Motheová O, Zemánek M, Faberova V, Trnovec T, Gabauer I, Styk J, Durisová M, Nosálová V
J Pharm Pharmacol. 1985 Nov;37(11):816-9. doi: 10.1111/j.2042-7158.1985.tb04975.x.
The absorption rate of the beta-adrenoceptor blocking drug, exaprolol, from the gastrointestinal tract was studied using in-situ methods in the rat and dog. Exaprolol was rapidly absorbed from the small and large intestine of rats and from the ileum of dogs. The cardiac output and regional blood flow decreased in rats to approximately one half of the original values within 30 min of the in-situ experiment. The logarithm of the amount vs time plots from dogs were linear, whereas with rats a curvilinearity appeared apparently because of the blood flow-limited absorption kinetics of this highly lipophilic drug. The data obtained suggest that exaprolol is suitable for administration in sustained release form.
采用大鼠和犬的原位方法研究了β-肾上腺素受体阻断药依沙洛尔从胃肠道的吸收速率。依沙洛尔能迅速从大鼠的小肠和大肠以及犬的回肠吸收。原位实验30分钟内,大鼠的心输出量和局部血流量降至约为初始值的一半。犬的药量对数-时间图呈线性,而大鼠的图则呈明显的曲线,这是由于这种高度亲脂性药物的血流限制吸收动力学所致。所得数据表明依沙洛尔适合制成缓释制剂给药。