Formulation Development and Oprimization of Extended Release Matrix Tablet of SNRIs Anti Depressant Drug

Abstract

In this project work, the attempt has been made to formulate and optimize extended release matrix tablet of SNRIs an anti-depressant drug. Drug X is available in salt form for the treatment of major depressive disorder. Drug is weakly basic in nature and also having pH dependent solubility so it has high solubility in lower pH conditions compared to higher pH conditions. Due to its pH dependant solubility it has variable solubility throughout GI tract so to formulate extended release formulation of Drug X is necessity. Here an attempt has been made to match release profile of formulation containing API as base with innovator product where it is in the salt form. Hence in order to match release profile with reference product various strategies are employed in order to develop extended release formulation of Drug X as plain base to avoid the route of synthesis of salt form of drug thereby achieving economy. Different Acidifiers, Permeation Enhancers, Solubilisers, Different Combination of Polymers and Organic Acids to Modulate Micro-Environment pH condition that were various strategies approached for formulation development. Hypromellose (HPMC) phthalate, Eudragit L100-55, Poly(methacrylic acid Co-ethylacrylate), SLS, Citric Acid Anhydrous, Alginic acid were used in different strategies from which modulation of micro-environmental pH in vicinity of the tablet using citric acid and Alginic acid was more comfortable as it may lower the pKa value of drug X create acidic environment surrounding the drug X. Central Composite Design (CCD) was applied for optimizing the prototype formulation. Based on DOE outcome concluded that Concentration Of HPMC K15M, Acidifiers and Carbopol 971 P have significant effects on the release of extended release formulation.