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[用于药物控释的珠状纤维素。4. 珠状纤维素及其衍生物与盐酸哌唑嗪的结合及其释放]

[The use of bead cellulose for controlled drug liberation. 4. Binding of bead cellulose and bead cellulose-derivatives with prazosin hydrochloride and its liberation].

作者信息

Wolf B, Finke I

机构信息

Sektion Biowissenschaften, Lehrstuhl Pharmazeutische Technologie, Universität Leipzig.

出版信息

Pharmazie. 1992 Jan;47(1):35-8.

PMID:1608982
Abstract

Pure bead cellulose and the ionic derivatives carboxymethyl and dihydrogen phosphate bead cellulose were coupled with prazosin hydrochloride. The degree of substitution achieved during loading mostly depends on the number of functional groups, what was verified by titrimetric determination of the ion exchange capacity. Because of predominant ionic binding of the protonated prazosin cation to the anionic groups of several types of bead cellulose in electrolytes containing liquids as well as in water a large amount of bonded drug is liberated considerable fast. Retardation of the liberation in comparison to the commercial product Adversuten is verified but not applicable to therapeutic use in the case of prazosin.

摘要

纯珠状纤维素及其离子衍生物羧甲基和磷酸二氢珠状纤维素与盐酸哌唑嗪偶联。负载过程中实现的取代度主要取决于官能团的数量,这通过离子交换容量的滴定测定得到了验证。由于质子化哌唑嗪阳离子在含电解质液体以及水中与几种类型珠状纤维素的阴离子基团主要通过离子键结合,大量结合的药物会相当快速地释放出来。与市售产品Adversuten相比,药物释放有所延缓,但对于哌唑嗪而言,这种延缓并不适用于治疗用途。

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