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辣椒果实单次及重复给药后家兔体内茶碱的药代动力学及代谢情况

Theophylline pharmacokinetics and metabolism in rabbits following single and repeated administration of Capsicum fruit.

作者信息

Bouraoui A, Brazier J L, Zouaghi H, Rousseau M

机构信息

Laboratoire de Pharmacologie, Faculté de Pharmacie, Monastir, Tunisia.

出版信息

Eur J Drug Metab Pharmacokinet. 1995 Jul-Sep;20(3):173-8. doi: 10.1007/BF03189666.

Abstract

Pharmacokinetics and metabolism of theophylline were studied in three groups of male rabbits, after intravenous administration (12 mg/kg), with and without oral ground Capsicum fruit suspension. Compared with control values, plasma theophylline half-life of distribution and of elimination, areas under plasma curves, clearance and volume of distribution did not show any significant difference. On the contrary, the elimination rate constant (k1,0) is significantly different (0.01 < P < 0.05) after a single dose of capsicum and remained unchanged after a repeated dose. Concerning the metabolism of theophylline in rabbits, the results showed that the oral administration of a single dose of Capsicum fruit suspension does not significantly affect the urinary excretion of theophylline and its metabolites--1,3-dimethyluric acid (1,3-DMU) and 1-methyluric acid (1-MU). On the other hand, after a repeated dose of Capsicum fruit for 7 days, the quantity of 1-MU was significantly reduced (0.01 < P < 0.05). In conclusion, it was found that a single dose of Capsicum fruit could affect pharmacokinetic parameters of theophylline (k1,0), while a repeated dose affected the metabolic pathway of xanthine oxidase.

摘要

在三组雄性兔子静脉注射(12毫克/千克)茶碱后,研究了有无口服辣椒果实混悬液情况下茶碱的药代动力学和代谢情况。与对照值相比,茶碱的分布半衰期、消除半衰期、血浆曲线下面积、清除率和分布容积均无显著差异。相反,单次给药辣椒后消除速率常数(k1,0)有显著差异(0.01 < P < 0.05),重复给药后保持不变。关于兔子体内茶碱的代谢,结果表明,单次口服辣椒果实混悬液对茶碱及其代谢产物——1,3 - 二甲基尿酸(1,3 - DMU)和1 - 甲基尿酸(1 - MU)的尿排泄无显著影响。另一方面,重复给药辣椒7天后,1 - MU的量显著减少(0.01 < P < 0.05)。总之,发现单次给药辣椒果实可影响茶碱的药代动力学参数(k1,0),而重复给药则影响黄嘌呤氧化酶的代谢途径。

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