[The pharmacokinetics of rhein in 12 healthy volunteers after oral administration of rhubarb extract].
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To study the pharmacokinetics of rhein in 12 healthy volunteers after oral administration of rhubarb extract.The blood sample were obtained at 0,0.083,0.5,1,1.5,2,3,4,5,7,10 h after a single dose oral administration of rhubarb (50 mg x kg(-1)). The plasma rhein concentration was determined by HPLC. The pharmacokinetics of rhein were analysed by 3P97 program.The absorption of rhein was very fastafter oral administration of rhubarb extract in the healthy volunteers. The main pharmacokinetic parameters of rhein were C(max) (3.20 +/- 1.08) microg x mL(-1); t(max) (1.03 +/- 0.41) h; t(1/2alpha) (0.21 +/- 0.02) h; t(1/2beta) (2.68 +/- 1.09) h; MRT(5.31 +/- 1.78) h; AUC(0-infinity) (1 573.08 +/- 366.48) microg x mL(-1) min(-1), respectively.Rhein could be absorbed rapidly and its pharmacokinetics was consistent with two-compartment model.Cite
Objective:To establish a HPLC method for measurement of serum concentration of sinomemine in rabbits and explore it’s pharmacokinetics. Methods:6 rabbits were intragastricly administrated sinomenine with the dosage of 45mg/kg,2 ml blood were collected at 0.25h、0.5h、1.0h、1.5h、2.0h、3.0h、4.0h、6.0h、8.0h、10.0h and 12.0h after oral administration.concentrations of drug were determined by HPLC,datas were calculated with 3P97 software and pharmacokinetics was explored. Results:T1/2(Ka) was(0.31±0.26)h,T1/2(Ke) was(3.15±0.82)h,Tmax was(1.05±0.53)h,Cmax was(15.09±4.15)μg/ml,AUC0→∞ was(84.27±13.02)(μg·h)/L,AUC0→T was(78.29±13.46)(μg·h)/L. Conclusion:absorption and elimination of Sinomenine were quickly and Tmax is short,concentration of drug is high in rabbits after intragastric administration.
Sinomenine
Drug Administration
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OBJECTIVE To investigate the pharmacokinetics of faropenem in multiple doses to Chinese healthy volunteers.METHODS The drug concentration was detected by HPLC-UV in human plasma and urine.10 volunteers were given with multi-dose faropenem,300 mg each time.The pharmacokinetics parameters were calculated by DAS 1.0.RESULTS The main pharmacokinetics parameters as follow:t1/2 was(1.008±0.205)h;tmaxwas(0.925±0.426)h ;Cmaxwas(4.933±1.323)g·m-1;AUC0-t was(8.732±4.713)g·h·mL-1.The original drug in human urine account for(2.873±3.637)%.CONCLUSION No accumulation in human body was observed after 5 day administrations.The steady state was formed at the 4th day after oral administration.
Oral dose
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Vitexin was isolated from the leaves of Crataegus pinnatifida Bge. var major, and its pharmacokinetics and bioavailability were carried out via validated high-performance liquid chromatography (HPLC) method using hesperidin as internal standard in healthy rats after intravenous and oral administration at a dose of 10 mg/kg and 30 mg/kg, respectively. The pharmacokinetic parameters were calculated by both compartmental and non-compartmental approach. When intravenous administration was usedi¼Œthe elimination half-life (t1/2β), the mean residence (MRT0→t), the total body clearance (CL) were 46.01 ± 0.810 min, 26.23 ± 1.51 min and 0.031 ± 0.035 L/kg·min. When oral administration was used, the tmax and Cmax were 15.82 ± 0.172 min and 0.51 ± 0.015 μg/ml, the MRT0→t and CL were 60.41 ± 5.41 min and 0.71 ± 0.056 L/kg·min. The result showed that vitexin was rapidly eliminated and presented a low absolute bioavailability (F), 4.91 ± 0.761%.
Key words: Bioavailability, high-performance liquid chromatography (HPLC), pharmacokinetics, rat plasma, vitexin.
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Objective To study the pharmacokinetics of ferulic acid (FA) in plasma of the healthy female volunteers after oral administration of Shenghua decoction.Methods Using p-hydroxybenzaldehyde as the internal standard, the plasma concentration of FA was determined by RP-HPLC. Plasma samples were extracted and treated with boiling water and 3P97 programme was used to calculate the pharmacokinetic parameters. Results The main pharmacokinetic parameters of FA were as follows: T1/2α=18.72 min ,T1/2β=79.21 min,T1/2 Ka=11.19 min,AUC=18004.87 μg·min·L-1,CL=0.17L·min-1·kg-1,Cmax=206.30 μg·L-1, Tpeak=22.78 min.Conclusion After oral administration of Shenghua decoction, FA could be absorbed and eliminated rapidly and pharmacokinetics of FA conforms to a two-compartment open model.
Decoction
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Decoction
Elimination rate constant
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The pharmacokinetics of puerarin was studied in 7 heal-thy volunteers after a single iv 5 mg/kg by RP-HPLC with fluorescencedetection. The plasma concentration-time data was fitted by the nonlinearregression automatic program and showed to be subjected to two-compar-tments open model. The plasma concentration-time average equation ofhealthy volunteers is Ct= 28. 42e~(-0.0758t)+11.47e~(-0.0095t), the importantparameters t1/2α=10. 3± 4. 1 min, t1/2β= 74.0±11.1 min, V_1=0.132± 0. 0361l/kg, CL=0.0032 ±0.0008 l/(kg·min), MRT= 1. 28±0. 10h;
Puerarin
Plasma levels
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Objective To explore the effects of preparation technology and different compositions on the pharmacokinetic of emodin by comparison its pharmacokinetic parameters from Sanhuang tablets and crude drug rhubarb.Methods Sprague Dawley rats were randomly divided into two groups:Sanhuang tablet group and rhubarb group (each n=5).The rats were administrated with Sanhuang tablets and Rhubarb (intragastric,i.g),respectively.Blood samples were collected at different time points from tail veins.The plasma concentrations of emodin were measured by the established RP-HPLC method.The pharmacokinetic parameters and the pharmacokinetics of dimensional model were determined by pharmacokinetic program 3P87.Results The pharmacokinetic character of emodin fitted two-compartment open model.The pharmacokinetic parameters were as follows:Sanhuang tablets:Cmax/μg·ml-1=3.528±0.72,t1/2(a)/h=1.429±0.201,t1/2(β)/h=4.620±0.536,t1/2(Ka)/h-1=0.405±0.097,Tmax/h=1.520±0.210,AUC0-∞/μg·h·ml-1=31.297±2.001,CL(s)/L·h-1·kg-1=0.018±0.002,Lag time/h=0.041±0.006;rhubarb group:Cmax/μg·ml-1=2.547±0.214,t1/2(a)/h= 1.501±0.929,t1/2(β)/h=4.598±0.541,t1/2(Ka)/h-1=0.389±0.101,Tmax/h=1.478±0.243,AUC0-∞/μg·h·ml-1=26.729±3.010,CL(s)/L·h-1·kg-1=0.024±0.002.Conclusions Compared with emodin in Sanhuang tablets,the emodin in rhubarb shows improved absorption,prolonged distribution time and peak time,reduced plasma clearance and better bioavailability,which is possibly related to the interaction of other components and the technology of the preparation.
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Objective To investigate the pharmacokinetics and safety of single dose of pitavastatin calcium tablets in Chinese healthy volunteers.Methods Twelve volunteers were divided into three groups by 3×3 design.The drug concentrations of plasma sample from the twelve volunteers after taking 1,2 and 4 mg pitavastatin calcium tablets respectively were determined by LC-MS/MS.The pharmacokinetic parameters were calculated by Das 2.0 software.Results The main pharmacokinetic parameters of pitavastatin after single oral doses(1 mg,2 mg and 4 mg)were as follows:t1/2β were(11.39 ±7.66),(10.00±7.30),(11.30±7.95)h;tmax were(0.83±0.29),(0.73±0.20),(0.85±0.46)h;Cmax were(30.48±11.66),(60.80±22.97),(120.98±35.51)ng·mL-1;AUC0→72 h were(93.19±26.61),(179.46±52.86),(364.37±94.74)ng·mL-1·h;AUC0→∞ were(96.70±27.42),(183.34±53.62),(372.86±95.84)ng·mL-1·h.The pharmacokinetic parameters such as Cmax,AUC0→72h,AUC0→ ∞ directly proportion to doses.There were no significant difference in K10,tmax,t1/2β,MRT0→72h,MRT0→ ∞,CL/F,V/F of three groups by analysis of variance.Conclusion The pharmacokinetics of pitavastatin in the dosage of 1-4 mg in human body nearly fit linear dynamic feature.The main pharmacokinetic parameters are similar to those in the reported literature.
Pitavastatin
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Diacerein is a symptomatic slow-acting drug used for treating osteoarthritis. This drug is completely metabolized into the active metabolite rhein before reaching the systemic circulation. This study evaluated the effects of food on the pharmacokinetics of rhein released from diacerein in healthy Chinese subjects. This was a single-center, randomized, single-dose, open-label, two-period, cross-over study. Twenty-four healthy subjects were randomly selected to receive a single oral dose of 50 mg diacerein capsule in either fasted or fed state on two separate visits. Plasma samples were analyzed with LC-MS/MS. Pharmacokinetic parameters were calculated using WinNonlin software. In the fasted and fed states, the main pharmacokinetic parameters of diacerein capsule were as follows: Cmax were (4471 ± 936), (3225 ± 755) ng/mL, t1/2 were (4.22 ± 0.42), (4.19 ± 1.05) h, tmax were (2.61 ± 1.25), (3.81 ± 1.29) h, AUC0-24 h were (24223 ± 4895), (24316 ± 5856) h·ng/mL, and AUC0-∞ were (24743 ± 5046), (25170 ± 6415) h·ng/mL. The absorption rate of diacerein capsule was obviously delayed by food intake but the absorption degree remained unaffected.
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Objective:To determine parameters of pharmacokinetics in healthy volunteers,provide a scientific basis for clinical application of Yinhuang compound microenema.Method:HPLC was used to determine the concentrations of chlorogenic acid and baicalin in the plasma samples of healthy volunteers,then analyze these data by the pharmacokinetics program 3P97 to determine the parameters of pharmacokinetics and the compartmental model for both ingredients inYinhuang compound microenema.Result:Baicalin showed two compartment model in healthy volunteers and the main parameters of pharmacokinetics were as follows:T1/2α of 0.325 h,T1/2β of 2.370 h,AUC of 6.236×10~(-3) g·h·L~(-1),Tm of 0.247 h,Vd of 2.314 L;chlorogenic acid showed two compartment model in healthy volunteers and the main parameters of pharmacokinetics were as follows:T1/2α of 0.106 h,T1/2β of 1.641 h,AUC of 1.514×10~(-2)g·h·L~(-1),Tm of 0.267h,Vd of 2.423 L.Conclusion:The main components in Yinhuang compound microenema,baicalin and chlorogenic acid,were absorbed quickly and completely after rectal administration.
Baicalin
Chlorogenic Acid
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