THE PROPERTIES AND POTENTIAL USES OF CYCLODEXTRIN DERIVATIVES

被引:103
作者
SZEJTLI, J
机构
[1] CYCLOLAB, Cyclodextrin Research and Development Laboratory, Budapest
来源
JOURNAL OF INCLUSION PHENOMENA AND MOLECULAR RECOGNITION IN CHEMISTRY | 1992年 / 14卷 / 01期
关键词
CYCLODEXTRIN DERIVATIVES; SOLUBILITY; DRUG CARRIER CHARACTERISTICS; COMPLEX FORMATION;
D O I
10.1007/BF01041363
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The hydroxyl groups can be selectively substituted to control the solubility and the complex forming selectivity of the modified cyclodextrins (CDs). Among the methylated CDs only two well-defined compounds can be taken into consideration: dimethyl- and trimethyl-betaCD (DIMEB and TRIMEB). In an aqueous solution of DIMEB the solubility of rather insoluble compounds and drugs like steroids, vitamin D3, lidocaine and hydrocortisone increases. In some cases their stability and bioavailability are also improved. On the other hand, the hydrolysis rate of carmofur, coumarins etc. is retarded by the methylated cyclodextrins with blocked hydroxyl groups. The drug solubilizing capacity of hydroxypropyl-betaCD (HPBCD) is in most cases lower than that of DIMEB. The degree of substitution (DS) shows no remarkable effect on the solubilizing properties of HPBCD in the case of indomethacin, Dipiridamole etc., but in the case of Tolnaftate the solubility was enhanced by increasing the DS, other examples are shown.
引用
收藏
页码:25 / 36
页数:12
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