations were closely related to the plasma theophylline concentration both between and within subjects with a mean saliva to plasma concentration ratio between subjects (S/P ratio) of 0.62 (+/- 0.05) and a mean within subject coefficient of variation of 8.2% (+/- 4.5%). There was a significant but small (10%) change in the mean S/P ratio during the dosing interval. Peak expiratory flow rate (PEFR) changed slightly but significantly during the dosing interval but forced expiratory volume in one second (FEV1) and forced vital capacity (FVC) did not. The drug was well tolerated at the dose used (600-1200 mg once daily).
对21名接受新型缓释茶碱胶囊（K1B利凯尔）长期口服治疗的哮喘患者进行了血浆和唾液茶碱浓度测定，该胶囊每日服用一次，经滴定使给药前浓度达到8mg/L或更高，或达到每日1200mg茶碱的最大剂量。给药后血浆浓度从平均±标准差的最低浓度（Cmin）7.9±2.3mg/L升至平均最高浓度13.6±3.3mg/L，中位时间为给药后10小时。唾液茶碱浓度在受试者之间和受试者内部均与血浆茶碱浓度密切相关，受试者之间唾液与血浆浓度比（S/P比）平均为0.62（±0.05），受试者内部变异系数平均为8.2%（±4.5%）。给药间隔期间平均S/P比有显著但较小（10%）的变化。给药间隔期间呼气峰值流速（PEFR）有轻微但显著的变化，但一秒用力呼气量（FEV1）和用力肺活量（FVC）没有变化。所用剂量（每日一次600 - 1200mg）时该药物耐受性良好。
