Percutaneous absorption of methylprednisolone aceponate after single and multiple dermal application as ointment in male volunteers.
Six healthy, elderly volunteers were treated once daily with Advantan ointment containing 0.1% of methylprednisolone aceponate (MPA, CAS 86401-95-8) in an area dose of 5 mg ointment/cm2 on a marked area of 80 cm2 of intact skin on the back for 14 days. The ointments used for treatment on days 1 and 8 contained 14C-MPA with a specific radioactivity of 2.5 MBq/mg MPA. Following the radioactive pulse doses, the concentrations of 3H-radioactivity in plasma and urine were monitored up to 48 h and 7 days, respectively. The concentration of 14C-radioactivity in the plasma did not exceed the limit of detection of 0.3 ng MPA-equiv./ml. Percutaneous absorption of MPA through intact skin was small (les than 1%) and did not change during repeated application, indicating that the penetration barrier is not influenced by the drug or the vehicle.
Täuber
U
U
Institute of Pharmacokinetics, Schering Aktiengesellschaft, Berlin, Fed. Rep. of Germany.
Matthes
H
H
D000368:Aged; D006801:Humans; D008297:Male; D008775:Methylprednisolone / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D008875:Middle Aged; D009824:Ointments; D014677:Pharmaceutical Vehicles; D012869:Skin Absorption
D009824:Ointments; D014677:Pharmaceutical Vehicles; C078007:methylprednisolone aceponate; D008775:Methylprednisolone