AIM： To investigate the effect of release behavior of sustained-release dosage forms of sinomenine hydrochloride （SM·HCl） on its pharmacokinetics in beagle dogs. METHODS： The in vitro release behavior of two ...AIM： To investigate the effect of release behavior of sustained-release dosage forms of sinomenine hydrochloride （SM·HCl） on its pharmacokinetics in beagle dogs. METHODS： The in vitro release behavior of two SM·HCl dosage forms, including commercial 12-h sustained-release tablets and 24-h sustained-release pellets prepared in our laboratory, was examined. The two dosage forms were orally administrated to beagle dogs, and then the in vivo SM.HCI pharmacokinetics was investigated and compared. RESULTS： The optimal SM·HCl sustained-release formulation was achieved by mixing slow- and rapidrelease pellets （9：1, w/w）. The SM·HCl release profiles of the sustained-release pellets were scarcely influenced by the pH of the dissolution medium. Release from the 12-h sustained-release tablets was markedly quicker than that from the 24-h sustained-release pellets, the cumulative release up to 12-h was 99.9% vs68.7%. From a pharmacokinetic standpoint, the 24-h SM.HCI sustainedrelease pellets had longer tmax and lower Cmax compared to the 12-h sustained-release tablets, the tmax being 2.67±0.52 h vs 9.83±0.98 h and the Cmax being 1334.45±368.76 ng/mL vs 893.12±292.55 ng/mL, respectively. However, the AUC0-tn of two SM·HCl dosage forms was comparable and both preparations were statistically bioequivalent. Furthermore, the two preparations had good correlations between SM·HCl percentage absorption in vivoand the cumulative percentage release in vitro. CONCLUSION： The in vitro release properties of the dosage forms strongly affect their pharmacokinetic behavior in vivo. Therefore, managing the in vitro release behavior of dosage forms is a promising strategy for obtaining the optimal in vivo pharmacokinetic characteristics and safe therapeutic drug concentration-time curves.展开更多
The production of chemicals from biomass is a very challenging process due to its diverse chemical composition. Lignin, cellulose and hemicellulose are the three main biopolymers of wood biomass, with cell walls ＆pla...The production of chemicals from biomass is a very challenging process due to its diverse chemical composition. Lignin, cellulose and hemicellulose are the three main biopolymers of wood biomass, with cell walls ＆plant origin. Lignin has been chosen for the present studies due to its range of different linkages and structures. The present work involved a computational study of the most dominant lignin dimers and their vibrational structures, based on the Density Functional Theory method. Full geometry optimization of the compartments used the StoBe code with cluster model and non-local functional （RPBE） approach. The calculations of the vibrational frequencies were performed with harmonic approximations as well as an anharmonicity fit in the Morse potential function, as implemented in the StoBe code. In the case oflignin, the calculations included three different precursors based on： coumaryl alcohol, coniferyl alcohol and sinapyl alcohol. To represent the cellulose and hemicellulose derivatives, selected aldopentoses and aldohexoses （arabinose, xylose, glucose, galactose, and mannose） were considered. Presented here are the theoretical investigations for a variety of biomass derived compounds, to give the possibility of obtaining a theoretical VBD （Vibrations Basis Database） for experimental spectra interpretation. Such a database could be further used in the preliminary composition assessment of biomass derived substrates, which will be discussed here in more detail.展开更多
文摘AIM： To investigate the effect of release behavior of sustained-release dosage forms of sinomenine hydrochloride （SM·HCl） on its pharmacokinetics in beagle dogs. METHODS： The in vitro release behavior of two SM·HCl dosage forms, including commercial 12-h sustained-release tablets and 24-h sustained-release pellets prepared in our laboratory, was examined. The two dosage forms were orally administrated to beagle dogs, and then the in vivo SM.HCI pharmacokinetics was investigated and compared. RESULTS： The optimal SM·HCl sustained-release formulation was achieved by mixing slow- and rapidrelease pellets （9：1, w/w）. The SM·HCl release profiles of the sustained-release pellets were scarcely influenced by the pH of the dissolution medium. Release from the 12-h sustained-release tablets was markedly quicker than that from the 24-h sustained-release pellets, the cumulative release up to 12-h was 99.9% vs68.7%. From a pharmacokinetic standpoint, the 24-h SM.HCI sustainedrelease pellets had longer tmax and lower Cmax compared to the 12-h sustained-release tablets, the tmax being 2.67±0.52 h vs 9.83±0.98 h and the Cmax being 1334.45±368.76 ng/mL vs 893.12±292.55 ng/mL, respectively. However, the AUC0-tn of two SM·HCl dosage forms was comparable and both preparations were statistically bioequivalent. Furthermore, the two preparations had good correlations between SM·HCl percentage absorption in vivoand the cumulative percentage release in vitro. CONCLUSION： The in vitro release properties of the dosage forms strongly affect their pharmacokinetic behavior in vivo. Therefore, managing the in vitro release behavior of dosage forms is a promising strategy for obtaining the optimal in vivo pharmacokinetic characteristics and safe therapeutic drug concentration-time curves.
文摘The production of chemicals from biomass is a very challenging process due to its diverse chemical composition. Lignin, cellulose and hemicellulose are the three main biopolymers of wood biomass, with cell walls ＆plant origin. Lignin has been chosen for the present studies due to its range of different linkages and structures. The present work involved a computational study of the most dominant lignin dimers and their vibrational structures, based on the Density Functional Theory method. Full geometry optimization of the compartments used the StoBe code with cluster model and non-local functional （RPBE） approach. The calculations of the vibrational frequencies were performed with harmonic approximations as well as an anharmonicity fit in the Morse potential function, as implemented in the StoBe code. In the case oflignin, the calculations included three different precursors based on： coumaryl alcohol, coniferyl alcohol and sinapyl alcohol. To represent the cellulose and hemicellulose derivatives, selected aldopentoses and aldohexoses （arabinose, xylose, glucose, galactose, and mannose） were considered. Presented here are the theoretical investigations for a variety of biomass derived compounds, to give the possibility of obtaining a theoretical VBD （Vibrations Basis Database） for experimental spectra interpretation. Such a database could be further used in the preliminary composition assessment of biomass derived substrates, which will be discussed here in more detail.
