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
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
收藏
页码:29 / 37
页数:9
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