[Correlation of the lipophilicity of the active agents with their topical anti-inflammatory activity].
The present study concerns the relation between the therapeutic activity of some FANS in formulation for topical use and their lipophylic nature. The efficacy of topic formulations of three widely used FANS: cinnoxicam, piroxicam and diclofenac have been evaluated through the decrease of plantar edema induced by egg's white in the rat's hind paw. The volume increases after one hour were 55% in the group of rats treated with cinnoxicam, 64% in the animals treated with piroxicam and 79% in those treated with diclofenac, against 86% of control group. The partition coefficient (P) of the three active drugs have been detected. The P found for the three drugs 4.9, 3.3, 0.9 respectively demonstrate the direct correlation between the pharmacological activity of the topic formulation and its lipophylic nature.
Berti
M
M
Centro Ricerche, PROTER S.p.A.-Opera.
Cantoni
R
R
Mosconi
P
P
Pattini
P
P
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry / Q000494:pharmacology*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005260:Female; D008055:Lipids / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar
D000893:Anti-Inflammatory Agents; D008055:Lipids
Correlazione tra lipofilia del principio attivo ed attività antiinfiammatoria per via topica.