CONTROLLED RELEASE OF 5-FLUOROURACIL FROM LINEAR POLY(ORTHO ESTERS)

被引：24

作者：

MAA, YF ^{[1
]}

HELLER, J ^{[1
]}

机构：

[1] SRI INT,CONTROLLED RELEASE & BIOMED POLYMERS PROGRAM,MENLO PK,CA 94025

来源：

JOURNAL OF CONTROLLED RELEASE | 1990年 / 13卷 / 01期

关键词：

5-fluorouracil; controlled drug release; implants; poly(ortho esters); surface erosion;

D O I：

10.1016/0168-3659(90)90070-A

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Linear poly(ortho esters) prepared by the reaction between 3,9-bis(ethylidene-2,4,8,10-tetraoxaspiro [5,5] undecane) and various ratios of trans-cyclohexanedimethanol (t-CDM) and 1,6-hexanediol (1,6-HD), were investigated as bioerodible matrices for the controlled release of 5-fluorouracil (5-FU). Polymer erosion and release of 5-FU was found to depend on the nature and concentration of the incorporated acidic excipient used to catalyze polymer erosion. Three acidic excipients were investigated: itaconic acid, adipic acid and suberic acid. Relatively high concentration of the more water soluble diacids increased polymer hydrophilicity and promoted diffusional release of 5-FU. Suberic acid was found to possess the best combination of water solubility and acid strength. The composition of the polymer was also found to have a significant effect on rate of erosion and release of 5-FU. Polymers with a high t-CDM /1,6-HD ratio produced devices with a microporous structure and consequent fast diffusional release of 5-FU. Polymers prepared with only 1,6-HD were capable of eroding at high rates and were found to release 5-FU by a predominant surface erosion process. Polymer mechanical properties could be improved by solution blending two polymers with different t-CDM/1,6-HD ratios. © 1990.

引用

页码：11 / 19

页数：9

共 20 条

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