Objective:To develop floating microspheres of cefpodoxime proxetil(CP) in order to achieve an extended retention in the upper GIT for 12 hour.Methods:The microspheres were prepared by non aqueous solvent evaporation m...Objective:To develop floating microspheres of cefpodoxime proxetil(CP) in order to achieve an extended retention in the upper GIT for 12 hour.Methods:The microspheres were prepared by non aqueous solvent evaporation method using different ratios of cefpodoxime proxetil, hydroxyl propyl methyl cellulose(HPMC K4M ) and ethyl cellulose(1:1:1,1:1:2,1:1:3,1:1:4, 1:1:5 & 1:1:6),in the mixture of dichloromethane and ethanol at ratio of(l:l),with tween80 as the surfactant.Results:The floating microspheres was extended over 10-12 hours and were characterized by particle size analysis(75-600μm),buoyancy percentage(68.1%-85.4%), drug entrapment efficiency(67.5%-88.8%),%yield(50.50%-77.31%) and in vitro drug release was studied for 12 hours.Conclusions:The floating microspheres show better result and it may be use full for prolong the drug release in stomach and improve the bioavailability.展开更多
Reversed-phase liquid chromatography coupled with electrospray ionization tandem mass spectrometry(ESI-MS/MS)was used to characterize impurities in cefpodoxime proxetil,an ester-modified prodrug.Based on the mechanism...Reversed-phase liquid chromatography coupled with electrospray ionization tandem mass spectrometry(ESI-MS/MS)was used to characterize impurities in cefpodoxime proxetil,an ester-modified prodrug.Based on the mechanisms by which cephalosporins are degraded,stress tests were designed and performed.The bulk material and capsule were eluted through a C18 column with formic acid–methanol–water as the mobile phase.In total,15 impurities were characterized in commercial samples,including 7 known impurities and 8 new impurities.The structures of these unknown compounds were deduced via comparison with the fragmentation patterns of cefpodoxime proxetil.Data from this systematic study will help improve the safety and quality of cefpodoxime proxetil.展开更多
文摘Objective:To develop floating microspheres of cefpodoxime proxetil(CP) in order to achieve an extended retention in the upper GIT for 12 hour.Methods:The microspheres were prepared by non aqueous solvent evaporation method using different ratios of cefpodoxime proxetil, hydroxyl propyl methyl cellulose(HPMC K4M ) and ethyl cellulose(1:1:1,1:1:2,1:1:3,1:1:4, 1:1:5 & 1:1:6),in the mixture of dichloromethane and ethanol at ratio of(l:l),with tween80 as the surfactant.Results:The floating microspheres was extended over 10-12 hours and were characterized by particle size analysis(75-600μm),buoyancy percentage(68.1%-85.4%), drug entrapment efficiency(67.5%-88.8%),%yield(50.50%-77.31%) and in vitro drug release was studied for 12 hours.Conclusions:The floating microspheres show better result and it may be use full for prolong the drug release in stomach and improve the bioavailability.
基金Financial support by the Twelfth Five-year National Science and Technology Support Program“The research and development of new material for separation and integration demonstration”(No.2012BAK25B02)is gratefully acknowledged.
文摘Reversed-phase liquid chromatography coupled with electrospray ionization tandem mass spectrometry(ESI-MS/MS)was used to characterize impurities in cefpodoxime proxetil,an ester-modified prodrug.Based on the mechanisms by which cephalosporins are degraded,stress tests were designed and performed.The bulk material and capsule were eluted through a C18 column with formic acid–methanol–water as the mobile phase.In total,15 impurities were characterized in commercial samples,including 7 known impurities and 8 new impurities.The structures of these unknown compounds were deduced via comparison with the fragmentation patterns of cefpodoxime proxetil.Data from this systematic study will help improve the safety and quality of cefpodoxime proxetil.
