合成和表征环丙沙星的聚酯缀合物。

Synthesis and characterization of polyester conjugates of ciprofloxacin.

机构信息

Medical University of Warsaw, Faculty of Pharmacy, Department of Inorganic and Analytical Chemistry, ul. Banacha 1, 02-097 Warsaw, Poland.

出版信息

Eur J Med Chem. 2010 Sep;45(9):3844-9. doi: 10.1016/j.ejmech.2010.05.037. Epub 2010 May 24.

DOI:10.1016/j.ejmech.2010.05.037

PMID:20541292

Abstract

Two-, three-, four and six-arm, star-shaped poly(epsilon-caprolactone) and polylactide homopolymers were synthesized via ring-opening polymerization of cyclic esters in the presence of glycerol, penthaerythritol, dipentaerythritol and poly(ethylene glycol) as initiators and stannous octoate as a catalyst. Thus obtained oligomers were successfully used in the synthesis of novel polyester conjugates of ciprofloxacin. The structures of the polymers and conjugates were determined by means of GPC, MALDI-TOF MS, NMR and IR studies. The in vitro release of ciprofloxacin from obtained conjugates was investigated.

摘要

通过环状酯在甘油、季戊四醇、二季戊四醇和聚乙二醇作为引发剂以及辛酸亚锡作为催化剂的存在下的开环聚合，合成了二、三、四和六臂星形聚（己内酯）和聚乳酸均聚物。由此得到的低聚物成功地用于合成环丙沙星的新型聚酯缀合物。聚合物和缀合物的结构通过 GPC、MALDI-TOF MS、NMR 和 IR 研究来确定。研究了从所得缀合物中释放的环丙沙星的体外释放。