Effect of hydroxypropyl-β-cyclodextrin on the central stimulant activity of (-)-ephedrine and an oxazolidine prodrug in rats

被引：16

作者：

Walker, RB

Dholakia, VN

Brasfield, KL

Bakhtiar, R

机构：

[1] Univ Arkansas, Dept Chem & Phys, Pine Bluff, AR 71611 USA

[2] Stevens Inst Technol, Dept Chem & Chem Engn, Hoboken, NJ 07030 USA

来源：

GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM | 1998年 / 30卷 / 05期

关键词：

ephedrine; oxazolidine; prodrug; cyclodextrin; locomotor activity;

D O I：

10.1016/S0306-3623(97)00341-8

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

1. Hydroxypropyl beta-cyclodextrin (HP-beta-CD) increases the stability of the oxazolidine prodrug toward hydrolysis. 2. The binding constant (K(b)) and rate constant (K(c)) for the hydrolysis of the prodrug-HP-beta-CD complex were calculated from the kinetic data. 3. Ion spray mass spectra confirmed prodrug-HP-beta-CD complexation. 4. Mass spectral and kinetic data indicated 1:1 stoichiometry for the complex. 5. A significant elevation of locomotor activity in rats was observed when either (-)-ephedrine or the prodrug was administered by either the intraperitoneal or the oral route. 6. Addition of HP-beta-CD potentiated the central nervous system effect of both (-)-ephedrine and the prodrug when administered intraperitoneally. However, when the drugs were administered orally, HP-beta-CD caused a decrease in activity. (C) 1998 Elsevier Science Inc.

引用

页码：725 / 731

页数：7

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