硝酸甘油软膏在健康人体中的药代动力学研究及安全性评价  

Pharmacokinetics of perianal coating nitroglycerin ointment in healthy volunteers

作　　者：邱枫[1] 何晓静[1] 孙亚欣[1] 肇丽梅[1] 

机构地区：[1]中国医科大学附属盛京医院药学部,沈阳110004

出　　处：《中国临床药理学杂志》2013年第10期748-750,754,共4页The Chinese Journal of Clinical Pharmacology

基　　金："重大新药创制"科技重大专项十二五基金资助项目(2012ZX09303015);辽宁省科学技术计划项目基金资助项目(2009225020)

摘　　要：目的研究中国健康志愿者单剂量涂敷硝酸甘油软膏后的药代动力学行为,并观察其对基本生命体征的影响。方法 10名健康志愿者单剂量在肛周涂敷硝酸甘油软膏0.375 g(含硝酸甘油0.75 mg);测定给药后180 min内的血药浓度,并记录试验期间生命体征的变化。结果硝酸甘油药代动力学参数:t max为(7.3±2.3)min,c max为(125.5±50.9)ng·L-1,t1/2为(20.0±11.4)min,AUC0-t为(2079.7±818.5)ng·L-1·min。硝酸甘油软膏给药后60 min内血压与给药前相比有所下降,90 min后恢复到给药前水平。结论肛周涂敷硝酸甘油软膏0.375 g后,体内吸收很少且不规则,给药后对舒张压、收缩压、心率等基本生命体征有一定影响,但均在正常范围内,不具有临床意义。Objective To study the pharmacokinetics of perianal coating nitroglycerin ointment in healthy subjects, and to observe its impact on basic vital signs. Methods Ten healthy subjects were took single peri- anal coating doses of 0. 75 mg nitroglycerin. Plasma concentrations were determined at selected time intervals for 180 min. The changes in vital signs were recorded during the period. Results The main pharmacokinetic parameters of nitroglycerin were as follows respectively： tmax was （7.3 ±2.3） min,cmax was （125.5±50.9） ng·L^-1,t1/2 was （20.0±11.4） min,AUC0-t was （2079.7 ±818.5） ng·L^-1 . min^-1 Within 60 min after administration nitroglycerin ointment, blood pressure decrease as compared with the previous administration, and return to the level of previous administration at 90 min after adminisfration. Conclusion After perianal coating nitroglycerin ointment （equivalent to nitroglycerin 0.75 mg ）, absorption of nitroglycerin was few and irregular. The diastolic pressure, systolic pressure, heart rate and other basic vital signs have a certain changes in the normal range after administration, which have no clinical significance.

关 键 词：硝酸甘油 药代动力学 生命体征 

分 类 号：R969.1[医药卫生—药理学] R944.21[医药卫生—药学]