Studies Of Rotigotine Transdermal Therapeutic System

Transdermal rotigotine (Neupro) is a nonergolinic dopamine receptor agonist forthe treatment of Parkinson’s disease. At present, marketed transdermal therapeuticpatches have not been found in domestic market.Rotigotine has a strong pharmacological dynamic effect. It has a reasonablemolecular weight (351.47) and a higher octanol/water partition coefficient（logP=4.03）. So it is suitable to be made as transdermal drug delivery systems.This topic belongs to one of the projects of Beijing KBD PharmaceuticalTechnology Development Co.Ltd., aiming at mading rotigotine transdermal patchesby oureselves on the base of existing patents and documents, and evaluating its seriesof properties. In this thesis, some physicochemical properties and the transdermaldelivery across Guinea pig skin in vitro of Rotigotine were studied. The prescriptionsof Rotigotine were designed. Pharmaceutical analysis methodology, properties in vitroand quality standards were studied.Using a modified Franz diffusion cell, samples were collected at various timepoints after the start of test. The concentrations of rotigotine in the samples weremeasured by HPLC. The transdermal amount of drugs has been influenced by thepermeation enhancer. The permeability of rotigotine has been greatly increased by thepermeation enhancer of5%A.There were good reproducibilities between the process of drug-releasing andtransdermal diffusion in vitro among different batches；The steady penetration rates ofrotigotine of self-made products and foreign products in vitro were9.210μg cm-2h-1,8.796μg cm-2h-1, respectively. There was no significant difference among thepermeation rates of two products. The self-made patches have good property ofpenetration, and the percutaneous absorption through guinea pig skins are similar toforeign products. Rotigotine residues were detected in the patches and skins after thetwo sources of the patches were removed from the tested skins. The amount ofrotigotine residues counted for2％～4％of the total medicine in patches.Quality measures included sample size and shape, homogeneity, detection ofrelated substances, residual solvent，release rates, penatration rates and adhesiveness.The experimental results indicate that all the items mentioned above are conforming to standards of the2010th edition of Chinese pharmacopoeia.