The purpose of the present study was to investigate the interaction of Cinnarizine(CIN)with Hydroxypropyl-β-Cyclodextrin(HPβCD)in the presence of Hydroxy Acids(HA).Various binary and ternary systems of CIN with HPβ...The purpose of the present study was to investigate the interaction of Cinnarizine(CIN)with Hydroxypropyl-β-Cyclodextrin(HPβCD)in the presence of Hydroxy Acids(HA).Various binary and ternary systems of CIN with HPβCD and HA were prepared by kneading and coevaporation methods.For the ternary systems,HA were tried in three different concentrations.The interaction in solution phase was studied in detail by the phase solubility method,and the solid phase interactions were characterized by Fourier Transform Infrared(FTIR)spectroscopy,Differential Scanning Calorimetry(DSC),X-Ray Diffractometry(XRD),Scanning Electron Microscopy(SEM)and Proton Nuclear Magnetic Resonance(^1H-NMR).Phase solubility revealed the positive effect of HA on the complexation of CIN with HPβCD.Solid phase characterization confirmed the formation of inclusion complex in the ternary systems.Solubility and dissolution studies illustrated that out of three different concentrations tried,HA were most effective at the 1 M concentration level.Ternary systems were very effective in improving the solubility as well as dissolution profile of CIN than the CIN–HPβCD binary systems.FTIR,^1H-NMR and Molecular docking studies gave some insight at molecular level that actually which part of CIN was interacting with the HPβCD.Molecular docking and free energy calculation even enlighten the role of tartaric acid in increasing solubility of CIN in the ternary system.展开更多
In the development of new drugs as well as new formulations of existing products(including generic products),it is of great interest to be able to predict to what extent the drug can be absorbed from the gastrointesti...In the development of new drugs as well as new formulations of existing products(including generic products),it is of great interest to be able to predict to what extent the drug can be absorbed from the gastrointestinal(GI)tract and how the formulation and dosing conditions may affect the absorption profile.The hypothesis behind Biorelevant release testing is that“the closer the test conditions can simulate the gastrointestinal environment,the better the prediction will be.”Typical aspects of GI physiology,which can influence drug bioavailability,are the composition of the GI fluids(which affects various processes including release from the dosage form and stability of the drug),GI motility and hydrodynamics(transit characteristics of the dosage form,release from the dosage form etc.).展开更多
文摘The purpose of the present study was to investigate the interaction of Cinnarizine(CIN)with Hydroxypropyl-β-Cyclodextrin(HPβCD)in the presence of Hydroxy Acids(HA).Various binary and ternary systems of CIN with HPβCD and HA were prepared by kneading and coevaporation methods.For the ternary systems,HA were tried in three different concentrations.The interaction in solution phase was studied in detail by the phase solubility method,and the solid phase interactions were characterized by Fourier Transform Infrared(FTIR)spectroscopy,Differential Scanning Calorimetry(DSC),X-Ray Diffractometry(XRD),Scanning Electron Microscopy(SEM)and Proton Nuclear Magnetic Resonance(^1H-NMR).Phase solubility revealed the positive effect of HA on the complexation of CIN with HPβCD.Solid phase characterization confirmed the formation of inclusion complex in the ternary systems.Solubility and dissolution studies illustrated that out of three different concentrations tried,HA were most effective at the 1 M concentration level.Ternary systems were very effective in improving the solubility as well as dissolution profile of CIN than the CIN–HPβCD binary systems.FTIR,^1H-NMR and Molecular docking studies gave some insight at molecular level that actually which part of CIN was interacting with the HPβCD.Molecular docking and free energy calculation even enlighten the role of tartaric acid in increasing solubility of CIN in the ternary system.
文摘In the development of new drugs as well as new formulations of existing products(including generic products),it is of great interest to be able to predict to what extent the drug can be absorbed from the gastrointestinal(GI)tract and how the formulation and dosing conditions may affect the absorption profile.The hypothesis behind Biorelevant release testing is that“the closer the test conditions can simulate the gastrointestinal environment,the better the prediction will be.”Typical aspects of GI physiology,which can influence drug bioavailability,are the composition of the GI fluids(which affects various processes including release from the dosage form and stability of the drug),GI motility and hydrodynamics(transit characteristics of the dosage form,release from the dosage form etc.).
