Nielsen-Kudsk F, Pedersen A K
Acta Pharmacol Toxicol (Copenh). 1979 May;44(5):391-9. doi: 10.1111/j.1600-0773.1979.tb02350.x.
Dipyridamole, though originally introduced as a coronary vasodilator, has lately been increasingly investigated in the treatment of thromboembolic diseases because of its inhibitory influence upon blood platelet function. The compound is eliminated from the organism by hepatic biotransformation to the monoglucuronide, which almost exclusively is subjected to biliary and faecal excretion with simultaneous partial enterohepatic circulation taking place. Only minute amounts are excreted through the kidneys. In experiments on four normal human volunteers it was found that the serum concentration curve after intravenous administration of dipyridamole rather closely fits the pharmacokinetics of an open two-compartment model with first order, linear disposition kinetics and elimination taking place from the central compartment. Experiments with oral ingestion of the compound could be described by the use of a corresponding pharmacokinetic model with two consecutive first order input steps, representing the dissolution and absorption processes. The disposition rate constants (beta) were within the range of 0.0051--0.0083 min.-1 corresponding to biological half-lives of 84--145 min. The absorption rate constant was about 0.07 min.-1, and the systemic availability of an oral dose of 100 mg dipyridamole in tablets varied from 37 to 66%.
双嘧达莫最初作为一种冠状血管扩张剂引入，近来由于其对血小板功能的抑制作用，在血栓栓塞性疾病的治疗中受到越来越多的研究。该化合物通过肝脏生物转化为单葡糖醛酸苷从机体中消除，几乎完全通过胆汁和粪便排泄，同时存在部分肝肠循环。只有极少量通过肾脏排泄。在对四名正常人类志愿者进行的实验中发现，静脉注射双嘧达莫后的血清浓度曲线相当符合具有一级线性处置动力学且从中央室消除的开放二室模型的药代动力学。口服该化合物的实验可以通过使用具有两个连续一级输入步骤的相应药代动力学模型来描述，这两个步骤分别代表溶解和吸收过程。处置速率常数（β）在0.0051 - 0.0083分钟⁻¹范围内，对应生物半衰期为84 - 145分钟。吸收速率常数约为0.07分钟⁻¹，口服100毫克双嘧达莫片剂的系统利用率在37%至66%之间变化。
