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局部给药的药代动力学评估:大鼠睾丸内和肾内给予醋硝香豆素

Pharmacokinetic evaluation of local drug delivery: the intratesticular and intrarenal administration of acenocoumarol in the rat.

作者信息

Daemen M J, Vervoort-Peters H T, Thijssen H H

机构信息

Department of Pharmacology, University of Limburg, Maastricht, The Netherlands.

出版信息

J Pharm Pharmacol. 1988 Apr;40(4):283-5. doi: 10.1111/j.2042-7158.1988.tb05245.x.

DOI:10.1111/j.2042-7158.1988.tb05245.x
PMID:2900311
Abstract

According to theory, the regional increase in drug concentration during target organ directed drug delivery as compared with systemic drug delivery is related to the quotient of the clearance of the drug and the blood flow of the target organ. We investigated the steady-state pharmacokinetic disposition of S-acenocoumarol in plasma, liver, testis, and kidney following its administration (constant rate infusion by an osmotic minipump) directly into the testis or the kidney of rats. The effects of clearance induction (phenobarbitone treatment) on the disposition of the drug were also investigated. The results confirm the theory of target-directed drug delivery.

摘要

根据理论,与全身给药相比,靶向器官给药过程中药物在靶器官区域的浓度增加与药物清除率和靶器官血流量的商有关。我们通过渗透微型泵以恒定速率输注,将S-醋硝香豆素直接注入大鼠的睾丸或肾脏,研究了其在给药后血浆、肝脏、睾丸和肾脏中的稳态药代动力学分布。还研究了清除率诱导(苯巴比妥治疗)对药物分布的影响。结果证实了靶向给药的理论。

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