System design and evaluation of stomach specific drug delivery systems for sustained release

Abstract

newlineDepression is a chronic, recurring, and potentially life-threatening illness that affects newlineup to 20% of the population across the globe. This disease is one of the top ten causes of newlinemorbidity and mortality worldwide and represents a high cost to country s economy. newlineAvailable therapy for depression treatment is often associated with several undesirable side newlineeffects, and its effectiveness achieves only a certain portion of the population. Therefore, the newlineidentification of alternative therapeutic tools for the treatment of depression is of high newlineimportance. newlineVenlafaxine hydrochloride is known as a serotonin-norepinephrine reuptake inhibitor newlineand used to treat depression. Due to the short elimination half life of 4-5 h, the drug has to newlinebe administred 2-3 times in a day to maintain the plasma concentration. Thus an attempt was newlinemade to decrease the dosing frequency. The present work was to formulate floating newlinemicrosphere and floating tablets of venlafaxine hydrochloride, used to treat depression. The newlinemicrospheres were prepared by non-aqueous solvent evaporation method. The floating newlinetablets were prepared by direct compression method using HPMC K100M and Pullulan gum newlineas polymer in different combinations. Sodium bicarbonate and citric acid were added to newlinecause effervescence. The microspheres were evaluated for particle size and morphology newlineusing a photomicroscope and scanning electron microscopy, respectively. The incorporation newlineefficiency of microspheres of batch FM2 and FM6 showed entrapment of 60.6±2.09 % and newline57.2±1.90 %, respectively. The mean diameters of particles for all batches were found in the newlinerange of 226.15 ± 24.37 and 283.37 ± 21.56 and#956;m. The Fourier transform infrared newlinespectroscopy revealed absence of any drug-polymer interactions. The microsphers remained newlinebuoyant for more than 12 h. The drug release from developed microspheres followed newlineFickian diffusion with swelling. The radiographic study of microspheres containing barium newlinemeal showed that microspheres remained buoyant for more than 8 h.