A combination of melt-granulated dispersion and surface adsorption techniques was used to enhance the dissolution and tableting properties of cefuroxime axetil(CA).Gelucire 50/13 was used as the melt-dispersion carrie...A combination of melt-granulated dispersion and surface adsorption techniques was used to enhance the dissolution and tableting properties of cefuroxime axetil(CA).Gelucire 50/13 was used as the melt-dispersion carrier and Sylysia 350 was used to adsorb the melt dispersion.Solubility studies showed an 8-fold increase in solubility at a ratio of 1:1.5 for CA:Gelucire 50/13.The minimum quantity of Sylysia 350 required to achieve the desired flowability and compressibility was 0.5 parts of Sylysia 350 per unit of Gelucire 50/13.Phase solubility studies showed negative ΔG_(tr)^(0) values for Gelucire 50/13 at various concentrations(2-10%,vv/v),indicating the spontaneous nature of solubilization.FT-IR and DSC spectra exhibited drug-excipient compatibility.Molecular modeling by a computational method employing energy minimization revealed entrapment of CA in Gelucire 50/13.The total potential energy of CA(70.562 keal/mol)was reduced to 33.578 keal/mol after solid dispersion with Gelucire 50/13.P-XRD studies indicated that the presence of Sylysia 350 is less likely to promote the reversion of the amorphous CA to a crystalline state.In vitro dissolution studies demonstrated an improved dissolution rate,and drug release at 15 min(Q_(15min))exhibited a 15-fold improvement.The rapidly dissolving CA tablets showed improved dissolution with improved tableting properties.展开更多
文摘A combination of melt-granulated dispersion and surface adsorption techniques was used to enhance the dissolution and tableting properties of cefuroxime axetil(CA).Gelucire 50/13 was used as the melt-dispersion carrier and Sylysia 350 was used to adsorb the melt dispersion.Solubility studies showed an 8-fold increase in solubility at a ratio of 1:1.5 for CA:Gelucire 50/13.The minimum quantity of Sylysia 350 required to achieve the desired flowability and compressibility was 0.5 parts of Sylysia 350 per unit of Gelucire 50/13.Phase solubility studies showed negative ΔG_(tr)^(0) values for Gelucire 50/13 at various concentrations(2-10%,vv/v),indicating the spontaneous nature of solubilization.FT-IR and DSC spectra exhibited drug-excipient compatibility.Molecular modeling by a computational method employing energy minimization revealed entrapment of CA in Gelucire 50/13.The total potential energy of CA(70.562 keal/mol)was reduced to 33.578 keal/mol after solid dispersion with Gelucire 50/13.P-XRD studies indicated that the presence of Sylysia 350 is less likely to promote the reversion of the amorphous CA to a crystalline state.In vitro dissolution studies demonstrated an improved dissolution rate,and drug release at 15 min(Q_(15min))exhibited a 15-fold improvement.The rapidly dissolving CA tablets showed improved dissolution with improved tableting properties.
