Formulation Development For The Enhancement Of Solubility Of Orlistat And Curcumin

Abstract

The usage of amorphous, solid dispersions is one of the most popular formulation strategies newlineused to improve in-vitro and in-vivo performance of low water-soluble medications. On newlinethe other hand, because of their meta-stable nature, the physical strength of amorphous newlinesolid dispersions is considered as the primary impediment to pharmaceutical research and newlinemarketing. This study aimed at understanding, predicting, improving the solubility of two newlineweakly water-soluble medicines and improving physical stability, namely Orlistat (ORL) newlineand Curcumin (CUR) by formulating solid dispersions and nanoemulgel using different newlinecarriers and adsorbents. and#946;-Cyclodextrin, Poloxomer-188and407, PVPK30, PVPP, PEG 400 newlineand 1000, HPMC, Microcrystalline cellulose, Lactose, Spray dried lactose, Mannitol, newlineCarbopol 934, Caffeine, Piperine, Olive oil and Tween 20 were used as physical property newlinemodifying agent for both the drugs. Solid dispersions with Orlistat and Curcumin were newlineprepared by physical mixing; melting method; kneading method and co-solvent newlineevaporation method while the nanoemulgel was prepared with olive oil, tween 20 and PEG newline400. Various techniques were used to characterize the solid dispersions, immediately after newlinethey were made and after three months of elevated temperature and relative humidity newlinestability studies. A series of physicochemical characterization techniques including newlineDifferential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy newline(FTIR), Scanning Electron Microscopy (SEM) and in vitro dissolution studies were used newlineto evaluate the systems. newlineA method development and validation of both Orlistat and Curcumin on High Performance newlineLiquid Chromatography were carried out with physical characterization of model drugs and newlinepolymers, prediction of drug-polymer error and solubility, and in real time with physical newlinestability studies on differing conditions (HPLC). In this study, it was shown that the physical newlinestrength of the amorphous drugs and the apparent solubility of the processing-related drug newlinepolymer are the two main factors