STABILIZATION OF DAUNORUBICIN AND 4-DEMETHOXYDAUNORUBICIN ON COMPLEXATION WITH OCTAKIS(2,6-DI-O-METHYL)-GAMMA-CYCLODEXTRIN IN ACIDIC AQUEOUS-SOLUTION

被引：5

作者：

SUENAGA, A

BEKERS, O

BEIJNEN, JH

UNDERBERG, WJM

TANIMOTO, T

KOIZUMI, K

OTAGIRI, M

机构：

[1] KUMAMOTO UNIV,FAC PHARMACEUT SCI,DEPT PHARMACEUT,5-1 OE HONMACHI,KUMAMOTO 862,JAPAN

[2] UNIV UTRECHT,FAC PHARM,DEPT PHARMACEUT ANAL,3511 GH UTRECHT,NETHERLANDS

[3] NETHERLANDS CANC INST,SLOTERVAART HOSP,1066 EC AMSTERDAM,NETHERLANDS

[4] MUKOGAWA WOMENS UNIV,FAC PHARMACEUT SCI,NISHINOMIYA,HYOGO 663,JAPAN

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 1992年 / 82卷 / 1-2期

关键词：

DAUNORUBICIN; 4-DEMETHOXYDAUNORUBICIN; DEGRADATION; INCLUSION COMPLEX; OCTAKIS(2,6-DI-O-METHYL)-GAMMA-CYCLODEXTRIN; STABILIZATION;

D O I：

10.1016/0378-5173(92)90068-D

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The effects of octakis(2,6-di-O-methyl)-gamma-cyclodextrin (DM-gamma-CyD) on the chemical stability of the anthracycline antibiotics daunorubicin (Dr) and 4-demethoxydaunorubicin (4-demethoxyDr) in acidic aqueous media have been investigated. As determined from the analysis of inclusion complexation of anthracyclines with CyDs, DM-gamma-CyD displayed the highest stabilizing ability, followed in descending order by 3-hydroxypropyl-gamma-CyD > gamma-CyD > hydroxyethyl-gamma-CyD, whilst octakis(2,3,6-tri-O-methyl)-gamma-CyD showed no effect. Nevertheless, 4-demethoxyDr formed a much more stable inclusion complex with DM-gamma-CyD; surprisingly, the effect of stabilization by DM-gamma-CyD is significantly smaller compared with Dr. H-1-NMR data indicate that the aglycone region of the anthracycline molecule is included within the DM-gamma-CyD cavity.

引用

页码：29 / 37

页数：9

共 20 条

[1] ANTITUMOR ANTHRACYCLINES - RECENT DEVELOPMENTS [J].