Enhancement of solubility & dissolution rate of Nifedipine by using Novel Solubilizer sepitrap 80 & Sepitrap 4000

Abstract

The enhancement in solubility and dissolution rate of BCS class-II drug Nifedipine was achieved by simple physical mixture with sepitrap 80 & sepitrap 4000 in 1:1 & 1:2 proportion. The saturation solubility studies shows 263 % & 368 % increase in the solubility in physical mixture of Nifedipine with sepitrap 80 & sepitrap 4000 respectively. The physicochemical properties of pure Nifedipine compared to their physical mixtures with sepitrap 80 & sepitrap 4000 were determined using FTIR, DSC & PXRD. The FTIR and DSC studies shows no any interaction in Nifedipine and sepitrap, the marked broadening and distinct reduction in intensity with shifting of drug endotherm was displayed physical mixture with sepitrap demonstrate positive effect. The PXRD diffractograms shows distinctive peaks but reduction in peak intensity in terms of counts indicating conversion of drug in amorphous forms. The surface morphology of the prepared physical mixture was examined by SEM which indicating no significant change in its surface morphology due to no use any solvent during the preparation of physical mixture . Photostability studies shows that rate of photo degradation is very slow in Physical mixture with sepitrap as compared to pure Nifedipine. Dissolution studies in SGF & SIF shows that significant enhancement by use of novel solubilizer sepitrap 80 as well as sepitrap 4000 in 1:2 proportions. The physical mixture containing sepitrap 4000 was found stable as there was no any significant change in appearance and drug dissolution after three month stability studies.