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[关于二甲基 -(2 - 羟乙基)- 烷基溴化铵同系物的二苯乙醇酸酯经颊粘膜吸收的研究。第五篇通讯:关于同系季铵化合物的最佳生物利用度(作者译)]

[Studies on the absorption of benzilic acid esters of homologous dimethyl-(2-hydroxyethyl)-alkylammonium bromides through buccal mucosa. 5th communication: On optimum bioavailability of homologous quaternary ammonium compounds (author's transl)].

作者信息

Lippold B C, Schneider G F

出版信息

Arzneimittelforschung. 1976;26(12):2202-5.

PMID:1037276
Abstract

Distribution studies in vitro predict increasing absorption rates in vivo with increasing distribution coefficients up to a limiting value. Buccal absorption tests with homologous, quaternary cholinesterbromides of benzilic acid do not confirm this hypothesis. The reasons could be the rather hydrophilic properties of the mucosal membranes and thus adsorption of drug to the mucosa. The evaluation of results with undissociated homologous carboxylic acids, however, shows a good correlation between the prediction from in vitro studies and the buccal absorption test.

摘要

体外分布研究预测,随着分布系数增加至极限值,体内吸收率也会增加。用二苯乙醇酸的同源季铵胆碱溴化物进行的颊部吸收试验并未证实这一假设。原因可能是粘膜相当亲水的特性,因此药物会吸附到粘膜上。然而,对未解离的同源羧酸结果的评估表明,体外研究预测与颊部吸收试验之间具有良好的相关性。

相似文献

1
[Studies on the absorption of benzilic acid esters of homologous dimethyl-(2-hydroxyethyl)-alkylammonium bromides through buccal mucosa. 5th communication: On optimum bioavailability of homologous quaternary ammonium compounds (author's transl)].[关于二甲基 -(2 - 羟乙基)- 烷基溴化铵同系物的二苯乙醇酸酯经颊粘膜吸收的研究。第五篇通讯:关于同系季铵化合物的最佳生物利用度(作者译)]
Arzneimittelforschung. 1976;26(12):2202-5.
2
[The optimization of the availability of homologous quaternary ammonium compounds. 2. In vitro studies on the partition of homologous benzilic acid esters of dimethyl-(2-hydroxyethyl)-alkylammonium bromides].[同源季铵化合物可用性的优化。2. 二甲基-(2-羟乙基)-烷基溴化铵的同源二苯乙醇酸酯分配的体外研究]
Arzneimittelforschung. 1975 Jun;25(6):843-52.
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[Optimating the availability of homologous quaternary ammonium compounds/3rd communication: The influence of salts on in vitro distribution of benzilic acid esters of homologous dimethyl-(2-hydroxyethyl)-alkyl-ammoniumbromides (author's transl)].
Arzneimittelforschung. 1975 Nov;25(11):1683-6.
4
[The optimization of availability of homologous quaternary ammonium compounds. 1. Physico-chemical properties and ion-pair dissociation of homologous benzilic acid esters of dimethyl (2-hydroxyethyl)alkylammonium bromides].
Arzneimittelforschung. 1974 Dec;24(12):1952-6.
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[The absorption of homologous alkyl sulphonates of tridihexethyl (author's transl)].[曲美苄铵同源烷基磺酸盐的吸收(作者译)]
Pharmazie. 1980;35(10):612-20.
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[Diffusion of homologous N-alkyl-N-[2-(2,2-diphenyl-2-hydroxyacetyloxy)ethyl]-N,N-dimethyl-ammonium bromides through lipid membranes (author's transl)].同源N-烷基-N-[2-(2,2-二苯基-2-羟基乙酰氧基)乙基]-N,N-二甲基溴化铵通过脂质膜的扩散(作者译)
Arch Pharm (Weinheim). 1978 Mar;311(3):244-7. doi: 10.1002/ardp.19783110310.
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Evaluation of galantamine transbuccal absorption by reconstituted human oral epithelium and porcine tissue as buccal mucosa models: part I.以重组人口腔上皮和猪组织作为颊黏膜模型评估加兰他敏的经颊吸收:第一部分。
Eur J Pharm Biopharm. 2008 Nov;70(3):869-73. doi: 10.1016/j.ejpb.2008.06.025. Epub 2008 Jul 4.
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[Pharmacodynamic study of quaternary ammonium salts of benzilic esters of amino alcohols].氨基醇二苯乙醇酸酯季铵盐的药效学研究
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Buccal penetration enhancers--how do they really work?口腔渗透促进剂——它们究竟是如何起作用的?
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Developments in buccal drug delivery.口腔给药的进展。
Crit Rev Ther Drug Carrier Syst. 1991;8(3):271-303.

引用本文的文献

1
Structure-pharmacokinetics relationship of quaternary ammonium compounds. Correlation of physicochemical and pharmacokinetic parameters.季铵化合物的结构-药代动力学关系。物理化学参数与药代动力学参数的相关性。
Naunyn Schmiedebergs Arch Pharmacol. 1984 Dec;328(2):111-8. doi: 10.1007/BF00512059.