RACEMIZATION OF CHLORTHALIDONE IN THE PRESENCE OF LIPOSOMES

被引：7

作者：

LAMPARTER, E ^{[1
]}

BLASCHKE, G ^{[1
]}

SCHLUTER, J ^{[1
]}

机构：

[1] UNIV MUNSTER,DEPT PHARMACEUT CHEM,W-4400 MUNSTER,GERMANY

来源：

CHIRALITY | 1993年 / 5卷 / 05期

关键词：

(+)-CHLORTHALIDONE; RACEMIZATION; PH PROFILE; INFLUENCE OF LIPOSOMES; REACTION KINETICS;

D O I：

10.1002/chir.530050518

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The extent of racemization of (+)-chlorthalidone as a function of pH is examined. The minimum of the log K/pH curve is pH 3. The reaction mechanism of inversion is postulated to involve a carbenium cation over the entire pH range and a ring opening reaction in the alkaline range. The influence of liposomes on the inversion rate is also studied, retardation of the racemization rate being observed with increasing liposome concentration. A model of drug distribution between liposome phase and aqueous phase based on the Nernst distribution principle is presented and reaction kinetic aspects are considered. (C) 1993 Wiley-Liss, Inc.

引用

页码：370 / 374

页数：5

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