Preparation Of Nitrendipine Tablets Based On Mesoporous SnO₂ And Its Properties Study

Objective The purpose of this experiment is to prepare the mesoporous SnO₂?MSn? with a three-dimensional mesoporous structure for increasing the solubility of the poorly water-soluble drugs,improving its dissolution rate and oral bioavailability.Nitrendipine?NDP? was chosed as a model drug to prepare NDP-MSn tablets and study its dissolution in vitro and pharmacokinetics in rabbits.Methods In this study,the mesoporous SnO₂?MSn?was prepared by template method.Nitrendipine?NDP? was incorporated into the pore channels of MSn by adsorption method.The structural features of MSn were characterized by transmission electron microscopy?TEM?,scanning electron microscopy?SEM?,and N₂ adsorption?desorption? analysis.The physical state of NDP in the NDP-MSn was characterized by powder X-ray diffraction?PXRD?,differential scanning calorimetry?DSC? and Fourier transform infrared spectroscopy?FTIR?.The biological safety of MSn was evaluated by cytotoxicity test?MTT?.The dissolution behavior of NDP was investigated by In vitro tests.The NDP-MSn tablets were prepared by direct compression method.The types and dosages of adhesives and disintegrants in the prescription were investigated and optimized based on the cumulative dissolution.The self-made NDP-MSn tablets were examined according to the quality requirements of tablets in the Pharmacopoeia?2015? and the bioavailability of self-made NDP-MSn tablets was studied by the in vivo pharmacokinetic assay.Results MSn was successfully prepared.DSC,PXRD and FT-IR indicated that NDP existed in the pore channels MSn with an amorphous state.MSn showed a good biocompatibility in the cell toxicity assay for Caco-2 cells.In vitro dissolution results suggested that MSn could significantly enhance the dissolution rate of NDP.The self-made MSn-NDP tablets were prepared by lactose as the filler,sodium carboxymethyl starch?CMS-Na? as disintegrant,polyvinylpyrrolidone?PVP? as adhesive,magnesium stearate as lubricant.And the quality test results of MSn-NDP tablets were in compliance with the pharmacopoeia requirements.Pharmacokinetic studies indicated that NDP-MSn tablets effectively enhanced the oral bioavailability of NDP.Conclusions MSn has high specific surface area and large pore volume,which can improve the water solubility.The NDP-MSn tablets prepared in this study can improve the dissolution rate and oral bioavailability of NDP.Hence,MSn,as a novel safe inorganic nanoporous carrier,provides a new way to increase the dissolution rate and oral bioavailability of insoluble drugs.