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Zhu, LiQin,Yang, JianWei,Zhang, Yuan,Wang, YongMing,Zhang, JianLei,Zhao, YuanYuan,Dong, WeiLin The Korean Society of Pharmacology 2015 The Korean Journal of Physiology & Pharmacology Vol.19 No.2
The aim of this study is to develop a physiologically based pharmacokinetic (PBPK) model in intra-abdominal infected rats, and extrapolate it to human to predict moxifloxacin pharmacokinetics profiles in various tissues in intra-abdominal infected human. 12 male rats with intra- abdominal infections, induced by Escherichia coli, received a single dose of 40 mg/kg body weight of moxifloxacin. Blood plasma was collected at 5, 10, 20, 30, 60, 120, 240, 480, 1440 min after drug injection. A PBPK model was developed in rats and extrapolated to human using GastroPlus software. The predictions were assessed by comparing predictions and observations. In the plasma concentration versus time profile of moxifloxcinin rats, $C_{max}$ was $11.151{\mu}g/mL$ at 5 min after the intravenous injection and $t_{1/2}$ was 2.936 h. Plasma concentration and kinetics in human were predicted and compared with observed datas. Moxifloxacin penetrated and accumulated with high concentrations in redmarrow, lung, skin, heart, liver, kidney, spleen, muscle tissues in human with intra-abdominal infection. The predicted tissue to plasma concentration ratios in abdominal viscera were between 1.1 and 2.2. When rat plasma concentrations were known, extrapolation of a PBPK model was a method to predict drug pharmacokinetics and penetration in human. Moxifloxacin has a good penetration into liver, kidney, spleen, as well as other tissues in intra-abdominal infected human. Close monitoring are necessary when using moxifloxacin due to its high concentration distribution. This pathological model extrapolation may provide reference to the PK/PD study of antibacterial agents.
LiQin Zhu,JianWei Yang,Yuan Zhang,YongMing Wang,JianLei Zhang,YuanYuan Zhao,WeiLin Dong 대한약리학회 2015 The Korean Journal of Physiology & Pharmacology Vol.19 No.2
The aim of this study is to develop a physiologically based pharmacokinetic (PBPK) model in intraabdominalinfected rats, and extrapolate it to human to predict moxifloxacin pharmacokinetics profilesin various tissues in intra-abdominal infected human. 12 male rats with intra- abdominal infections,induced by Escherichia coli, received a single dose of 40 mg/kg body weight of moxifloxacin. Bloodplasma was collected at 5, 10, 20, 30, 60, 120, 240, 480, 1440 min after drug injection. A PBPK modelwas developed in rats and extrapolated to human using GastroPlus software. The predictions wereassessed by comparing predictions and observations. In the plasma concentration versus time profileof moxifloxcinin rats, Cmax was 11.151 μg/mL at 5 min after the intravenous injection and t1/2 was2.936 h. Plasma concentration and kinetics in human were predicted and compared with observed datas. Moxifloxacin penetrated and accumulated with high concentrations in redmarrow, lung, skin, heart,liver, kidney, spleen, muscle tissues in human with intra-abdominal infection. The predicted tissue toplasma concentration ratios in abdominal viscera were between 1.1 and 2.2. When rat plasma concentrationswere known, extrapolation of a PBPK model was a method to predict drug pharmacokineticsand penetration in human. Moxifloxacin has a good penetration into liver, kidney, spleen, as well asother tissues in intra-abdominal infected human. Close monitoring are necessary when using moxifloxacindue to its high concentration distribution. This pathological model extrapolation may provide referenceto the PK/PD study of antibacterial agents.
Meng Yuan,Yu Cao,Haoyang Zheng,Kunlin Chen,Yuping Lu,Jing Wang,Liqin Zhu,Ming Chen,Zhipeng Cai,Yonggen Shen 한국식품과학회 2024 Food Science and Biotechnology Vol.33 No.7
This study used glucose, fructose, maltose and dextran to explore the effects of different carbohydrates on the Maillard reaction of casein phosphopeptides (CPP). The color parameter results showed that heating time from 1 to 5 h led to brown color, which was consistent with the observed increased in browning intensity. Fourier transform infrared spectroscopy results verified that four carbohydrates reacted with CPP to produce Maillard conjugates. Fluorescence spectroscopy showed that the Maillard reaction changed the tertiary structure of CPP by decreasing the intrinsic fluorescence intensity and surface hydrophobicity compared with the CPP-carbohydrate mixture. At the same time, the Maillard reaction effectively improved the emulsifying properties, reducing power and DPPH radical scavenging activity of CPP. Furthermore, this study also found that glucose and fructose improved CPP more than maltose and dextran. Therefore, monosaccharides have good potential in modifying CPP via the Maillard reaction.