Transdermal formulations of deprenyl:
guinea pig and pig models

Gaal J, Szebeni G, Szekacs G, Fejer E,
Wagner O, Szatmari I, Magyar K, Mezei M
MEGAPharma Ltd.,
Budapest, Hungary.
Neurobiology (Bp) 2000; 8(2):143-66


The efficacy of many drugs relies on their presence at the site of action over a period of time. The retardation or programmed release capability of the conventional dosage forms like oral and parenteral are limited and toxic and undesired side-effects may occur after their applications. These problems may be solved using transdermal delivery systems. Transdermal systems are aimed for local, or systemic action. In the letter case controlling the rate of delivery or modulating the distribution in the organism. The selection of an adequate biological method of evaluating a new transdermal formulation is a critical point of the development. The in vitro methods can help in the characterization of the different formulas, but without an in vivo disposition study they cannot give relevant information about the expectable therapeutic behavior. We adapted and improved an in vivo test system for the evaluation of new transdermal particulate systems (patches) and liposomes containing deprenyl selegiline as active ingredient. The in vivo evaluation system consists of two steps: 1. Full biodisposition study on guinea pig, using isotope labeled selegiline. 2. Biodisposition studies on domestic pigs including dose, area, surface dependence and comparative bioavailability with traditional dosage forms and application moods. Specific examples of these studies and experimental technology are presented.
Transdermal selegiline
Selegiline and nitric oxide
Selegiline and life-expectancy
Selegiline for longer-lived flies
Selegiline for cocaine dependence
Selegiline patch (Emsam) as an antidepressant
Transdermal selegiline without dietary restrictions
Feb 2006: EMSAM (selegiline transdermal system) licensed by FDA

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