TongMai Granules is a Chinese medicine patent drug to treat cardiovascular diseases.It is prepared from the water extract of Dan-shen,Chuan-xiong and Ge-gen.The main compounds of TongMai Granules are isoflavone glycos...TongMai Granules is a Chinese medicine patent drug to treat cardiovascular diseases.It is prepared from the water extract of Dan-shen,Chuan-xiong and Ge-gen.The main compounds of TongMai Granules are isoflavone glycosides,isoflavones,and phenolic acids.However,it is difficult to detect low-polar compounds such as tanshinones and phthalides though they may also contribute to the therapeutic effect.In this work,an off-line two-dimensional chromatography method was developed to enrich the minor constituents in TongMai Granules.The extract was subjected to an SEP-PAK silica SPE column and eluted with petroleum ether,ethyl acetate–methanol(6:1,v/v),and methanol,successively.The three fractions were then analyzed using ultra-high performance liquid chromatography coupled with orbitrap mass spectrometry(UHPLC/orbitrap-MS).The isoflavones from Ge-gen,phenolic acids from Dan-shen and phthalides from Chuan-xiong were distributed in different fractions.A total of 131 compounds,including 59 from Ge-gen,26 from Dan-shen,43 from Chuan-xiong,and 3 common ones from Dan-shen and Chuan-xiong were tentatively identified.Among them,26 compounds were identified by comparing with reference standards.This study set a good example for comprehensive analysis of the constituents in traditional Chinese medicine formula.展开更多
In the present study,we aimed to investigate the pharmacokinetics and dosage proportionality for a single,intravenous utilization of Pazufloxacin Mesilate Sodium Chloride,an injectable synthetic fluoroquinolone antiba...In the present study,we aimed to investigate the pharmacokinetics and dosage proportionality for a single,intravenous utilization of Pazufloxacin Mesilate Sodium Chloride,an injectable synthetic fluoroquinolone antibacterial agent,in healthy Chinese volunteers.In this open-labeled,three-dosage parallel study,subjects were randomized to receive a single dose of Pazufloxacin Mesilate at 150,300 or 600 mg(n=10,10 and 10,respectively)administered as a 30-min intravenous infusion.Blood and urine samples were serially collected from 0 to 24 h after drug administration.Moreover,the sample’s drug concentrations were analyzed via validated RP-HPLC method.Subjects receiving a single dose of Pazufloxacin Mesilate 150,300 or 600 mg were in accordance with the two compartment model.The Cmax for each dosage group was 2.37±0.89,4.27±0.74 and 10.74±4.06 mg·mL(–1),respectively;and the AUC0→∞was 3.24±1.2,5.89±1.51 and 13.32±2.35 mg·h·mL–1,respectively.In addition,Tmax for groups treated with 150,300 and 600 mg was 0.48±0.08,0.50±0.00 and 0.53±0.08 h,respectively.The correlation analysis for AUC0→∞,Cmax and dosage suggested that pazufolxacin mesilate displayed dose proportion at the dose ranging from 150 to 600 mg.The data suggested that all three different dosage regimens fit with the two compartment model.Meanwhile,it presented a linear correlation between AUC0→∞,Cmax and dosage over the range of 150–600 mg.展开更多
基金National Key Research and Development Program of China(Grant No.2018YFC1707301,2018YFC1707304)。
文摘TongMai Granules is a Chinese medicine patent drug to treat cardiovascular diseases.It is prepared from the water extract of Dan-shen,Chuan-xiong and Ge-gen.The main compounds of TongMai Granules are isoflavone glycosides,isoflavones,and phenolic acids.However,it is difficult to detect low-polar compounds such as tanshinones and phthalides though they may also contribute to the therapeutic effect.In this work,an off-line two-dimensional chromatography method was developed to enrich the minor constituents in TongMai Granules.The extract was subjected to an SEP-PAK silica SPE column and eluted with petroleum ether,ethyl acetate–methanol(6:1,v/v),and methanol,successively.The three fractions were then analyzed using ultra-high performance liquid chromatography coupled with orbitrap mass spectrometry(UHPLC/orbitrap-MS).The isoflavones from Ge-gen,phenolic acids from Dan-shen and phthalides from Chuan-xiong were distributed in different fractions.A total of 131 compounds,including 59 from Ge-gen,26 from Dan-shen,43 from Chuan-xiong,and 3 common ones from Dan-shen and Chuan-xiong were tentatively identified.Among them,26 compounds were identified by comparing with reference standards.This study set a good example for comprehensive analysis of the constituents in traditional Chinese medicine formula.
基金the support of Laboratory of National Institution of Drug Clinical Trial,Xiangya Hospital,Central South University
文摘In the present study,we aimed to investigate the pharmacokinetics and dosage proportionality for a single,intravenous utilization of Pazufloxacin Mesilate Sodium Chloride,an injectable synthetic fluoroquinolone antibacterial agent,in healthy Chinese volunteers.In this open-labeled,three-dosage parallel study,subjects were randomized to receive a single dose of Pazufloxacin Mesilate at 150,300 or 600 mg(n=10,10 and 10,respectively)administered as a 30-min intravenous infusion.Blood and urine samples were serially collected from 0 to 24 h after drug administration.Moreover,the sample’s drug concentrations were analyzed via validated RP-HPLC method.Subjects receiving a single dose of Pazufloxacin Mesilate 150,300 or 600 mg were in accordance with the two compartment model.The Cmax for each dosage group was 2.37±0.89,4.27±0.74 and 10.74±4.06 mg·mL(–1),respectively;and the AUC0→∞was 3.24±1.2,5.89±1.51 and 13.32±2.35 mg·h·mL–1,respectively.In addition,Tmax for groups treated with 150,300 and 600 mg was 0.48±0.08,0.50±0.00 and 0.53±0.08 h,respectively.The correlation analysis for AUC0→∞,Cmax and dosage suggested that pazufolxacin mesilate displayed dose proportion at the dose ranging from 150 to 600 mg.The data suggested that all three different dosage regimens fit with the two compartment model.Meanwhile,it presented a linear correlation between AUC0→∞,Cmax and dosage over the range of 150–600 mg.
