Yap P S, Fung H L
J Pharm Sci. 1978 Apr;67(4):584-6. doi: 10.1002/jps.2600670446.
The plasma nitroglycerin levels obtained after intracardial (0.7 mg/kg), oral (7 mg/kg), and topical (7--14 mg/kg) doses of nitroglycerin in rats are reported. Nitroglycerin followed essentially one-compartment kinetics after intracardial administration, showing a mean half-life of about 4 min and a mean apparent volume of distribution of about 3 liters/kg. After oral drug administration, "flip-flop" kinetics were evident. The mean oral bioavailability was determined to be 1.6%, firmly supporting the contention that nitroglycerin is extensively metabolized during first passage through the liver. Under the experimental conditions studied, no detectable levels of nitroglycerin were observed after topical application.
报道了大鼠心内注射（0.7毫克/千克）、口服（7毫克/千克）和局部应用（7 - 14毫克/千克）硝酸甘油后所测得的血浆硝酸甘油水平。心内注射硝酸甘油后基本呈现一室动力学，平均半衰期约为4分钟，平均表观分布容积约为3升/千克。口服给药后，呈现“翻转”动力学。口服生物利用度平均测定为1.6%，有力地支持了硝酸甘油在首次通过肝脏时会被广泛代谢这一观点。在所研究的实验条件下，局部应用后未观察到可检测水平的硝酸甘油。
