Larionov V. Transdermal delivery enhancement for 1.4-benzdiazepine derivatives

Transdermal delivery enhancement for 1,4-benzdiazepine derivatives. Development of methods of intensifying of infiltration of 1,4-benzdiazepine derivatives through dermal layers. Methods of research - spectroscopical, radioisotope, pharmacological, statistical. The prevailing mechanism of increase of permeability of skin under action of aliphatic acids, alcohols, alkylpyridine salts. The enhancement effect of all chemicals found to be complex, involving influence on both lipid and protein structures of stratum corneum and partial lipid and cholesterol extraction. There was shown the dependence between lipophilicity of 1.4-benzdiazepine derivative and enhancement effect of various chemical permeability enhancers. Lauric acid, when used as permeability enhancer for phenazepam, increases its bioavailability ( at ~ 3 times). The highest ability penetrate skin was noted at lauric ester. The substance synthesized has prolonged pharmacological effect and circulates the organism for a long time (has little value). Sphere of use - bioorganic chemistry, pharmacology, medicine.