INVITRO NITROSATION OF METHAPYRILENE

被引：13

作者：

MERGENS, WJ ^{[1
]}

VANE, FM ^{[1
]}

TANNENBAUM, SR ^{[1
]}

GREEN, L ^{[1
]}

SKIPPER, PL ^{[1
]}

机构：

[1] MIT,CAMBRIDGE,MA 02139

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 1979年 / 68卷 / 07期

关键词：

Ascorbic acid—methapyrilene nitrosation; prevention of nitrosodimethylamine formation; in vitro; Carcinogens—nitrosodimethylamine; formation from methapyrilene; prevention by ascorbic acid; Methapyrilene—nitrosation; with sodium nitrite; nitrosodimethylamine formation; effect of pH; prevented by ascorbic acid; Nitrosodimethylamine—formation from methapyrilene;

D O I：

10.1002/jps.2600680710

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The reactions of sodium nitrite and methapyrilene were studied in aqueous solution at neutral pH and under simulated gastric fluid conditions. Reaction product formation was much more complex than nitrosation of the parent molecule dimethylamino moiety to form nitrosodimethylamine. Several new nitroso compounds were formed under the reaction conditions studied. The simultaneous incorporation of 2 moles of ascorbic acid/mole of nitrite ion prevented any destruction of methapyrilene under all conditions studied. The implications of these observations with respect to nitrosation theory, the general carcinogenicity of nitroso compounds, and methapyrilene dosage formulation are discussed. Copyright © 1979 Wiley‐Liss, Inc., A Wiley Company

引用

页码：827 / 832

页数：6