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评估磺丁基醚β-环糊精作为几种药物的增溶剂/稳定剂的性能。

Evaluation of a sulfobutyl ether beta-cyclodextrin as a solubilizing/stabilizing agent for several drugs.

作者信息

Ueda H, Ou D, Endo T, Nagase H, Tomono K, Nagai T

机构信息

Department of Physical Chemistry, Hoshi University, Tokyo, Japan.

出版信息

Drug Dev Ind Pharm. 1998 Sep;24(9):863-7. doi: 10.3109/03639049809088532.

Abstract

To evaluate the potential use of beta-cyclodextrin sulfobutyl ether, 7 sodium salt (SBE7-beta-CD) as a drug solubilizing and stabilizing agent, the solubilizing effects of SBE7-beta-CD on 22 different poorly water-soluble drugs were compared with those of intact beta-CD and heptakis-(2,6-di-O-methyl)-beta-CD (DMCD). SBE7-beta-CD was generally a more effective solubilizer for poorly water-soluble drugs than was intact beta-CD, but SBE7-beta-CD was not as effective as DMCD. The effects of SBE7-beta-CD on the acid hydrolysis rate of prostaglandin I2, the alkaline hydrolysis rate of indomethacin, the dehydration of prostaglandin E1, and the isomerization of prostaglandin A1 were also investigated and compared to those for intact beta-CD, DMCD, and 2,3,6 partially methylated-beta-CD (PMCD). The stabilizing effects of SBE7-beta-CD on chemically unstable drugs were generally higher than those of other CDs.

摘要

为评估磺丁基醚-β-环糊精七钠盐(SBE7-β-CD)作为药物增溶剂和稳定剂的潜在用途,将SBE7-β-CD对22种不同的难溶性药物的增溶效果与未修饰的β-环糊精和七(2,6-二-O-甲基)-β-环糊精(DMCD)的增溶效果进行了比较。总体而言,对于难溶性药物,SBE7-β-CD比未修饰的β-环糊精是更有效的增溶剂,但SBE7-β-CD不如DMCD有效。还研究了SBE7-β-CD对前列腺素I2酸水解速率、吲哚美辛碱水解速率、前列腺素E1脱水以及前列腺素A1异构化的影响,并与未修饰的β-环糊精、DMCD和2,3,6-部分甲基化-β-环糊精(PMCD)的影响进行了比较。SBE7-β-CD对化学不稳定药物的稳定作用通常高于其他环糊精。

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