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色甘酸钠在人体静脉注射和吸入给药后的药代动力学。

The pharmacokinetics of sodium cromoglycate in man after intravenous and inhalation administration.

作者信息

Neale M G, Brown K, Hodder R W, Auty R M

出版信息

Br J Clin Pharmacol. 1986 Oct;22(4):373-82. doi: 10.1111/j.1365-2125.1986.tb02905.x.

DOI:10.1111/j.1365-2125.1986.tb02905.x
PMID:3094571
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1401160/
Abstract

The pharmacokinetics of sodium cromoglycate in four healthy volunteers after slow intravenous infusion have been evaluated following measurement of plasma concentrations by radioimmunoassay. The results confirm earlier findings that sodium cromoglycate is rapidly eliminated from the body and that the data can be fitted to a two compartment open model. The pharmacokinetic parameters derived from the intravenous administration were used to evaluate the pharmacokinetics after inhalation administration via the Spinhaler. A model for absorption from the lungs is described which involves absorption at two different rates; this gives a better fit to the observed data than a single absorption rate. A fast absorption rate constant with a mean value of 0.54 min-1 and a slower rate constant with a mean value of 0.0097 min-1 were found. Of a mean total of 2.84 mg absorbed from a 20 mg inhaled dose, 0.68 +/- 0.15 (s.e. mean) mg were absorbed at the fast rate and 2.17 +/- 0.37 mg at the slower rate. These rates probably reflect absorption from different sites within the lungs. The results may have important implications for interpretation of clinical findings.

摘要

通过放射免疫分析法测定血浆浓度后,评估了4名健康志愿者缓慢静脉输注色甘酸钠后的药代动力学。结果证实了早期的研究结果,即色甘酸钠能迅速从体内消除,且数据可拟合为二室开放模型。静脉给药得到的药代动力学参数用于评估通过Spinhaler吸入给药后的药代动力学。描述了一种肺部吸收模型,该模型涉及两种不同速率的吸收;与单一吸收速率相比,这能更好地拟合观察到的数据。发现快速吸收速率常数的平均值为0.54 min⁻¹,较慢吸收速率常数的平均值为0.0097 min⁻¹。从20 mg吸入剂量中平均总共吸收2.84 mg,其中0.68±0.15(标准误均值)mg以快速率吸收,2.17±0.37 mg以慢速率吸收。这些速率可能反映了肺部不同部位的吸收情况。这些结果可能对临床研究结果的解释具有重要意义。

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本文引用的文献

1
Determination of sodium cromoglycate in human urine by high-performance liquid chromatography on an anion-exchange column.采用阴离子交换柱高效液相色谱法测定人尿中色甘酸钠的含量。
J Chromatogr. 1984 Jan 13;305(1):228-32. doi: 10.1016/s0378-4347(00)83335-6.
2
Radioimmunoassay of sodium cromoglycate in human plasma.人血浆中色甘酸钠的放射免疫测定法
Ann Clin Biochem. 1983 Jan;20 Pt 1:31-6. doi: 10.1177/000456328302000105.
3
The pharmacokinetic assessment of sodium cromoglycate.色甘酸钠的药代动力学评估。
J Pharm Pharmacol. 1983 May;35(5):289-92. doi: 10.1111/j.2042-7158.1983.tb02936.x.
4
Hepatic and renal clearance of sodium cromoglycate.色甘酸钠的肝清除率和肾清除率。
J Pharm Pharmacol. 1981 Nov;33(11):744-5. doi: 10.1111/j.2042-7158.1981.tb13922.x.
5
Plasma levels and urinary excretion of disodium cromoglycate afer inhalation by human volunteers.色甘酸二钠经人体志愿者吸入后的血浆水平及尿排泄情况。
Toxicol Appl Pharmacol. 1971 Oct;20(2):147-56. doi: 10.1016/0041-008x(71)90041-x.
6
Distribution and metabolism of disodium cromoglycate in rats.色甘酸钠在大鼠体内的分布与代谢
Toxicol Appl Pharmacol. 1970 Nov;17(3):691-8. doi: 10.1016/0041-008x(70)90043-8.
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