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一种制备6-聚乳酸环麦芽七糖的简便方法,该物质作为阿莫西林控释的动力学可降解衍生物。

A convenient preparation of 6-oligo(lactic acid)cyclomaltoheptaose as kinetically degradable derivative for controlled release of amoxicillin.

作者信息

Shen Jian, Hao Aiyou, Du Guangyan, Zhang Huacheng, Sun Hongyuan

机构信息

School of Chemistry and Chemical Engineering, Shandong University, Jinan 250100, People's Republic of China.

出版信息

Carbohydr Res. 2008 Oct 13;343(15):2517-22. doi: 10.1016/j.carres.2008.06.010. Epub 2008 Jun 17.

Abstract

6-Oligo(lactic acid)cyclomaltoheptaose (6-OLA-betaCD) with an average substitution of about 7.0 lactic acid units was prepared as a new water-soluble cyclomaltoheptaose (betaCD) derivative (solubility of about 70.7-fold that of betaCD), based on the ring-opening polymerization of 3,6-dimethyl-1,4-dioxane-2,5-dione (lactide). The product was characterized by (1)H NMR, (13)C NMR, IR, and MS spectroscopy. The complexation of amoxicillin with 6-OLA-betaCD was found to be much stronger than that with betaCD at first, and then 6-OLA-betaCD was shown to decompose moderately into betaCD and lactic acid. 6-OLA-betaCD might be greatly valuable in a controlled release system for Amoxicillin (AMX).

摘要

基于丙交酯(3,6 - 二甲基 - 1,4 - 二氧六环 - 2,5 - 二酮)的开环聚合反应,制备了平均取代度约为7.0个乳酸单元的6 - 聚乳酸环麦芽七糖(6 - OLA - β - CD),作为一种新型水溶性环麦芽七糖(β - CD)衍生物(溶解度约为β - CD的70.7倍)。该产物通过¹H NMR、¹³C NMR、红外光谱和质谱进行表征。起初发现阿莫西林与6 - OLA - β - CD的络合作用比与β - CD的络合作用强得多,随后表明6 - OLA - β - CD会适度分解为β - CD和乳酸。6 - OLA - β - CD在阿莫西林(AMX)控释系统中可能具有重大价值。

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