THE EFFECT OF CYCLODEXTRINS ON THE SOLUBILITY AND STABILITY OF MEDROXYPROGESTERONE ACETATE AND MEGESTROL-ACETATE IN AQUEOUS-SOLUTION

被引:24
作者
LOFTSSON, T
BALDVINSDOTTIR, J
SIGURDARDOTTIR, AM
机构
[1] Department of Pharmacy, University of Iceland
关键词
AQUEOUS SOLUTION; CYCLODEXTRIN; MEDROXYPROGESTERONE ACETATE; MEGESTROL ACETATE; SOLUBILITY; STABILITY;
D O I
10.1016/0378-5173(93)90060-S
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The degradation of medroxyprogesterone acetate and megestrol acetate in aqueous buffered solutions was investigated over the pH range 1-10. The degradation followed first-order kinetics. The pH-rate profiles were of typical V-shape with a minimum at Ph between 4 and 5. In aqueous solutions the shelf-life of the drugs at physiological pH and 25-degrees-C was estimated to be about 1 year. The effects of six cyclodextrin (CD) derivatives on the stability was investigated and 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD) of molar substitution (MS) 0.9 and methyl-beta-cyclodextrin (MbetaCD) of degree of substitution (DS) 1.8 appeared to have the greatest stabilising effect. The drugs degraded 2.5-4-times slower within the HPbetaCD and MbetaCD cavities than outside the cavities. Of the two CD derivatives, MbetaCD DS 1.8 resulted in better solubilisation of the drugs.
引用
收藏
页码:225 / 230
页数:6
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