Isenschmid M, Müller M, Bührer M, Vorkauf H, Bircher J
Int J Clin Pharmacol Ther Toxicol. 1985 Jul;23(7):345-51.
The absolute bioavailability of glyceryl trinitrate from a transdermal therapeutic system (Nitroderm TTS, 20 cm2) was assessed with a new method in 6 healthy volunteers. Instead of measuring plasma concentrations the pharmacological effects of glyceryl trinitrate were followed by digital plethysmography. Each experiment consisted of the establishment of an intravenous dose response curve which was followed by a 1-hour application of the transdermal system and a second intravenous dose response curve. The investigations were repeated after pretreatment of each subject with 0.4 mg pindolol i.v. The results show a satisfactory overall consistency of the data and indicate a release rate of 4.4 +/- SD 1.7 micrograms/min of bioavailable glyceryl trinitrate during the first hour of application of this transdermal system. This corresponds to 75 +/- 29% of the release rate obtained by analysis of residual amounts in the TTS.
采用一种新方法在6名健康志愿者中评估了经皮治疗系统（Nitroderm TTS，20 cm²）中硝酸甘油的绝对生物利用度。未测定血浆浓度，而是通过数字体积描记法跟踪硝酸甘油的药理作用。每个实验包括建立静脉给药剂量反应曲线，随后应用经皮系统1小时，然后再建立第二条静脉给药剂量反应曲线。在每名受试者静脉注射0.4 mg吲哚洛尔进行预处理后重复这些研究。结果表明数据总体一致性良好，并表明在应用该经皮系统的第一小时内，生物可利用硝酸甘油的释放速率为4.4±标准差1.7微克/分钟。这相当于通过分析经皮治疗系统中的残留量所获得释放速率的75±29%。
