Andriuoli G, Caramazza I, Galimberti G, Zoppetti G, Benedini F, Sala A, Del Soldato P
Italfarmaco Research Center, Cinisello Balsamo, Milan, Italy.
Haemostasis. 1992;22(3):113-6. doi: 10.1159/000216305.
The intraduodenal absorption of a new low-molecular-weight heparin (LMWH) diamine salt (ITF 1331) was compared with the parent compound ITF 1060 and with sodium LMWH, in anaesthetized rabbits. The administration of either salt, but not of sodium LMWH, resulted in a dose-related increase in plasma anti-Xa activity. In this respect ITF 1331 was slightly superior to ITF 1060, and in acute-toxicity studies the counterion itself (ITF 258) was less toxic than that in ITF 1060 (counterion No. 4). These data confirm that a tertiary diamine within the counterion is an important structural requirement for the bioavailability of heparin by the intraduodenal route, and suggest that ITF 1331 may represent an important advance in the search for an oral heparin.
在麻醉兔中，比较了一种新型低分子量肝素（LMWH）二胺盐（ITF 1331）与母体化合物ITF 1060以及低分子量肝素钠的十二指肠内吸收情况。给予任何一种盐，而非低分子量肝素钠，都会导致血浆抗Xa活性呈剂量相关增加。在这方面，ITF 1331略优于ITF 1060，并且在急性毒性研究中，抗衡离子本身（ITF 258）的毒性低于ITF 1060中的抗衡离子（抗衡离子4号）。这些数据证实，抗衡离子中的叔二胺是十二指肠途径肝素生物利用度的重要结构要求，并表明ITF 1331可能代表了口服肝素研究的一项重要进展。
