Activity of topically applied methylprednisolone aceponate in relation to other topical glucocorticosteroids in healthy volunteers.
Topical glucocorticosteroids are useful in the treatment of various skin diseases. Although there are already many corticosteroids available, there is still need for highly potent and well tolerated ones. The anti-inflammatory activity of methylprednisolone aceponate (MPA, CAS 86401-95-8) has been investigated in 165 healthy volunteers of either sex. UV-B irradiation or cellophane tape stripping has served to produce erythema. First, the dose response relationship of MPA ointment (0.01%, 0.05%, 0.1% and 0.5%) has been evaluated. MPA effects have been related to those of the vehicle and difluocortolone 21-valerate 0.1% (DFV) ointment. Then the activity of 0.1% MPA (cream, ointment and fatty ointment) has been related to those of the respective vehicles as well as commercially available preparations of five corticosteroids: betamethasone 17,21-dipropionate 0.64% (BDP), betamethasone 17-valerate 0.1% (BV), clobetasol 17-propionate 0.05% (CP), hydrocortisone 17-butyrate 0.1% (HCB), prednicarbate 0.25% (P). In each experiment, MPA activity significantly exceeded that of the respective vehicle (p < or = 0.05). MPA 0.01-0.5% ointment exhibited strong anti-inflammatory activity, at least corresponding to that of 0.1% DFV ointment. A dose-dependent activity could only be observed in the UV-B-erythema test using 3 fold MED (minimal erythema doses) for irradiation, a test model differentiating strong corticosteroids. The comparison of 0.1% MPA formulations with respective reference preparations showed the following results: On stripped skin no significant differences could be detected which is demonstrated in the example of cream formulations.(ABSTRACT TRUNCATED AT 250 WORDS)
Kecskés
A
A
Department of Human Pharmacology, Schering Aktiengesellschaft, Berlin.
Jahn
P
P
Wendt
H
H
Kleine-Kuhlmann
R
R
Lange
L
L
D000287:Administration, Topical; D000328:Adult; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D004890:Erythema / Q000188:drug therapy; D005260:Female; D005938:Glucocorticoids; D006801:Humans; D008297:Male; D008775:Methylprednisolone / Q000031:analogs & derivatives* / Q000494:pharmacology; D008875:Middle Aged; D012867:Skin / Q000187:drug effects*; D014466:Ultraviolet Rays; D014662:Vasoconstrictor Agents / Q000494:pharmacology
D000893:Anti-Inflammatory Agents; D005938:Glucocorticoids; D014662:Vasoconstrictor Agents; C078007:methylprednisolone aceponate; D008775:Methylprednisolone