[Anti-inflammatory effects of methylprednisolone aceponate in animals].
In the case of dermal application of the drugs to croton oil-induced ear edema in rats and picryl chloride-induced delayed type hypersensitivity in mice, the anti-inflammatory effect of methylprednisolone aceponate (MPA) was slightly weaker than those of clobetasol 17-propionate and diflucortolone 21-valerate, but stronger than those of hydrocortisone 17-butyrate and hydrocortisone 17-butyrate 21-propionate. Betamethasone 17-valerate applied dermally was less and more effective than MPA to ear edema in rats and delayed type hypersensitivity in mice, respectively. The anti-inflammatory effect of MPA was weaker in subcutaneous administration than in topical application to the two inflammatory models. It was suggested that MPA has strong anti-inflammatory effects and weak systemic effects by topical application. Methylprednisolone 17-propionate (MP-17P) and methylprednisolone (MP), unesterified in only the C-21 position and in both the C-17 and 21 positions of MPA, respectively, showed weaker anti-inflammatory activities than MPA by topical application to croton oil-induced ear edema. The ratio of the anti-inflammatory effects by topical application to subcutaneous administration of MPA was higher than those of MP-17P and MP. The excellent characteristics of MPA as a dermal anti-inflammatory drug are suggested to be derived from di-esterification of MP, which has a weak activity intrinsically.
Ikoma
Y
Y
Research Department, Nihon Schering K.K., Osaka, Japan.
Yamashita
M
M
Kamitani
K
K
Nakagawa
H
H
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology* / Q000627:therapeutic use; D003436:Croton Oil; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D005260:Female; D006099:Granuloma / Q000188:drug therapy; D006968:Hypersensitivity, Delayed / Q000188:drug therapy; D007279:Injections, Subcutaneous; D008297:Male; D008775:Methylprednisolone / Q000494:pharmacology* / Q000627:therapeutic use; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains; D012871:Skin Diseases / Q000188:drug therapy
D000893:Anti-Inflammatory Agents; D003436:Croton Oil; D008775:Methylprednisolone