The objective of this study was to develop once-daily metformin hydrochloride sustained-release tablets (MHSRT) and evaluate their in vitro release behavior. MHSRT were prepared by the film coating method. The in vitr...The objective of this study was to develop once-daily metformin hydrochloride sustained-release tablets (MHSRT) and evaluate their in vitro release behavior. MHSRT were prepared by the film coating method. The in vitro drug release rate of MHSRT and the commercial tablets Fortamet? made in the United States of America in water was fitted with zero order kinetic equation, and Ritger-Peppas kinetic equation in 0.1 M HCl and pH 6.8-phosphate buffer, respectively. The similarity factor f2 values of MHSRT in three different dissolution medium were 82, 80 and 74, respectively in comparison with imported Fortamet?, which were all greater than 50. The results of storage-stability showed that MHSRT were stable for at least 6 months under stress condition (40℃ ± 2℃, RH 75% ± 5%). Therefore, in this study, MHSRT were successfully prepared using optimized formulation technologies that meet mass produce. The in vitro release behavior of MHSRT was almost similar to that of imported Fortamet?.展开更多
In this work, a novel and simple flexible aromatic multi-carboxylate compound N,N＇（4,4＇-biphenylyl） iminodi- acetic acid （BP-IDA） was synthesized, with which two new stable metaMDA gels （denoted as MIGl and MlG...In this work, a novel and simple flexible aromatic multi-carboxylate compound N,N＇（4,4＇-biphenylyl） iminodi- acetic acid （BP-IDA） was synthesized, with which two new stable metaMDA gels （denoted as MIGl and MlG2） with three-dimensional network structures have been prepared successfully by employing Cr^3＋ and Al^3＋ as the metal ions, respectively. The rheological performance was investigated by means of dynamic rheology measurement. The morphology and microstructure were characterized by scanning electron microscopy, transmission elec- tron microscopy, and X-ray diffraction technique. Nitrogen sorption isotherm measurement suggests that the MlG1 aerogel has considerable porosity with the Brunauer-Emmett-Teller specific surface area up to 760 m^2·g^-1. Owing to easy preparation, good stability, and three-dimensional network structure, the as-prepared metal-organic gels will possess potential applications in separation, catalysis, and drug delivery.展开更多
The novel 1,2-diaryl substituted pyrrolo[3,4-b]pyridine-5,7-diones were selectively synthesized in high yields by the base catalyzed cyclization reaction of 3-arylamino-l-methyl-lH-pyrrole-2,5-diones with cinnamaldehy...The novel 1,2-diaryl substituted pyrrolo[3,4-b]pyridine-5,7-diones were selectively synthesized in high yields by the base catalyzed cyclization reaction of 3-arylamino-l-methyl-lH-pyrrole-2,5-diones with cinnamaldehyde and its derivatives in acetonitrile at room temperature. However, when piperidinium trifluoroacetate was employed as catalyst, the reaction afforded a mixture of 1,2-diaryl and 1,4-diaryl substituted pyrrolo[3,4-b]pyridine-5,7-diones in comparable yields.展开更多
We have developed a facile N-terminus helix-nucleating strategy using an unnaturally tethered aspartic acid(TD strategy). Relatively weak nuclear translocation efficiency of TD PERM limits its further biological appli...We have developed a facile N-terminus helix-nucleating strategy using an unnaturally tethered aspartic acid(TD strategy). Relatively weak nuclear translocation efficiency of TD PERM limits its further biological applications. A potent peptide inhibitor of estrogen receptor α(ER-α) with significantly increased cellular uptake and cellular distribution was developed by cell penetrating peptide attachment.The resulted peptide conjugate showed selective toxicity towards estrogen receptor positive cell lines and induced decreased transcription of estrogen receptor a downstream genes.展开更多
文摘The objective of this study was to develop once-daily metformin hydrochloride sustained-release tablets (MHSRT) and evaluate their in vitro release behavior. MHSRT were prepared by the film coating method. The in vitro drug release rate of MHSRT and the commercial tablets Fortamet? made in the United States of America in water was fitted with zero order kinetic equation, and Ritger-Peppas kinetic equation in 0.1 M HCl and pH 6.8-phosphate buffer, respectively. The similarity factor f2 values of MHSRT in three different dissolution medium were 82, 80 and 74, respectively in comparison with imported Fortamet?, which were all greater than 50. The results of storage-stability showed that MHSRT were stable for at least 6 months under stress condition (40℃ ± 2℃, RH 75% ± 5%). Therefore, in this study, MHSRT were successfully prepared using optimized formulation technologies that meet mass produce. The in vitro release behavior of MHSRT was almost similar to that of imported Fortamet?.
文摘In this work, a novel and simple flexible aromatic multi-carboxylate compound N,N＇（4,4＇-biphenylyl） iminodi- acetic acid （BP-IDA） was synthesized, with which two new stable metaMDA gels （denoted as MIGl and MlG2） with three-dimensional network structures have been prepared successfully by employing Cr^3＋ and Al^3＋ as the metal ions, respectively. The rheological performance was investigated by means of dynamic rheology measurement. The morphology and microstructure were characterized by scanning electron microscopy, transmission elec- tron microscopy, and X-ray diffraction technique. Nitrogen sorption isotherm measurement suggests that the MlG1 aerogel has considerable porosity with the Brunauer-Emmett-Teller specific surface area up to 760 m^2·g^-1. Owing to easy preparation, good stability, and three-dimensional network structure, the as-prepared metal-organic gels will possess potential applications in separation, catalysis, and drug delivery.
文摘The novel 1,2-diaryl substituted pyrrolo[3,4-b]pyridine-5,7-diones were selectively synthesized in high yields by the base catalyzed cyclization reaction of 3-arylamino-l-methyl-lH-pyrrole-2,5-diones with cinnamaldehyde and its derivatives in acetonitrile at room temperature. However, when piperidinium trifluoroacetate was employed as catalyst, the reaction afforded a mixture of 1,2-diaryl and 1,4-diaryl substituted pyrrolo[3,4-b]pyridine-5,7-diones in comparable yields.
基金financial support from the National Natural Science Foundation of China (Nos. 21778009 and 81701818 MOST2015DFA31590)the Shenzhen Science and Technology Innovation Committee (Nos. JCYJ20170412150719814 and GJHS20170310093122365)
文摘We have developed a facile N-terminus helix-nucleating strategy using an unnaturally tethered aspartic acid(TD strategy). Relatively weak nuclear translocation efficiency of TD PERM limits its further biological applications. A potent peptide inhibitor of estrogen receptor α(ER-α) with significantly increased cellular uptake and cellular distribution was developed by cell penetrating peptide attachment.The resulted peptide conjugate showed selective toxicity towards estrogen receptor positive cell lines and induced decreased transcription of estrogen receptor a downstream genes.
