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某些大分子离子复合物对家兔眼用环喷托酯药代动力学和药效动力学的影响。

The effect of some macromolecular ionic complexes on the pharmacokinetics and -dynamics of ocular cyclopentolate in rabbits.

作者信息

Huupponen R, Kaila T, Saettone M F, Monti D, Ilsalo E, Salminen L, Oksala O

机构信息

Department of Clinical Pharmacology, University of Turku, Finland.

出版信息

J Ocul Pharmacol. 1992 Spring;8(1):59-67. doi: 10.1089/jop.1992.8.59.

DOI:10.1089/jop.1992.8.59
PMID:1402295
Abstract

The effect of mucoadhesive polymeric vehicles on the mydriatic efficacy, and on the systemic and ocular absorption of cyclopentolate from eyedrops was studied in albino rabbits. Combining cyclopentolate base to polygalacturonic (CY-PGA) or hyaluronic (CY-HA) acid resulted in an increased mydriatic effect when compared with cyclopentolate hydrochloride (CY-HCl). During the first half an hour, the systemic absorption of cyclopentolate was lower after CY-PGA than after CY-HCl. The ocular penetration of cyclopentolate, based on drug concentrations in aqueous humor 30 minutes after the eyedrop instillation, was increased 3 fold when the polygalacturonate complex was used. CY-PGA, as well as other polymeric salts, might offer a possibility to increase the therapeutic index of cyclopentolate.

摘要

在白化兔中研究了粘膜粘附性聚合物载体对散瞳效果以及环喷托酯从滴眼液中的全身和眼部吸收的影响。与盐酸环喷托酯(CY-HCl)相比,将环喷托酯碱与聚半乳糖醛酸(CY-PGA)或透明质酸(CY-HA)结合可增强散瞳效果。在前半小时内,CY-PGA给药后环喷托酯的全身吸收低于CY-HCl给药后。根据滴眼后30分钟房水中的药物浓度,使用聚半乳糖醛酸盐复合物时环喷托酯的眼部渗透增加了3倍。CY-PGA以及其他聚合物盐可能为提高环喷托酯的治疗指数提供可能性。

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引用本文的文献

1
Plasma concentrations and ocular effects of cyclopentolate after ocular application of three formulations.三种制剂眼部应用后环喷托酯的血浆浓度及眼部效应
Br J Clin Pharmacol. 1993 May;35(5):479-83. doi: 10.1111/j.1365-2125.1993.tb04173.x.