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1,2‐dihydro‐3,1‐benzoxazin‐4‐one and 4 H ‐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
Author(s) -
Schwenker Gerhard,
Chen Jianbing
Publication year - 1991
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.2503241113
Subject(s) - mefenamic acid , prodrug , chemistry , permeation , drug , stereochemistry , in vitro , chromatography , pharmacology , biochemistry , medicine , membrane
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 R M values and the melting points were interpreted.