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[两次单剂量口服硫酸乙酰肝素对人体凝血-纤溶系统的影响。一项药效学研究]

[Effects of 2 single oral doses of mesoglycan on the coagulation-fibrinolysis system in man. A pharmacodynamic study].

作者信息

Messa G, Blardi P, La Placa G, Puccetti L, Ghezzi A

机构信息

Istituto di Clinica Medica Generale e Terapia Medica, Università, Siena.

出版信息

Recenti Prog Med. 1995 Jul-Aug;86(7-8):272-81.

PMID:7569283
Abstract

In this study the profibrinolytic activity of two single oral doses of mesoglycan was evaluated. Furthermore, a mathematical model describing the patterns of the resulting phenomena was applied. Ten patients with impaired fibrinolytic system (euglobulin lysis time > 180 min) were enrolled in the study. In the morning following a 24 hour fast period, the patients were given orally a single dose (100 and 50 mg) of mesoglycan and placebo, with an interval of 48 hours between each treatment. The following parameters were evaluated at the time 0 and after 2, 4, 6, 8, 10 and 12 hours from each administration: tissue plasminogen activator (t-PA) and its inhibitor PAI-1, euglobulin lysis time, plasminogen and alfa-2-antiplasmin as indexes of the fibrinolytic system; aPTT, TT, fibrinogen as indexes of the hemostatic-coagulative system. Mesoglycan showed a dose-dependent profibrinolytic activity, that was also present after placebo but in a less entity. The mathematical study confirms the experimental observations and thus may allow to describe, with a high degree of approximation, the in vivo pharmacology of mesoglycan through the use of the mathematical function.

摘要

在本研究中,评估了两次单剂量口服硫酸软骨素的纤溶活性。此外,应用了一个描述所产生现象模式的数学模型。十名纤维蛋白溶解系统受损(优球蛋白溶解时间>180分钟)的患者参与了该研究。在禁食24小时后的早晨,给患者口服单剂量(100毫克和50毫克)的硫酸软骨素和安慰剂,每次治疗间隔48小时。在每次给药后的0小时以及2、4、6、8、10和12小时评估以下参数:作为纤维蛋白溶解系统指标的组织纤溶酶原激活物(t-PA)及其抑制剂PAI-1、优球蛋白溶解时间、纤溶酶原和α-2-抗纤溶酶;作为止血凝血系统指标的活化部分凝血活酶时间(aPTT)、凝血酶时间(TT)、纤维蛋白原。硫酸软骨素显示出剂量依赖性纤溶活性,安慰剂后也有这种活性,但程度较低。数学研究证实了实验观察结果,因此通过使用数学函数,可能允许高度近似地描述硫酸软骨素的体内药理学。

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