Philip-Joet F, Bruguerolle B, Lagier F, Arnaud A
Rev Pneumol Clin. 1986;42(6):279-83.
Plasma levels of two slow-release theophylline preparations, Theostat 200 and Theodur 200, administered in one single evening dose during steady state were compared in a double-blind cross-over study involving 10 male volunteers (mean age: 52.3 +/- 7.5 years) with chronic obstructive lung disease and free from pathology or treatment that might have interfered with theophylline kinetics. Mean areas under the drug plasma concentration curves were 222 +/- 101 mg.h/l with Theostat 200 and 264 +/- 114 mg.h/l with Theodur 200. Mean percentages of fluctuation were 72 +/- 13 and 71 +/- 17 respectively (N.S.). The free fractions measured at peak level were higher with Theodur (9 +/- 2.9 mg/l) than with Theostat (7.1 +/- 2.4 mg/l) (P less than 0.05). While mean values were approximately the same with the two products, interindividual variations were pronounced, with several plasma levels of Theostat 200 in areas regarded as ineffective and several plasma levels of Theodur 200 in areas regarded as toxic. This type of preparation therefore is mostly useful to patients who would benefit from high plasma levels of theophylline in the early morning.
在一项双盲交叉研究中,对10名患有慢性阻塞性肺病且无可能干扰茶碱动力学的病理或治疗情况的男性志愿者(平均年龄:52.3±7.5岁),比较了两种缓释茶碱制剂Theostat 200和Theodur 200在稳态下于一个晚上单次给药后的血浆水平。Theostat 200的药物血浆浓度曲线下平均面积为222±101mg·h/l,Theodur 200为264±114mg·h/l。平均波动百分比分别为72±13和71±17(无显著差异)。在峰值水平测得的游离分数Theodur(9±2.9mg/l)高于Theostat(7.1±2.4mg/l)(P<0.05)。虽然两种产品的平均值大致相同,但个体间差异明显,Theostat 200有几个血浆水平处于被认为无效的范围,Theodur 200有几个血浆水平处于被认为有毒的范围。因此,这种制剂对那些能从清晨高血浆水平茶碱中获益的患者最为有用。