1,2-Dihydro-3,1-benzoxazin-4-one and 4H-1,2-dihydro-pyrido-[2,3-d]- [1,3]-oxazin-4-one derivatives as potential prodrugs. Part III: Permeability through excised human skin in vitro.
The percutaneous permeation characteristics of 6 potential prodrugs 2-7 in comparison with their parent drug mefenamic acid (1) in vitro using excised human skin were studied. The results show that all potential prodrugs tested were at least 2.0 times as effective as mefenamic acid; compounds 2 and 7 permeated almost 5 times as quickly as mefenamic acid through excised human skin. The relations between the permeation behaviour, the RM values and the melting points were interpreted.
Schwenker
G
G
Pharmazeutisch-chemisches Institut, Universität Heidelberg.
Chen
J B
JB
D006801:Humans; D066298:In Vitro Techniques; D010078:Oxazines / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D011355:Prodrugs / Q000493:pharmacokinetics*; D011725:Pyridines / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D012869:Skin Absorption; D013056:Spectrophotometry, Ultraviolet
D010078:Oxazines; D011355:Prodrugs; D011725:Pyridines