Millar K, Standen P J
Br J Clin Pharmacol. 1982 Jul;14(1):49-55. doi: 10.1111/j.1365-2125.1982.tb04933.x.
1 study examined whether different sustained release systems would cause variation in the effect of an antihistamine, brompheniramine maleate 10 mg, upon mood and psychomotor performance. Two commercial preparations were examined, one giving linear release (LR) of the drug over time, the other releasing the drug in a non-linear fashion (NLR). 2 Thirty-six males were allocated to four separate groups receiving either the drug with LR, drug with NLR, placebo or drug-free control. Single dosage of the drug occurred at 08.30 h and subjects completed mood inventories and performed serial choice reaction time and visual search tasks at 1 h, 2.75 h, 5.5 h and 7.25 h post dosage. 3 The NLR system significantly increased feelings of unco-ordination at 2.75 h and significantly slowed reaction time at both 2.75 and 5.5 h post dosage. The LR system significantly slowed reaction time only at 5.5 h but increased pausing in serial choice performance at that time. Neither system impaired visual search. 4 Results suggest that two preparations having identical active constituents may vary in their effects on psychomotor performance and mood as a function of their sustained release systems. A system giving linear release of the drug can reduce the early post-dosage performance decrement associated with a non-linear release system.
1项研究考察了不同的缓释系统是否会使10毫克马来酸溴苯那敏这种抗组胺药对情绪和精神运动表现的影响产生差异。研究了两种商业制剂,一种能使药物随时间呈线性释放(LR),另一种以非线性方式释放药物(NLR)。36名男性被分为4个独立的组,分别接受LR药物、NLR药物、安慰剂或无药物对照。药物单次给药时间为08:30,受试者在给药后1小时、2.75小时、5.5小时和7.25小时完成情绪量表测试,并进行系列选择反应时间和视觉搜索任务。NLR系统在给药后2.75小时显著增加了不协调感,在给药后2.75小时和5.5小时均显著减慢了反应时间。LR系统仅在5.5小时显著减慢了反应时间,但在那时增加了系列选择表现中的停顿。两种系统均未损害视觉搜索。结果表明,两种具有相同活性成分的制剂,其对精神运动表现和情绪的影响可能因其缓释系统而有所不同。一种能使药物呈线性释放的系统可以减少与非线性释放系统相关的给药后早期表现下降。