Anti-inflammatory and ulcerogenic effects of 3-(N,N-diethylamino) propylindometacin HCl
Abstract
AIM: To study anti-inflammatory effects of a novel indometacin ester,
3-(N,N-diethylamino) propyl-indometacin HCl (prodrug) and its ulcerogenicity in
fats.
METHODS: Carrageenin (Car)-induced paw edema and ulcer index were examined.
RESULTS: 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.
CONCLUSION: The prodrug is a potent anti-inflammatory agent with lower
ulcerogenicity in the stomach.
Keywords:
3-(N,N-diethylamino) propyl-indometacin HCl (prodrug) and its ulcerogenicity in
fats.
METHODS: Carrageenin (Car)-induced paw edema and ulcer index were examined.
RESULTS: 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.
CONCLUSION: The prodrug is a potent anti-inflammatory agent with lower
ulcerogenicity in the stomach.