The pharmacokinetic profile of gallocatechin-7-gallate (J10688) was studied in rats after intravenous administration. Male and female Sprague-Dawley (SD) rats received 1, 3, and 10 mg/kg (i.v.) of J10688 and plasma dr...The pharmacokinetic profile of gallocatechin-7-gallate (J10688) was studied in rats after intravenous administration. Male and female Sprague-Dawley (SD) rats received 1, 3, and 10 mg/kg (i.v.) of J10688 and plasma drug concentrations were determined by a high performance liquid chromatography-mass spectrometry (LC-MS) method. The pharmacokinetic software Data Analysis System (Version 3.0) was used to calculate the pharmacokinetic parameters. For different i.v. doses of J10688, the mean peak plasma concentration (C-0) values ranged from 11.26 to 50.82 mg/L, and mean area under the concentration -time curve (ALC(0-i)) values ranged from 1.75 to 11.80 (mg ' h/L). J10688 lacked dose dependent pharmacokinetic properties within doses between 1 and 10 mg/kg, based on the power model. The method developed in this study was sensitive, precise, and stable. The pharmacokinetic properties of J10688 in SD rats were shown to have rapid distribution and clearance values. These pharmacokinetic results may contribute to an improved understanding of the pharmacological actions of J10688. (C) 2016 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.展开更多
目的研究大鼠多剂量sc丹红注射液后丹酚酸B的药动学。方法将Wistar大鼠分为3组,分别于尾sc低、中、高剂量(1.25、2.5、5.0 m L·kg-1)丹红注射液,用LC-MS/MS法测定给药后不同时间点丹酚酸B的血药浓度,并采用DAS 2.0软件以非房室模...目的研究大鼠多剂量sc丹红注射液后丹酚酸B的药动学。方法将Wistar大鼠分为3组,分别于尾sc低、中、高剂量(1.25、2.5、5.0 m L·kg-1)丹红注射液,用LC-MS/MS法测定给药后不同时间点丹酚酸B的血药浓度,并采用DAS 2.0软件以非房室模型计算药动学参数。结果注射低、中、高剂量后,大鼠体内丹酚酸B的Cmax分别为1.8071、3.6004、7.3480μg·m L-1,AUC0-t分别为0.4927、0.9926、1.9145μg·m L-1·h,t1/2分别为1.34、1.64、1.42 h;Cmax、AUC0-t与剂量呈线性关系,t1/2与剂量无明显相关性。结论静脉注射丹红注射液后,丹酚酸B在大鼠体内的药动学行为与剂量呈线性。展开更多
Azithromycin and Chinese medicine forsythia are often used together to treat pediatric mycoplasma infections in China. We aimed to investigate the pharmacokinetic interaction of Forsythia suspensa extract and azithrom...Azithromycin and Chinese medicine forsythia are often used together to treat pediatric mycoplasma infections in China. We aimed to investigate the pharmacokinetic interaction of Forsythia suspensa extract and azithromycin after single and co-intravenous administration in rats. Male Sprague-Dawley rats received single(Forsythia suspensa extract or azithromycin) treatment or co-administration of Forsythia suspensa extract and azithromycin. Blood samples were collected at scheduled times, and drug concentrations were determined by HPLC-UV or HPLC-MS/MS methods. Both non-compartmental analyses and nonlinear mixed-effects modeling approaches were applied to fit pharmacokinetic data and evaluate the impact of co-administration. Pharmacokinetic analysis showed that the area under the curve of azithromycin and forsythiaside increased, and clearance decreased significantly(P < 0.05),after co-administration. The in vivo behavior of both azithromycin and forsythiaside could be appropriately described by the two-compartmental model. The final population pharmacokinetic model indicated that co-administration decreased the central volume of azithromycin and forsythiaside clearance significantly. Co-administration of Forsythia suspensa extract and azithromycin significantly decreased the clearance and increased exposure for both drugs. Pharmacokinetic data suggest that drug co-administration may increase efficiency.展开更多
Two different salts of diclofenac,diclofenac sodium and diclofenac potassium,in tablet dosage form were tested for their bioavailability and disposition kinetics in a group of eighteen rabbits in normal and experiment...Two different salts of diclofenac,diclofenac sodium and diclofenac potassium,in tablet dosage form were tested for their bioavailability and disposition kinetics in a group of eighteen rabbits in normal and experimentally induced dehydrated conditions with a wash out period of 7 days between both stages of study.Biochemical and physiological parameters were also measured in both normal and dehydrated states.Diclofenac levels in plasma were determined using a validated reversed phase HPLC method.Primary kinetic parameters i.e.AUC0-∞,Cmax,Tmax and other disposition kinetics were obtained with non-compartmental procedure.Biochemical parameters i.e.packed cell volume,plasma glucose and total lipid concentration in dehydrated rabbits increased significantly.Plasma concentration of diclofenac sodium and diclofenac potassium decreased significantly in water deprived rabbits.In comparison,diclofenac potassium in normal and dehydrated state of the same group of rabbits showed a significantly increased plasma concentration when compared with diclofenac sodium.展开更多
基金supported by Beijing Natural Science Foundation(7152103)the National Great Science and Technology Projects(2014ZX09507003-002 and 2012ZX09301002-2013HXW-11)the International Collaboration Project(2011DFR31240)
文摘The pharmacokinetic profile of gallocatechin-7-gallate (J10688) was studied in rats after intravenous administration. Male and female Sprague-Dawley (SD) rats received 1, 3, and 10 mg/kg (i.v.) of J10688 and plasma drug concentrations were determined by a high performance liquid chromatography-mass spectrometry (LC-MS) method. The pharmacokinetic software Data Analysis System (Version 3.0) was used to calculate the pharmacokinetic parameters. For different i.v. doses of J10688, the mean peak plasma concentration (C-0) values ranged from 11.26 to 50.82 mg/L, and mean area under the concentration -time curve (ALC(0-i)) values ranged from 1.75 to 11.80 (mg ' h/L). J10688 lacked dose dependent pharmacokinetic properties within doses between 1 and 10 mg/kg, based on the power model. The method developed in this study was sensitive, precise, and stable. The pharmacokinetic properties of J10688 in SD rats were shown to have rapid distribution and clearance values. These pharmacokinetic results may contribute to an improved understanding of the pharmacological actions of J10688. (C) 2016 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.
文摘Azithromycin and Chinese medicine forsythia are often used together to treat pediatric mycoplasma infections in China. We aimed to investigate the pharmacokinetic interaction of Forsythia suspensa extract and azithromycin after single and co-intravenous administration in rats. Male Sprague-Dawley rats received single(Forsythia suspensa extract or azithromycin) treatment or co-administration of Forsythia suspensa extract and azithromycin. Blood samples were collected at scheduled times, and drug concentrations were determined by HPLC-UV or HPLC-MS/MS methods. Both non-compartmental analyses and nonlinear mixed-effects modeling approaches were applied to fit pharmacokinetic data and evaluate the impact of co-administration. Pharmacokinetic analysis showed that the area under the curve of azithromycin and forsythiaside increased, and clearance decreased significantly(P < 0.05),after co-administration. The in vivo behavior of both azithromycin and forsythiaside could be appropriately described by the two-compartmental model. The final population pharmacokinetic model indicated that co-administration decreased the central volume of azithromycin and forsythiaside clearance significantly. Co-administration of Forsythia suspensa extract and azithromycin significantly decreased the clearance and increased exposure for both drugs. Pharmacokinetic data suggest that drug co-administration may increase efficiency.
文摘Two different salts of diclofenac,diclofenac sodium and diclofenac potassium,in tablet dosage form were tested for their bioavailability and disposition kinetics in a group of eighteen rabbits in normal and experimentally induced dehydrated conditions with a wash out period of 7 days between both stages of study.Biochemical and physiological parameters were also measured in both normal and dehydrated states.Diclofenac levels in plasma were determined using a validated reversed phase HPLC method.Primary kinetic parameters i.e.AUC0-∞,Cmax,Tmax and other disposition kinetics were obtained with non-compartmental procedure.Biochemical parameters i.e.packed cell volume,plasma glucose and total lipid concentration in dehydrated rabbits increased significantly.Plasma concentration of diclofenac sodium and diclofenac potassium decreased significantly in water deprived rabbits.In comparison,diclofenac potassium in normal and dehydrated state of the same group of rabbits showed a significantly increased plasma concentration when compared with diclofenac sodium.
