Pharmacokinetics of 2 epimers of glycyrrhizic acid in rats
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Objective To determine the pharmacokinetic parameters of 2 epimers of glycyrrhizic acid (GL) after oral administration of α-GL and β-GL in rats.Methods α-GL and β-GL solvent were administered orally at a dose of 25 mg·kg-1.The concentration in the plasma was measured by HPLC method.Experimental data and the pharmacokinetic parameters were processed with the computer program DAS 2.0 and SPSS.Results The main pharmacokinetic parameters were:AUC0-36=(57.04±14.64)μg·mL-1·h;Cmax= (4.68±2.56)μg·mL-1 t1/2=(5.56±1.65)h,tmax=(10.0±4.0)h after oral administration of α-GL;AUC0-36=(36.55±13.18)μg·mL-1·h;Cmax=(4.24±1.69)μg·mL-1,t1/2=(7.88±2.40)h,tmax=(9.0±1.1)h respectively after oral administration of β-GL.Conclusion The main pharmacokinetic parameters of GA after the oral administration of α-GL and β-GL are different.Keywords:
Epimer
Oral dose
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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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An analytical method for the determination of stachydrine concentration in rabbits after oral administration with 4 % suspension of tablet powder was established. The pharmacokinetics in rabbits is a two compartment model. The main pharmacokinetic parameters are: C\- max is 6.29±0.84 μg/mL, T\- max is 3.36±0.64 h; T\- 1/2\+α is 5.35±3.79 h; T\- 1/2\+β is 32.38±24.33 h; AUC is 208.15±118.4 μg/(mL·h)
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Pharmacokinetics of a new derivative of ginkgolide B and its absolute bioavailability in Beagle dogs
Objective: To investigate the pharmacokinetics and absolute bioavailability of a new derivative of ginkgolide B(10-O-dimethylaminoethyl ginkgolide B,XQ-1H) in Beagle dogs.Methods: By applying double cycle self crossover design,a single dose of XQ-1H was administrated(3 mg·kg-1,iv or 7.5 mg·kg-1,ig) to 8 Beagle dogs.Blood samples were collected before and at different intervals after XQ-1H administration.The concentration of XQ-1H in dog plasma was determined by LC/ESI-MS method.The pharmacokinetic parameters were estimated by DAS 2.0 pharmacokinetic program.Absolute bioavailability was calculated.Results: The concentration-time curves of iv administration fitted to two compartment model.The t1/2β,AUC0-τ and AUC0-∞ were(10.84±2.10) h,(1 020.26±162.88) ng·mL-1·h and(1 111.76±165.57) ng·mL-1·h.The Tmax,Cmax,t1/2,AUC0-τ and AUC0-∞ of ig administration were(0.51±0.21) h,(752.24±224.80) ng·mL-1,(7.50±1.34) h,(2 069.05±516.80) ng·mL-1·h and(2 367.89±592.89) ng·mL-1·h,respectively.The mean absolute bioavailability of XQ-1H following ig administration was(81.87±19.20)%.Conclusion: The absolute bioavailability of XQ-1H in dogs is high,and the elimination of XQ-1H is slow.
Beagle
Crossover study
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OBJECTIVE To study the pharmacokinetics of Danshensu the chief active component in Rujiean.METHODS HPLC was used to determine Danshensu concentration in rabbits'serum at different time-points after oral administration.The pharmacokinetic parameter were calculated by 3P87.RESULTS The main pharmacokinetic parameters were as follows:ka(5.5±1.2)h-1,k(0.95±0.18)h-1,t1/2(0.75±0.12)h,Cmax(5.3±0.6)μg·mL-1,tmax(0.40±0.06)h,AUC0-t(6.3±1.2)μg·h·mL-1,AUC0-∞(7.0±1.3)mg·h·L-1.CONCLUSION The pharmacokinetics of Danshensu showed a rapid distribution and effect.The present research provided valuable data for advanced development of Rujiean.
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Several pharmacokinetics relative datas such as absorption, distribution, elimination and bioavailability have been set up in this study on pharmacokinetics of Norfloxacin in carp following different forms administration. Following single muscular injection and oral administration, the serum concentration the data of Norfloxacin in carp were best described by a two-compartment open model for dose of 10 mg Norfloxacin /kg body weight. Following single mixed in diet oral administration, the serum concentration-time data for Norfloxacin were best described as a one-compartment open model. The main pharmacokinetics parameters by muscular injection administration: AUC 24.9481 μg·h·mL-1, Cmaxl6.8992 μg·mL- 1, t1/2α 0. 1279 h, t1/2β 3.4032 h. The main pharmacokinetics prameters by orally administration: AUC 150.6029 μg·h·mL-l, Cmax5.7998 μg·mL-l, t1/2α3.407lh, t1/2β77. 1239h. The chief pharmacokinetics parameters by mixed in diet oral administered: AUC 6.8183 μg·h·mL- l, Cmax1 .7217μg·mL- l, t1/2ka 0.22643h,t1/2ke 2.0213h. The results showed that the main parameters following different forms administration were significantly different (P 0.01).
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Objective To study the pharmacokinetics and relative bioavailability of FNB-HP-β-CD complex in rats. Methods FNB and its HP-β-CD complex were administered orally to 2 groups of rats. The plasma fenofibric acid concentrations at different time intervals following the administration was determined by HPLC. The pharmacokinetic parameters were estimated by 3P97 pharmacokinetic program. Results The in vivo pharmacokinetic process in rats for FNB and its HP-β-CD complex followed the one-compartment open model. The main pharmacokinetic parameters were as follows: tmax were(6.67±3.50) h and(3.17±2.62) h, Cmax were(6.31±3.04) μg·mL-1 and(39.82±16.25) μg·mL-1, AUC0 ~ t were(81.36±51.00) μg·h·mL-1 and(462.74±196.68) μg·h·mL-1, AUC0 ~ ∞ were(90.34±51.72) μg·h·mL-1 and(483.90±260.92) μg·h·mL-1. There was significant difference in the pharmacokinetic parameters such as tmax, Cmax and AUC0 ~ ∞ between FNB and its HP-β-CD complex groups(P 0.01). The relative bioavailability of the FNB-HP-β-CD complex was 535.6%. Conclusion The absorption rate, especially the plasma drug peak concentration and bioavailability of the drug in rats are significantly increased when FNB is included with HP-β-CD.
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This article investigated the pharmacokinetics of berberine hydrochloride in chickens.The plasma concentration of berberine was determined by HPLC.The plasma concentration-time data of berberine hydrochloride was analyzed by Drug and Statistics(DAS).Following intravenous administration(3 mg·kg-1),the drug concentration-time data was best described by a three-compartment open model,t1/2β,t1/2γ,Vc,CL and AUC were(0.41±0.24) h,(3.66±1.06) h,(25.49±21.77)L·kg-1,(43.20±16.21)L·h-1·kg-1 and(78.92±30.58)μg·L-1·h respectively.The drug concentration-time data was best described by a two-compartment open model after oral administration of 50 mg·kg-1,t1/2α,t1/2β,t1/2ka,Tmax,Cmax and AUC were(1.87±0.76) h,(4.18±3.14) h,(0.89±0.46) h,(2.64±0.63) h,(4.09±0.11)μg·L-1 and(26.18±10.73)μg·L-1·h respectively.The absolute bioavailability was 2.03% after oral administration.Berberine hydrochloride had a low rate of bioavailability by oral administration,and its elimination was fast.
Berberine hydrochloride
Hydrochloride
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OBJECTIVE:To study the bioavailability of 2 kinds of cyclosporin A preparations in human body.METHODS:Two-stage and two-way cross over was adopted in this determination,the whole blood concentrations of 20 healthy volunteers were determined by HPLC after a single oral dose of 500 mg cyclosporin A oral solution(the testing drug)and cyclosporin A capsule(the reference drug).RESULTS:The main pharmacokinetic parameters of the testing drug and the reference drug were as follows,AUC0～24 were(15 033.4±3 474.9)(ng·h)/ml and(16 106.4±2 975.5)(ng·h)/ml;AUC0～∞were(16 755.5±3 827.5)(ng·h)/ml and(17 488.5±3 233.89)(ng·h)/ml;tmax were(2.05±0.58)h and(2.60±0.53)h;Cmax were(2 660.3±491.5)ng/ml and(2 665.5±527.1)ng/ml;t1/2 were(8.30±2.60)h and(7.15±2.09)h,respectively.The statistical analysis showed that the main pharmacokinetic parameters between the 2 preparations were of no great difference(P0.05)except that the tmax of the testing preparation was faster than that of the control drug.The relative bioavailability of the testing drug was(93.83±15.21)%.CONCLUSION:The AUC0～24,AUC0～∞and Cmax of 2 preparations are similar,but there is a significant difference in tmax.
Capsule
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Objective To investigate the pharmacokinetics of single dose pioglitazone hydrochloride tablets in Chinese healthy volunteers.Methods A single administration of 30 mg pioglitazone hydrochloride tablets was given to 24 healthy male volunteers.The concentration of pioglitazone and its two active metabolites(M-Ⅲ and M-IV)in human plasma were determined by HPLC-MS/MS.The main pharmacokinetic parameters were analyzed.Results The main pharmacokinetic parameters of pioglitazone were as follows:Cmax was(1504.9±447.8)ng·mL-1,tmax was(1.46±0.69)h,t1/2Ke was(7.58±3.21)h,AUC0-48 was(11.22±2.60)μg·h·mL-1.The main pharmacokinetic parameters of M-Ⅲ were as follows:Cmax was(249.4±82.7)ng·mL-1,tmax was(11.94±6.14)h,t1/2Ke was(20.09±4.13)h,AUC0-120 was(10.90 ±3.55)μg·h·mL-1.The main pharmacokinetic parameters of M-IV were as follows:Cmax was(487.2±108.6)ng·mL-1,tmax was(13.33±5.23)h,t1/2Ke was(21.07±3.99)h,AUC0-120 was(22.78 ±5.04)μg·h·mL-1.Conclusion The tmax of M-Ⅲ and M-IV was rough 12～13 h,the Cmax of M-Ⅲ and M-IV are 16% and 32% of Cmax of pioglitazone,respectively.the AUC0-120 of M-Ⅲ and M-IV are 97% and 203% of AUC0-48 of pioglitazone,respectively.
Pioglitazone
Hydrochloride
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Objective To study the pharmacokinetics of butylphathlide capsule in healthy volunteers.Methods Twelve healthy volunteers received 200 mg butylphathlide capsule at a single oral dose.The concentration of butylphathlide and butylphathlide metabolite-1 in plasma were determined by HPLC-MS/MS.The pharmacokinetic parameters were calculated by WinNolin program.Results After a single dose of 200 mg butylphathlide capsule,the pharmacokinetic parameters for butylphathlide and butylphathlide metabolite 1 were as follows: t1/2 were(10.35±0.79),(3.69±0.93) h;tmax were(1.23±0.73),(1.9±0.76) h;Cmax were(196.95±165.2),(1174.29±322.33) ng·mL-1;AUC0-t were(360.92±342.8),(5918.1±1627.51) h·ng·mL-1;CL/F were(977.03±664.06),(35.82±10.39) L·h-1.Conclusion Butylphthalide is rapid absorbed after oral administration,in addition to its original form,larger amount of metabolite could also be detected.
Capsule
Active metabolite
Oral dose
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