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静脉注射后茶碱在骆驼体内的处置情况。

The disposition of theophylline in camels after intravenous administration.

作者信息

Wasfi I A, Elghazali M, Boni N S, Hadi A A, Alhadrami G A, Almuhrami A M, Alkatheeri N A, Barezaiq I M, Agha B A, Wajid S A

机构信息

Camelracing Laboratory, Abu Dhabi, United Arab Emirates.

出版信息

J Vet Pharmacol Ther. 1999 Aug;22(4):255-60. doi: 10.1046/j.1365-2885.1999.00220.x.

Abstract

The pharmacokinetics of theophylline were determined after an intravenous (i.v.) dose of 2.36 mg/kg in six camels and 4.72 mg/kg body weight in three camels. The data obtained (median and range) for the low and high dose, respectively, were as follows: the distribution half-lives (t1/2 alpha) were 1.37 (0.64-3.25) and 2.66 (0.83-3.5) h, the elimination half-lives (t1/2 beta) were 11.8 (8.25-14.9) and 10.4 (10.0-13.5) h, the steady state volumes of distribution (Vss) were 0.88 (0.62-1.54) and 0.76 (0.63-0.76) L/kg, volumes of the central compartment (Vc) were 0.41 (0.35-0.63) and 0.51 (0.36-0.52) L/kg, total body clearances (Clt) were 62.3 (39.4-97.0) and 50.2 (47.7-67.4) mL/h.kg body weight and renal clearance (Vr) for the low dose was 0.6 (0.42-0.96) mL/h.kg body weight. There was no significant difference in the pharmacokinetic parameters between the two doses. Theophylline protein binding at a concentration of 5 micrograms/mL was 32.2 +/- 3.3%. Caffeine was identified as a theophylline metabolite but its concentration in serum and urine was small. Based on the pharmacokinetic values obtained in this study, a dosage of 7.5 mg/kg body weight administered by i.v. injection at 12 h intervals can be recommended. This dosing regimen should achieve an average steady state serum concentration of 10 micrograms/mL with peak serum concentration not exceeding 15 micrograms/mL.

摘要

对6头骆驼静脉注射剂量为2.36 mg/kg以及3头骆驼静脉注射剂量为4.72 mg/kg体重的氨茶碱后,测定了其药代动力学。低剂量和高剂量分别获得的数据(中位数和范围)如下:分布半衰期(t1/2α)分别为1.37(0.64 - 3.25)小时和2.66(0.83 - 3.5)小时,消除半衰期(t1/2β)分别为11.8(8.25 - 14.9)小时和10.4(10.0 - 13.5)小时,稳态分布容积(Vss)分别为0.88(0.62 - 1.54)L/kg和0.76(0.63 - 0.76)L/kg,中央室容积(Vc)分别为0.41(0.35 - 0.63)L/kg和0.51(0.36 - 0.52)L/kg,总体清除率(Clt)分别为62.3(39.4 - 97.0)和50.2(47.7 - 67.4)mL/h·kg体重,低剂量的肾清除率(Vr)为0.6(0.42 - 0.96)mL/h·kg体重。两种剂量的药代动力学参数无显著差异。浓度为5微克/毫升时氨茶碱的蛋白结合率为32.2±3.3%。咖啡因被鉴定为氨茶碱的代谢产物,但其在血清和尿液中的浓度较低。基于本研究获得的药代动力学值,可推荐每12小时静脉注射一次,剂量为7.5 mg/kg体重。这种给药方案应能使平均稳态血清浓度达到10微克/毫升,血清峰值浓度不超过15微克/毫升。

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