IMPROVED ORAL BIOAVAILABILITY OF SALICYLAMIDE IN RABBITS BY A 1,3-BENZOXAZINE-2,4-DIONE PRODRUG

被引：10

作者：

KAHNS, AH ^{[1
]}

MOSS, J ^{[1
]}

BUNDGAARD, H ^{[1
]}

机构：

[1] ROYAL DANISH SCH PHARM,DEPT PHARMACEUT CHEM,2 UNIV PARKEN,DK-2100 COPENHAGEN,DENMARK

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 1992年 / 78卷 / 2-3期

关键词：

SALICYLAMIDE; 1,3-BENZOXAZINE-2,4-DIONE; 1ST-PASS METABOLISM; ABSORPTION; PRODRUG;

D O I：

10.1016/0378-5173(92)90371-8

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The oral bioavailability of 1,3-benzoxazine-2,4-dione was investigated in rabbits and compared with that of salicylamide. The benzoxazinedione was shown to be hydrolyzed to salicylamide both in vitro and in vivo. The oral bioavailability of salicylamide was increased 2.5-fold following administration as 1,3-benzoxazinedione comapared to oral dosing of an equimolar amount of salicylamide per se. This increased bioavailability of salicylamide was ascribed to a diminished first-pass metabolism achieved by protecting the vulnerable phenolic group in the form of a benzoxazinedione ring structure.

引用

页码：199 / 202

页数：4

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