Aim To investigate the relation between pharmacokinetics and pharmacodynamics of dauricine in dogs with the combined PK-PD model. Methods The plasma drug concentration was determined by a validated reversed-phase HPLC method that entailed ultraviolet detector and the effects on cardiac electrophsiology; blood pressure and hemodynamics were recorded by polygraph. Results The main pharmacokinetic parameters T_(1/2?),T_(1/2?),V_d, and AUC were (0.049?0.016) h, (2.7?0.6) h, (15.8?3.5) L?kg~(-1),and (1.48?0.17) mg?h?L~(-1),respectively.The maximal increase in Q-Tc intervals was(25.5?9.4)%, whereas the maximal decrease in SBP,DBP,?(dp/dt)_(max) were (23.0?4.9)%,(21.9?5.9)%,(42.8?6.6)%, and(39.0?17.1)%, respectively.The peak effects were detected approximately 10～15 min later than the plasma concentration. Relation between effects and effect compartments was analyzed with the sigmoid-E_(max) model. Conclusion The relation between plasma concentrations,time and effects is established in beagle dogs.

AIM: To investigate the influence of Buxinqi Capsule (BXQ) on myocardial ischemia reperfusion injury in rats. METHODS: In this study, the experimental model was established by reperfusion for 60 minutes in rats after ligaturing left anterior descending coronary artery (LAD) for 30 minutes. Serum creatine phosphokinase (CPK), lactate dehydrogenase (LDH), superoxide dismutase (SOD) and malondialdehyodebis (MDA), area of myocardial infarction and occurrence of arrhymia were investigated. RESULTS: BXQ significantly decreased level of CPK and LDH and MDA, and obviously improved the activity of SOD, decreased reperfusion arrhythmias and arrhythmias severity index (ASI), and decreased the area of myocardial infarction. CONCLUSION: BXQ has protective effect on the damage of myocardia ischemia reperfusion in rats

The pharmacokinetics and relative bioavailability were studied in 18 healthy volunteers. A single oral dose of 150 mg irbesartan capsule (test) or tablet (reference) was given to each volunteer according to a randomized 2-way crossover study. The concentrations in plasma were determined by HPLC-UV method. The main parameters of irbesartan capsules were: Cmax: 1.502 +/- 0.295 micrograms/ml, tmax: 1.44 +/- 0.34 h, t 1/2: 20.21 +/- 14.71 h, AUC0-t: 11.087 +/- 3.443 micrograms/ml-1.h. The relative bioavailability of capsule to tablet was (101.4 +/- 28.9)%. The results of statistical analysis showed that two formulations were bioequivalent.
Biological Availability ; Biphenyl Compounds/blood ; Biphenyl Compounds/*pharmacokinetics ; Capsules ; Cross-Over Studies ; Receptors, Angiotensin/*antagonists & inhibitors ; Tablets ; Tetrazoles/blood ; Tetrazoles/*pharmacokinetics

The 3T3-L1 preadipocytes were used as carriers in the investigation of total extract, n-butanol extract, CB-1 and CB-2 of Coreopsis tinctoria Nutt. on cell proliferation and differentiation. Three groups at different doses were set for each of the four extract regions of C. tinctoria Nutt., respectively. MTT assay was used to detect 3T3-L1cell proliferation by four extract regions of C. tinctoria Nutt. Oil Red O staining was used to analyze the formation and accumulation of cytoplasmic lipid during cell differentiation. The results showed that compared with the control group, there were significant inhibition on cell proliferation when thetotal extract of C. tinctoriaNutt. at 100 μg·mL-1, n-butanol extract at 0.5, 5, and 50 μg·mL-1, CB-1 and CB-2 at 50 μg·mL-1 (P< 0.01). N-butanol extract showed certain dose-dependent manner (r = -0.903). Oil Red O staining showed that compared with the control group, thetotal extract of C. tinctoria Nutt. at 1, 10, 100 μg·mL-1 can obviously inhibit cell differentiation, reduce the formation of cytoplasmic lipid (P< 0.01). N-butanol extract can inhibit cell differentiation in a dose-dependent manner (r= -0.779). CB-1 and CB-2 obviously inhibited cell differentiation at the concentration of 50 μg·mL-1 (P < 0.01). It was concluded that thetotal extract, n-butanol extract, CB-1 and CB-2 of C. tinctoria Nutt. can inhibit the proliferation and differentiation of 3T3-L1 preadipocytes and reduce the formation of cytoplasmic lipid.

0 05). The main pharmacokinetic parameters are: C max : (2 31?0 16) ?g?L -1 and (2 44?0 20) ?g?L -1 ; T max : (48 75?12 99) min and (52 50?16 31) min; T 1/2ke : (92 93?11 86) min and (97 61?11 23) min; K e: (0 0079?0 0023) min -1 and (0 0084?0 0014) min -1 ; AUC (0～360 min) : (297 70?44 45) ?g?min?L -1 and (313 64?46.03) ?g?min?L -1 respectively in domestic and imported salcaltonin injections. The relative bioavailability of domestic formulation is 97 6%?25 6%. CONCLUSION The domestic and imported salcaltonin injections administered produce similar biological response and bioavailability and they are bioequivalent.

AIM　To compare the bioactivity and bioavailability of domestic and imported salcaltonin injections in Chinese healthy volunteers. METHOD　Using randomized cross design, to determine the concentrations of calcium and salcaltonin in serum of healthy volunteers after single dose of domestic and imported injections. RESULT　Two preparations reduced concentration of calcium in serum obviously and there was no difference of mean changes of calcium between the two kinds of injections (P>0.05). The main pharmacokinetic parameters are: Cmax: (2.31±0.16) μg*L-1 and (2.44±0.20) μg*L-1；Tmax: (48.75±12.99) min and (52.50±16.31) min；T1/2ke: (92.93±11.86) min and (97.61±11.23) min；Ke: (0.0079±0.0023) min-1 and (0.0084±0.0014) min-1；AUC(0～360 min): (297.70±44.45) μg*min*L-1 and (313.64±46.03) μg*min*L-1 respectively in domestic and imported salcaltonin injections. The relative bioavailability of domestic formulation is 97.6%±25.6%. CONCLUSION　The domestic and imported salcaltonin injections administered produce similar biological response and bioavailability and they are bioequivalent.

The pharmacokinetics and relative bioavailability were studied in 18 healthy volunteers. A single oral dose of 150 mg irbesartan capsule (test) or tablet (reference) was given to each volunteer according to a randomized 2-way crossover study. The concentrations in plasma were determined by HPLC-UV method. The main parameters of irbesartan capsules were: Cmax: 1.502 +/- 0.295 micrograms/ml, tmax: 1.44 +/- 0.34 h, t 1/2: 20.21 +/- 14.71 h, AUC0-t: 11.087 +/- 3.443 micrograms/ml-1.h. The relative bioavailability of capsule to tablet was (101.4 +/- 28.9)%. The results of statistical analysis showed that two formulations were bioequivalent.
Adult ; Angiotensin Receptor Antagonists ; Biological Availability ; Biphenyl Compounds ; blood ; pharmacokinetics ; Capsules ; Cross-Over Studies ; Humans ; Male ; Tablets ; Tetrazoles ; blood ; pharmacokinetics