氧氟沙星/β-环糊精络合作用

Ofloxacin/beta-cyclodextrin complexation.

作者信息

Koester L S, Guterres S S, Le Roch M, Eifler-Lima V L, Zuanazzi J A, Bassani V L

机构信息

Curso de Pós-graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brasil.

出版信息

Drug Dev Ind Pharm. 2001 Jul;27(6):533-40. doi: 10.1081/ddc-100105178.

DOI:10.1081/ddc-100105178

PMID:11548860

Abstract

Ofloxacin (OFX) is a fluorquinolone characterized by photochemical instability. With the goal to improve its photostability in aqueous solutions, the complexation of ofloxacin with beta-cyclodextrin was investigated. The complexes showed a water solubility enhancement of approximately 2.6 times; nevertheless, the photodegradation of ofloxacin was not reduced. The complexes obtained were characterized by thermal and 1H nuclear magnetic resonance (NMR) analysis, which revealed an interaction between ofloxacin and beta-cyclodextrin. The last analysis indicated that only partial inclusion of the N-methylpiperazinyl moiety occurred, which can explain the fact that photostabilization was not improved. This partial inclusion phenomenon could be explained also by computer-aided molecular modeling.

摘要

氧氟沙星（OFX）是一种具有光化学不稳定性的氟喹诺酮类药物。为了提高其在水溶液中的光稳定性，研究了氧氟沙星与β-环糊精的络合作用。络合物的水溶性提高了约2.6倍；然而，氧氟沙星的光降解并没有减少。通过热分析和1H核磁共振（NMR）分析对所得络合物进行了表征，结果表明氧氟沙星与β-环糊精之间存在相互作用。最后的分析表明，仅发生了N-甲基哌嗪基部分的部分包合，这可以解释光稳定性未得到改善的事实。这种部分包合现象也可以通过计算机辅助分子建模来解释。