Huang Z L, Kagoshima M, Kagawa E, Wang W Q, Shimada H
Department of Clinical Pharmacology, School of Pharmaceutical Sciences, Kitasato University, Tokyo, Japan.
Zhongguo Yao Li Xue Bao. 1997 Jul;18(4):306-8.
To study anti-inflammatory effects of a novel indometacin ester, 3-(N,N-diethylamino) propyl-indometacin HCl (prodrug) and its ulcerogenicity in fats.
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 i.p. injection of the prodrug 7.09 mg.kg-1. On the same molar basis, indometacin (Ind) 5 mg.kg-1 i.p. 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 micrograms/paw exhibited 64% inhibition of the swelling, the prodrug > 10 micrograms/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 p.o.
The prodrug is a potent anti-inflammatory agent with lower ulcerogenicity in the stomach.
研究一种新型吲哚美辛酯，即3-(N,N-二乙氨基)丙基-吲哚美辛盐酸盐（前体药物）的抗炎作用及其在体内的致溃疡作用。
检测角叉菜胶（Car）诱导的爪肿胀和溃疡指数。
单次腹腔注射前体药物7.09 mg·kg-1后3小时，Car诱导的爪肿胀受到36.6%的抑制（P<0.01），5小时时受到34.6%的抑制（P<0.01）。在相同摩尔基础上，腹腔注射吲哚美辛（Ind）5 mg·kg-1在3小时时抑制肿胀45.6%，5小时时抑制39.2%，然而，前体药物和Ind的肿胀抑制效果之间无统计学显著差异（P>0.05）。剂量为10微克/爪时肿胀抑制率为64%，前体药物剂量>10微克/爪时未显示出额外的肿胀抑制作用；口服给药6小时后，前体药物的急性胃损伤特性远低于Ind。
该前体药物是一种强效抗炎剂，在胃中的致溃疡性较低。
