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

Abstract

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.

Physicochemical and crystallographic characterization of mefenamic acid complexes with alkanolamines

“…Unfortunately, MH has a number of unsuitable physicochemical properties, such as its poor solubility in water. To overcome problems arising from skin impermeability, various strategies including the use of a penetration enhancer3 and a prodrug approach4 have been used to increase the transdermal transport of MH. However, none of these methods has been able to achieve sufficient skin permeation to produce its desired therapeutic effect.…”