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[健康个体口服和静脉注射胺碘酮后的吸收与消除]

[Amiodarone absorption and elimination after oral and intravenous administration in healthy individuals].

作者信息

Gaete L E, Ortiz M, Soto J, Saavedra I

机构信息

Departamento de Bioquímica, Facultad de Medicina, Universidad de Chile, Santiago de Chile.

出版信息

Rev Med Chil. 1995 Jun;123(6):713-9.

PMID:8525224
Abstract

We studied amiodarone absorption and disposal in eight male healthy subjects aged 21 +/- 1 years old and weighting 69.8 +/- 7.1 kg. An intravenous dose of 5 mg/kg and an oral dose of 600 mg of amiodarone were administered. Amiodarone concentrations were measured by HPLC and calculations were performed using a compartment model independent pharmacokinetic analysis program. After oral administration a Cmax of 1.17 +/- 0.3 mg/ml was achieved at 3.25 +/- 0.46 h (tmax). Absolute bioavailability ranged from 50.4 to 87.8% (68.6 +/- 12.6%). Compared to previous reports, the variability of this parameter is similar and the mean value is one of the highest informed. After intravenous administration, Amiodarone had a half life of 7.53 +/- 0.96 h, a total body clearance of 4.25 +/- 0.73 ml/kg/min and a distribution volume of 2.99 +/- 0.71 l/kg. Except the later figure, which is in the inferior range, all other parameters are within previously reported values. It is concluded that amiodarone absorption and disposal values found in Chilean subjects are similar to those reported abroad.

摘要

我们研究了8名年龄在21±1岁、体重69.8±7.1千克的健康男性受试者对胺碘酮的吸收和代谢情况。静脉注射了5毫克/千克的胺碘酮,并口服了600毫克的胺碘酮。通过高效液相色谱法测量胺碘酮浓度,并使用独立于房室模型的药代动力学分析程序进行计算。口服给药后,在3.25±0.46小时(达峰时间)达到了1.17±0.3毫克/毫升的峰浓度(Cmax)。绝对生物利用度范围为50.4%至87.8%(68.6±12.6%)。与之前的报告相比,该参数的变异性相似,且平均值是所报道的最高值之一。静脉给药后,胺碘酮的半衰期为7.53±0.96小时,全身清除率为4.25±0.73毫升/千克/分钟,分布容积为2.99±0.71升/千克。除了最后一个数值处于较低范围外,所有其他参数均在先前报告的值范围内。得出的结论是,在智利受试者中发现的胺碘酮吸收和代谢值与国外报道的相似。

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