Formulation development and evaluation of extended release multiparticulate system for anti depressant drugs

Abstract

quotBackground: Due to unfavorable physicochemical properties of many successful API, expected pharmacological action cannot be achieved through conventional dosage forms. Moreover, sustained release dosage forms (e.g. matrix tablet) elicit toxicity if dose dumping occurred. To overcome such issues, extended-release multiparticulate system (Pellets) can be employed. newline newlineAim: Antidepressant drugs (Venlafaxine HCl and Desvenlafaxine Succinate) are highly water soluble molecules which are required to be formulated into pellets delivery system to achieve consistent and extended release. newline newlineMaterials and Methods: Preformulation study with detailed drug excipient study was carried out with FTIR and DSC profiling of drugs. Analytical method (UV) was developed for both drugs in different media. Development of drug loaded pellets was carried out using controlled strategies like extrusion and spheronization followed by controlled release coat and finally were encapsulated in hard gelatin capsule. Physicochemical, performance and structural characterization was done for developed system. newlineResults and Discussion: newlineResults of preformulation studies indicated suitability of selected drugs for oral solid dosage forms. Developed UV methods showed desired linearity with minimum noise. Drugs were found compatible with selected excipients. Application of QbD tools including (risk assessment, screening design) and DoE assisted in optimization of pellets. Drug release profiles at 2, 4, 8, 12, and 20 hrs was found 3.8%, 25.2%, 54.8%, 71.3% and 89.5% from VEN loaded optimized pellets and 6.5%, 24.8%, 55.3%, 72.5% and 92.5%from DVS loaded optimized pellets respectively. newline newlineConclusions: newlineDesired drug release profile was obtained from developed multiparticulate (pellets) system for both selected drugs. So, uniform blood plasma concentration can be anticipated if BCS class I drugs are incorporated into developed system. newlinequot newline