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...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.展开更多
A simple and selective micellar electrokinetic chromatographic （MEKC） method has been developed for the analysis of five pharmaceutical binary mixtures containing three non-steroidal antiinflammatory drugs （NSAIDs...A simple and selective micellar electrokinetic chromatographic （MEKC） method has been developed for the analysis of five pharmaceutical binary mixtures containing three non-steroidal antiinflammatory drugs （NSAIDs）. The investigated mixtures were Ibuprofen （IP）-Paracetamol （PC）, Ibuprofen （IP）-Chlorzoxazone （CZ）, Ibuprofen （IP）Methocarbamol （MC）, Ketoprofen （KP） Chlorzoxazone （CZ） and Diclofenac sodium （DS）-Lidocaine hydrochloride （LC）. The separation was run for all mixtures using borate buffer （20 mM, pH 9） containing 15% （v/v） methanol and 100 mM sodium dodecyl sulphate （SDS） at 15 kV and the components were detected at 214 nm. Different factors affecting the electrophoretic mobility of the seven investigated drugs were studied and optimized. The method was validated according to international conference of harmonization （ICH） guidelines and United States pharmacopoeia （USP）. The method was applied to the analysis of five pharmaceutical binary mixtures in their dosage forms. The results were compared with other reported high performance liquid chromatographic methods and no significant differences were observed.展开更多
基金supported by National Major Projects for Science and Technology Development of Ministry Science and Technology of China (2009ZX09304-003)
文摘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.
文摘A simple and selective micellar electrokinetic chromatographic （MEKC） method has been developed for the analysis of five pharmaceutical binary mixtures containing three non-steroidal antiinflammatory drugs （NSAIDs）. The investigated mixtures were Ibuprofen （IP）-Paracetamol （PC）, Ibuprofen （IP）-Chlorzoxazone （CZ）, Ibuprofen （IP）Methocarbamol （MC）, Ketoprofen （KP） Chlorzoxazone （CZ） and Diclofenac sodium （DS）-Lidocaine hydrochloride （LC）. The separation was run for all mixtures using borate buffer （20 mM, pH 9） containing 15% （v/v） methanol and 100 mM sodium dodecyl sulphate （SDS） at 15 kV and the components were detected at 214 nm. Different factors affecting the electrophoretic mobility of the seven investigated drugs were studied and optimized. The method was validated according to international conference of harmonization （ICH） guidelines and United States pharmacopoeia （USP）. The method was applied to the analysis of five pharmaceutical binary mixtures in their dosage forms. The results were compared with other reported high performance liquid chromatographic methods and no significant differences were observed.
