Studies Of Selegiline Transdermal Therapeutic System

Selegiline is a preferential MAO-B inhibitor wich is currently used as an adjunct therapy to treat late stage Parkinson's disease. However, at present, marketed transdermal therapeutic patches were not found.Selegiline has a strong pharmaco dynamic effect. It has a compatible molecular weight (223.75) and a higher octanol/water partition coefficient. So it is adapted to be made as Transdermal drug delivery systems (TDDS).In this thesis, some physicochemical properties and the transdermal delivery across Guinea pig skin in vitro of selegiline with 3 kinds of penetration enhancers used alone were studied. For the successful development, a series of systematic studies were conducted. The prescription of selegiline TDDS were designed. Pharmaceutical analysis methodology, quality standard and the properties of preparations were studied.In order to obtain the optimal drug delivery, the main ingredients, pressure sensitive adhesives (PSA) and permeation enhancers were chosen through orthogonal tests. The results show that crylic acid PSA and single permeation enhancers of A can make a remarked synergistic enhancement of selegiline permeating through Guinea pig skin. Finally, based on the extensive development studies, a prototype of selegiline TDDS is prepared with x₁% selegiline, y₁% A,15%D, 60% crylic acid PSA, and aluminium mylar films.The method of UV was used as distinguished. The method of HPLC has been developed to determine the content and relative substances of selegiline TDDS.Quality measures included sample size and shape, homogeneity, detection of relative substances, release rates, penatration rates and adhesiveness.The experimentation results indicate that selegiline -TDDS is capable of 1 days continuous delivery of selegiline with a stable permeation rate and has not any skin irritation. So it is a safe and effective transdermal therapeutic system.