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环糊精对药物诱导的体外溶血的保护作用。

Protective effects of cyclodextrins on drug-induced hemolysis in vitro.

作者信息

Uekama K, Irie T, Sunada M, Otagiri M, Tsubaki K

出版信息

J Pharmacobiodyn. 1981 Feb;4(2):142-4. doi: 10.1248/bpb1978.4.142.

Abstract

beta-Cyclodextrin (beta-CyD) significantly protected the human erythrocytes from hemolysis and shape changes induced with chlorpromazine and flufenamic acid in isotonic solution. A good correlation between the stability constants of inclusion complexes (beta- greater than gamma- greater than alpha-CyD) and the inhibitory effects on drug-induced hemolysis was found. From the observations of drug uptake into erythrocytes and changes in surface tension, the protective effects of CyDs appeared to be due to the decrease in effective concentration of drug through inclusion complexation rather than the direct interaction of CyDs with erythrocyte membrane.

摘要

β-环糊精(β-CyD)能显著保护人类红细胞,使其免受等渗溶液中氯丙嗪和氟芬那酸诱导的溶血和形态变化影响。发现包合物的稳定常数(β-环糊精大于γ-环糊精大于α-环糊精)与对药物诱导溶血的抑制作用之间存在良好的相关性。从药物摄入红细胞的观察结果和表面张力的变化来看,环糊精的保护作用似乎是由于通过包合作用降低了药物的有效浓度,而不是环糊精与红细胞膜的直接相互作用。

相似文献

8
Reduction in the local tissue toxicity of chlorpromazine by beta-cyclodextrin complexation.
J Pharmacobiodyn. 1983 Oct;6(10):790-2. doi: 10.1248/bpb1978.6.790.

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