Comparative evaluation of the severity of gastric ulceration by solid dispersions and coprecipitates of indomethacin.
The ulcerogenic activity of indomethacin was studied in rats following single and chronic doses of indomethacin in the form of pure drug, solid dispersions and coprecipitates. Each formulation was administrated as a suspension in a 2% methylcellulose solution. Gastrointestinal ulceration was assessed, four hours after a single dose and 24 hours following the last dose of a chronic four day dosing regimen, by counting the number of lesions and ulcers present. A rating scale was employed to evaluate the severity index. The coprecipitate formulation produced less severe ulceration than the solid dispersion and pure drug. This suggests that the severity of ulceration than the solid dispersion and pure drug. This suggests that the severity of ulceration may be related to the preparation methodology and drug release kinetics.
Karnachi
A A
AA
Division of Pharmaceutics, School of Pharmacy, Northeast Louisiana University, Monroe.
Reddy
I K
IK
Degennaro
M D
MD
Khan
M A
MA
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000633:toxicity*; D011232:Chemical Precipitation; D007213:Indomethacin / Q000008:administration & dosage / Q000633:toxicity*; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D013276:Stomach Ulcer / Q000139:chemically induced*
D000894:Anti-Inflammatory Agents, Non-Steroidal; D007213:Indomethacin