Anti-inflammatory and ulcerogenic effects of 3-(N,N-diethylamino)propylindometacin HCl  

作　　者：黄志力[1] 鹿儿岛正丰 香川荣一郎 王尉青 岛田英世 

机构地区：[1]北里大学药学部临床药理学教室

出　　处：《中国药理学报》1997年第4期306-308,共3页Acta Pharmacologica Sinica

摘　　要：目的：考察盐酸３（Ｎ，Ｎ二乙胺）丙基吲哚美辛（ｐｒｏｄｒｕｇ）抗炎及致溃疡作用．方法：观察大鼠角叉菜胶（Ｃａｒ）性炎症反应及口服给药胃溃疡指数的变化．结果：腹腔给药显著抑制Ｃａｒ性趾水肿，３ｈ及５ｈ的抑制率分别为３６５７％和３４５６％，与等摩尔浓度的吲哚美辛（Ｉｎｄ）差异无显著性；足趾１０μｇ／ｐａｗ给药达到６４％的抑制率，再增加剂量不能增加效果；１４１８ｍｇ·ｋｇ－１的ｐｒｏｄｒｕｇ灌胃６小时后溃疡指数显著低于同摩尔数Ｉｎｄ．结论：该药为一抗炎作用强，致溃疡性低的药物．IM: To study anti inflammatory effects of a novel indometacin ester, 3 ( N,N diethylamino) propyl-indo-metacin HCl (prodrug) and its ulcerogenicity in rats. METHODS: Carrageenin (Car) induced paw edema and ulcer index were examined. Car induced paw edema was inhibited by 36 6 % ( P <0 01) at 3 h and 34 6 % ( P <0 01) at 5 h after a single ip injection of the prodrug 7 09 mg·kg -1 . On the same molar basis, indometacin (Ind) 5 mg·kg -1 ip inhibited edema by 45 6 % at 3 h and 39 2 % at 5 h, however, there was no statistical significant difference ( P >0 05) between the edema inhibitory effect of the prodrug and that of Ind. The dose 10 μg/paw exhibited 64 % inhibition of the swelling, the prodrug >10 μg/paw showed no additional inhibition of swelling; the acute gastric lesion properties of the prodrug were much lower than those of Ind 6 h after po . The prodrug is a potent anti inflammatory agent with lower ulcerogenicity in the stomach.

关 键 词：丙基吲哚美辛 吲哚美辛 角叉莱胶 水肿 胃溃疡 

分 类 号：R971.1[医药卫生—药品]