Pharmacokinetic Study of Berberine Hydrochloride in Chickens
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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.Keywords:
Berberine hydrochloride
Hydrochloride
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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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Objective:To study the pharmacokinetics of minocycline hydrochloride in 10 Chinese healthy volunteers after a single intravenous administration of 200mg minocycline.Methods:Minocycline hydrochloride concentration in plasma was measured by an improved HPLC method,and the pharmacokinetic parameters were calculated.Results:After single dose administration of 200 mg minocycline,the main pharmacokinetic parameters t1/2,Cmax,tmax,AUC0→72h,AUC0→∞were(18.1±4.07) h,(4.744±0.887) mg/L,2.0 h,(75.71 ±10.68) mg·h/L,(79.90±12.81) mg·h/L,respectively.Conclusion:The main pharmacokinetic parameters of minocycline are consistent with those reported previously.
Minocycline
Hydrochloride
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The pharmacokinetics and bioavailability of enrofloxacin lactate were investigated in 24 healthy Suqin yellow chickens following single intravenous and oral(10 mg/kg b.w.) administration.The concentrations of enrofloxacin lactate were determined by high-performance liquid chromatography(HPLC) and the plasma concentration-time data was analyzed by the pharmacokinetic computer program 3p87.Following intravenous administration,the drug concentration-time data was best described by a two-compartment open model.The main pharmacokinetic parameters of enrofloxacin lactate were: t1/2α(0.45±0.16) h,t1/2β(7.02±1.42) h,CL(s)(0.38±0.10) mg/kg/h,AUC(23.69±5.56)(mg/L) ×h.The drug concentration-time data was best described by a two-compartment open model after oral administration with t1/2ka(0.60±0.01)h,t1/2ke(8.25±1.73)h,tpeak(2.44±0.17) h,Cmax(1.44±0.30) mg/L,AUC(20.74±3.80)(mg/L) ×h,F 87.54%.The results showed that the pharmacokinetic characteristics of enrofloxacin lactate in healthy Suqin yellow chickens manifested with the rapid absorption,wide distribution and slow elimination.The bioavailability was high by the oral routes.
Compartment (ship)
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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 pharmacokinetics and relative bioavailability of metformin hydrochloride sustained release capsule in healthy volunteers.METHODS The serum concentrations of 20 volunteers were determined by HPLC after a single and multiple oral doses of 1 000 mg of metformin hydrochloride capsule or reference metformin hydrochloride tablet in a randomized crossover design study.The pharmacokinetic parameters were calculated and the relative bioavailability and bioequivalence of two formulations were evaluated.RESULTS The pharmacokinetic parameters for test and reference drugs after a single oral dose were as follows:ρ_(max)(1.27±0.32) and(1.82±0.32)mg·L~(-1);t_(max)(5.0±1.62)and(2.95±0.72)h;AUC_(0～t)(13.53±3.87)and(12.36±2.24) mg·h·L~(-1);AUC_(0～∞)(14.44±4.09) and(12.66±2.34) mg·h·L~(-1),respectively.The relative bioavailability of the test preparation was(109.62±26.81)%.The pharmacokinetic parameters for test and reference preparations after multiple oral doses were as follows:ρ_(min)(0.10±0.05) and(0.33±0.09)mg·L~(-1);AUCss(12.28±2.73) and(8.59±2.01) mg·h·L~(-1);DF(239.68±30.98)% and(118.68±22.34)%.The relative bioavailability was(72.82±11.37)%. CONCLUSION The ρ_(max) of metformin sustained release capsules is lower and t_(max) is longer than those of regular ones.The results indicate that two formulations are bio-equivalent.
Bioequivalence
Metformin Hydrochloride
Capsule
Crossover study
Hydrochloride
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OBJECTIVE To study the pharmacokinetics of diltiazem hydrochloride sustained-release capsule in healthy volunteers.METHODS 60mg and 120mg diltiazem hydrochloride sustained-release capsules were given orally in a single dose to 12 healthy volunteers in a cross-over way.The diltiazem concentrations in serum were determined by RP-HPLC.The pharmacokinetic parameters were fitted and calculated by 3P87 program. RESULTS The main pharmacokinetics parameters of diltiazem hydrochloride sustained-release capsules after oral 60mg,120mg were as follows :T 1/2 K a( 0.60± 0.356),( 0.7± 0.4)h;T 1/2 K( 15.8± 2.7),( 13.9± 4.4)h;V( 33.2± 11.9),( 29.8± 11.8)L·kg -1;Cl( 1.4± 0.4),( 1.5± 0.5)L·h·kg -1;T max( 4.8± 0.9),( 4.6± 1.0)h;C max( 28.9± 10.8),( 65.6± 24.8)ng·ml -1;AUC( 751.2± 211.1),( 1487.4± 533.1)μg·h·L -1.CONCLUSIONS The parameters such as T 1/2 K, K , T max ,C max/D 0 and AUC/D 0 etc.in two kinds of dosage had no significant difference(P 0.05). It's pharmacokinetics were linear.
Diltiazem hydrochloride
Capsule
Hydrochloride
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Objective:To develop an LC-MS method to determine berberine and palmatin in rats plasma simultaneously.The method was employed to investigate pharmacokinetics of berberine and palmatin.Method: Blood samples were collected at different time after oral administration of extracts Rhizoma Coptidis,The plasma concentration of berberine and palmatin was determined by LC-MS.Pharmacokinetic parameters were calculated by WinNonlin 5.1 software.Result:The linear range of berberine and palmatin was 5～1 000 ng·mL(r=9 989),2.5～500 ng·mL-1(r=9 994) respectively.The average recovery of berberine and palmatin was exceeded 85%(n=5),the precision of inner-day and inter-day was less than 15%.The pharmacokinetics parameters calculated by noncompartment model,such as AUC,T1/2,Cmax of berberine were: 707.91 h.ng.mL-1,1 220.32 h.ng-1.mL-1,2 424.62 h.ng-1·mL-1;1.89 h,2.29 h,4.79 h;315.78 ng·mL-1,501.58 ng-1.mL-1,584.57 ng.mL-1;Tmax was all 1 h.The pharmacokinetics parameters AUC,T1/2.,Cmax of palmatin were: 130.29 h.ng-1·mL-1、348.61 h.ng-1.mL-1,872.76 h.ng-1·mL-1;1.71 h,2.64 h,5.89 h;Tmax was all 1 h.The relationship between dose and AUC showed good linearity.Conclusion: The method described in this report has high sensitivity and selectivity,and was suitable for pharmacokinetic studies of berberine and palmatin.The kinetic process of berberine in rats in vivo was fitted to a one-compartment model at low dosage,while it was fitted to two-compartment model at middle and high dosages;the kinetic process of palmatine was all fitted to a one-compartment model.
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t Objective:To study pharmacokinetics and relative bioavailability of fexofenadine hydrochloride capsules in healthy male volunteers.Method:A single oral dose of 120 mg fexofenadine hydrochloride capsule were adminis- trated to 20 healthy volunteers in a randomized cross-over design.Plasma concentration of fexofenadine hydrochlo- ride was determined by HPLC-fluorescence method,and pharmacokinetics and relative bioavailability were evalua- ted by DAS 1.0.Results:Main pharmacokinetic parameters for single dose were as follows:T_(max) were(2.55±0.72) h and (2.60±0.84 ) h;C_(max) were (370.8±84.7)μg·L~(-1) and (354.5± 88.3)μg·L~(-1);t_(1/2) were(5.34±1.15) h and(5.62±1.23)h;C1 were(51.0±8.1)L·h and(53.8±9.4)L·h;V_d were(390.6±96.8)L and(438.4± 122.4) L;MRT_(0-t),were (6.61±0.82 ) h and (6.56±0.87 ) h;AUC_(0-t) were (2290.1± 368.1)μg·h·L~(-1) and (2159.5±372.8)μg·h·L~(-1);AUC_(0-∞) were(2409.8±389.5)μg·h·L~(-1) and(2290.6±382.8)μg·h·L~(-1) for the test and reference drugs,respectively.Condusion:The relative bioavailability of the test drug is (107.6± 17.3)%.The test and reference drugs of fexofenadine hydrochloride capsules are bioequivalent.
Fexofenadine
Bioequivalence
Hydrochloride
Capsule
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OBJECTIVE To study the pharmacokinetics and relative bioavailability of Buspirone Hydrochloride tablets.METHODS Plasma levels of Buspirone were detected by HPLC.RESULTS The main pharmacokinetic parameters of the test and control drugs were as follows:Tmax were(0.87±0.18)h and(0.81±0.09)h,Cmax were(25.2±8.0)μg·L-1 and(25.1±7.9)μg·L-1,AUC0-t were(52.7±17.9)μg·h·L-1 and(51.9±17.2)μg·h·L-1,AUC0-∞ were(55.1±18.2)μg·h·L-1 and(54.9±17.0)μg·h·L-1,T1/2 were(2.8±0.5)h and(2.8±0.4)h,respectively.The relative bioavailability of the test tablet was(102.7±5.9)%.CONCLUSION The results of the statistical analysis show that the preparations are bioequivalent.
Bioequivalence
Hydrochloride
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OBJECTIVE To study the relative bioavailability between two products of ticlopidine hydrochLoride(tablet A,B).METHODS Healthy volunteers were orally given 500 mg of either ticlopidine hydrochloride in an open randomized cross-over test.The ticlopidine hydrochloride concentration in plasma was determined by HPLC method.RESULTS The peak time(t_(max)) of tablet A and B were((2.1)±(0.6))h and ((1.9)±(0.5))h,the pesk plassmaL levels(C_(max)) were((1 589.1)±(718.7))μg·L~(-1) and((1 520.8)±(678.1))μg·L~(-1),and AUC_(0→∞) were ((7 875.6)±(3 175.0))μg·h·L~(-1)和((8 146.1)±(3 391.0))μg·h·L~(-1) and tablet A to tablet B was((105.6)±(30.4))%.There were no significant differences in parameters C_(max),AUC_(0→∞) between two products (P(0.05)).CONCLUSION The two products of ticlopidine hydrochloride tablets are bioequivalent.
Bioequivalence
Ticlopidine
Hydrochloride
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