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用于药物包合与分离的聚乙烯醇/环糊精微球的制备与表征

Preparation and characterisation of poly(vinyl alcohol)/cyclodextrin microspheres as matrix for inclusion and separation of drugs.

作者信息

Constantin Marieta, Fundueanu Gheorghe, Bortolotti Fabrizio, Cortesi Rita, Ascenzi Paolo, Menegatti Enea

机构信息

Department of Pharmaceutical Sciences, University of Ferrara, Via Fossato di Mortara, 19 44100 Ferrara, Italy.

出版信息

Int J Pharm. 2004 Nov 5;285(1-2):87-96. doi: 10.1016/j.ijpharm.2004.07.025.

Abstract

Poly(vinyl alcohol) (PVA) microspheres containing cyclodextrin (CD) were obtained by chemical cross-linking with glutaraldehyde of an acidified mixture solution of PVA and alpha-, beta- or gamma-CD. The amount of linked CD in microspheres, estimated by tetrazolium blue method, decreases in the order beta- > gamma- > alpha-CD. The dimensions of PVA/gamma-CD microspheres are much higher than those of PVA/alpha- and beta-CD. The cross-linking density of microspheres was estimated by the amount of iodine retained by the polymer matrix. The pore size as well as the porous volume of PVA/CD microspheres decrease significantly on increasing the amount of glutaraldehyde, but are enough large to permit the access of drugs to the CD cavity. In order to test the PVA/CD microsphere inclusion ability, the microspheres were packed in a glass column and the liquid chromatographic behaviour by isocratic elution of different drugs or typical organic compounds, taken as model drugs, was investigated.

摘要

通过用戊二醛对聚乙烯醇(PVA)与α-、β-或γ-环糊精(CD)的酸化混合溶液进行化学交联,得到了含有环糊精的聚乙烯醇(PVA)微球。用四氮唑蓝法估算,微球中连接的CD量按β->γ->α-CD的顺序减少。PVA/γ-CD微球的尺寸远大于PVA/α-和β-CD微球。通过聚合物基质保留的碘量估算微球的交联密度。随着戊二醛用量的增加,PVA/CD微球的孔径和孔体积显著减小,但仍足够大,能使药物进入CD腔。为了测试PVA/CD微球的包合能力,将微球填充在玻璃柱中,并研究了以不同药物或典型有机化合物作为模型药物进行等度洗脱时的液相色谱行为。

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