ABSTRACT
The stereoselective hydrolysis of esmolol in whole blood and in its separated components from rat,rabbit and human was investigated.Blood esterase activities were variable in different species in the order of rat ＞ rabbit ＞ human.Rat plasma showed the high esterase activity and had no stereoselectivity to enantiomers.Rabbit red blood cell (RBC) membrane,RBC cytosol and plasma all hydrolyzed esmolol but with different esterase activity,whereas the hydrolysis in RBC membrane and cytosol showed significant stereoselectivity towards R-(+)-esmolol.Esterase in RBC cytosol from human blood mainly contributed to the esmolol hydrolysis,which was demonstrated with no stereoselctivity.Esterase in human plasma showed a low activity,but a remarkable stereoselectivity with R-(+)-esmolol.In addition,the protein concentration affected the hydrolysis behavior of esmolol in RBC suspension.Protein binding of esmolol enantiomers in human plasma,human serum albumin (HSA) and α1-acid glycoprotein (AGP) revealed that there was a significant difference in bound fractions between two enantiomers,especially for AGP.Our results indicated that the stereoselective protein binding might play a role in the different hydrolysis rates of esmolol enantiomers in human plasma.
ABSTRACT
The protein binding of non-steroidal anti-inflammatory drugs flurbiprofen,ketoprofen and etodolac with human serum albumin (HSA) was investigated using indirect chiral high performance liquid chromatography (HPLC) and ultrafiltration techniques.S-(-)-2-(1-naphthyl)-ethylamine (S-NEA) was utilized as chiral derivatization reagent and pre-column derivatization RP-HPLC method was established for the separation and assay of the three pairs of enantiomer.The method had good linear relationship over the investigated concentration range without interference.The average extraction efficiency was higher than 85％ in different systems,and the intra-day and inter-day precisions were less than 15％.In serum albumin,the protein binding of etodolac enantiomers showed significant stereoselectivity that the affinity of S-enantiomer was stronger than R-enantiomer,and the stereoselectivity ratio reached 6.06; Flurbiprofen had only weak stereoselectivity in HSA,and ketoprofen had no stereoselectivity at all.Scatchard curves showed that all the three chiral drugs had two types of binding sites in HSA.
ABSTRACT
The protein binding of non-steroidal anti-inflammatory drugs flurbiprofen, ketoprofen and etodolac with human serum albumin （HSA） was investigated using indirect chiral high performance liquid chromatography （HPLC） and ultrafiltration techniques. S-（-）-1-（1-naphthyl）- ethylamine （S-NEA） was utilized as chiral derivatization reagent and pre-column derivatization RP-HPLC method was established for the separation and assay of the three pairs of enantiomer. The method had good linear relationship over the investigated concentration range without interference. The average extraction efficiency was higher than 85% in different systems, and the intra-day and inter-day precisions were less than 15%. In serum albumin, the protein binding of etodolac enantiomers showed significant stereoselectivity that the affinity of S-enantiomer was stronger than R-enantiomer, and the stereoselectivity ratio reached 6.06; Flurbiprofen had only weak stereoselectivity in HSA, and ketoprofen had no stereoselectivity at all. Scatchard curves showed that all the three chiral drugs had two types of binding sites in HSA.
ABSTRACT
Under the great support of the government,the vocational education of the three gorges reservoir area has made great progress in recent years.But the model and idea of the traditional vocational education,together with the construction on low level,become the block of its development.This passage finds out the lack in the vocational education in the three gorges reservoir.It also gives the suggestion of how to improve the current situation and expand the thoughts of employment to actualize the transference of labor force and the reemployment.
ABSTRACT
According to the changeover of modern medical teaching mode and the undergraduates' need of knowledge structure,we started the course Sociology of Sexuality in our university.In more than 3 years teaching experience and exploration,we arranged the content for each part of each chapter based on the teaching outline,teaching scheme and the students' knowledge and ability structure.As to teaching method,we adopted multimedia computer instruction,heuristic instruction,interactive instruction,participating teaching and audio-visual digital teaching method and so on.We are to introduce such a teaching means of exchange communication,and such an examination method combined with the traditional test as well as testing the capability of handling the actual problem,which can help to implementing the teaching work for Sociology of Sexuality.