Improvement of clofibrate dissolution by complexation with cyclodextrin

被引:13
作者
AnguianoIgea, S
OteroEspinar, FJ
VilaJato, JL
BlancoMendez, J
机构
[1] Departamento de Farmacología, Facultad de Farmacia, Univ. de Santiago de Compostela, Santiago de Compostela
[2] Univ. de Santiago de Compostela, Campus Universitario
关键词
clofibrate; cyclodextrin; inclusion complexation; solubility; solid form; coprecipitation; kneading; sealed heating;
D O I
10.1016/0378-5173(96)04477-8
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Inclusion complexes of clofibrate with beta-cyclodextrin (beta CD) were prepared by coprecipitation, kneading and sealed heating methods and characterized by UV spectrophotometry, differential scanning calorimetry, X-ray diffractometry and infrared spectroscopy. All results were in keeping with the formation of 1:1 inclusion complex. Dissolution studies showed that clofibrate entrapped in inclusion complexes dissolved much faster than uncomplexed liquid clofibrate. The complex prepared by the sealed heating method showed the greatest improvement in dissolution rate: this complex released 50 mg of clofibrate into water within 10 min. These results show that a more easily manipulated, solid form of clofibrate may be obtained through formation of its inclusion complex with beta CD, and that complex formation simultaneously enhances the solubility and dissolution rate of this drug.
引用
收藏
页码:161 / 166
页数:6
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