DESIGN AND CHARACTERIZATION OF MATRIX TYPE TRANSDERMAL DRUG DELIVERY SYSTEM USING METOPROLOL TARTARATE

摘要

Transdermal drug delivery is an alternative route for systemic drug delivery which minimizes the absorption and increases the bioavailability. Oral Metoprolol tartrate has a short elimination half life (2-3 hrs), low bioavailability (35 %) undergoes extensive first pass metabolism and frequent high doses (100 mg two divided doses for 24 hrs) are required to maintain the therapeutic level as a result, dose development toxic side effects are frequently observed, so has chosen as transdermal drug delivery system. The present study was to design and characterize transdermal drug delivery system of Metoprolol tartrate using various polymers such as HPMC, PVP by solvent casting technique. Propylene glycol (30% v/v) used as a plasticizer. The prepared formulation were evaluated for different physicochemical characteristics like thickness, folding endurance, drug content, percentage moisture absorption, percentage moisture loss and weight uniformity. The drug release characteristics of the formulation were studied in In-vitro conditions by using artificial semi-permeable membrane. In-vitro dissolution studies were performed in phosphate buffer (7.4 pH) for 12 hrs by using keshery chein apparatus. The in-vitro drug release plot has shown that the drug release followed zero order kinetics, which was evidenced from the regression value. Based on the drug release and physicochemical values obtained the formulation M VI is considered as an optimized formulation which shows higher percentage of drug release (98.92 % at 12 hour) with non-fickian type diffusion mediated mechanism.