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首页> 外文期刊>The Veterinary Journal >Pharmacokinetics of the low molecular weight heparin dalteparin in cats.
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Pharmacokinetics of the low molecular weight heparin dalteparin in cats.

机译:低分子量肝素达肝素在猫中的药代动力学。

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Low molecular weight heparin (LMWH) is used as an anticoagulant in cats although only limited pharmacokinetic data are available in this species. The aim of the present study was to establish the pharmacokinetics of dalteparin in cats based on anti-FXa heparin activities. Groups of clinically healthy cats (six animals per treatment) received individual LMWH injections at three different doses intravenously (IV) (25, 50, 100 anti-factor Xa international units [IU anti-FXa]/kg) or subcutaneously (SC) (50, 100, 200 IU anti-FXa/kg). Blood samples were collected before and at various times after injection. Anti-FXa activity was measured with a chromogenic substrate test. Following IV injection, maximum plasma heparin activities (Cmax) were 0.67+or-0.14, 1.44+or-0.22 and 2.87+or-0.38 IU anti-FXa/mL, respectively. The calculated mean half-life (t1/2) was between 39 and 57 min and was not significantly dose-dependent (P=0.139). The volume of distribution (35-39 mL/kg) was almost equivalent to the plasma volume. After SC injection, Cmax values of 0.41+or-0.10, 0.86+or-0.17 or 1.91+or-0.16 IU anti-FXa/mL, respectively, were calculated at 91-110 min post-injection. The t1/2 values were between 106 and 122 min and were not significantly influenced by dose (P=0.784). The bioavailability after SC injection was approximately 100%. The high bioavailability of the SC administered LMWH dalteparin in cats was consistent with other species and indicated predictable blood levels. However, the comparatively short t1/2 may indicate the necessity of multiple daily injections, which should be verified in clinical trials.
机译:低分子量肝素(LMWH)在猫中用作抗凝剂,尽管在该物种中仅可获得有限的药代动力学数据。本研究的目的是建立基于抗FXa肝素活性的达肝素在猫体内的药代动力学。临床健康的猫组(每只治疗六只动物)以三种不同剂量分别静脉注射(IV)(25、50、100抗Xa因子国际单位[IU anti-FXa] / kg)或皮下(SC)接受LMWH注射( 50、100、200 IU抗FXa / kg)。在注射之前和之后的不同时间收集血液样品。用生色底物测试测量抗FXa活性。静脉注射后,最大血浆肝素活性( C max )分别为0.67+或-0.14、1.44+或-0.22和2.87+或-0.38 IU抗-FXa / mL , 分别。计算的平均半衰期( t 1/2 )在39至57分钟之间,并且与剂量没有显着相关性( P = 0.139 )。分布体积(35-39 mL / kg)几乎等于血浆体积。注射SC后,分别计算出 C max 值分别为0.41+或-0.10、0.86+或-0.17或1.91+或-0.16 IU抗-FXa / mL在注射后91-110分钟。 t 1/2 值在106和122分钟之间,并且不受剂量的显着影响( P = 0.784)。 SC注射后的生物利用度约为100%。在猫中,SC施用LMWH达肝素的高生物利用度与其他物种一致,并表明可预测的血液水平。但是,相对较短的 t 1/2 可能表明需要每天多次注射,这需要在临床试验中加以验证。

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